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Future Journal of Pharmaceutical Sciences 3 (2017) 33e45

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Future Journal of Pharmaceutical Sciences


journal homepage: http://www.journals.elsevier.com/future-journal-of-
pharmaceutical-sciences/

Pharmaceutical significance of Eudragit: A review


Ch. Niranjan Patra a, *, Richa Priya a, Suryakanta Swain b, Goutam Kumar Jena a,
Kahnu Charan Panigrahi a, Debashish Ghose a
a
Roland Institute of Pharmaceutical Sciences, Berhampur, 760010, India
b
SIMS College of Pharmacy, Guntur, India

a r t i c l e i n f o

Article history: tablet and capsule dosage forms. Films of different solubility can be
Received 19 September 2016 produced by using different polymer grades. Table 1 outlines the
Accepted 13 February 2017 solubility profile of each grade of Eudragit. Broadly poly-
Available online 9 March 2017 methacrylates are used as film former, tablet binder and tablet
diluents. Apart from the above applications, recent studies revealed
that polymethacrylates have got widespread applications in
formulation vis-a -vis taste masking, better permeation across skin,
intestinal epithelium and corneal permeation, dissolution
enhancement, bioavailability enhancement, enteric coating, sustain
1. Introduction
release, radioprotection, pH dependent release, colon targeting etc.
Therefore polymethacrylates play a pivotal role in formulation and
The Eudragit® range of polymers, like the versatile acrylic ma-
development of different type of dosage forms with versatile ap-
terial Plexiglas (introduced in 1933), grew out of Dr. Rohm’s deep
plications. Hence the objective of the present manuscript is to make
knowledge of acrylic acid and its derivatives. In the year 1954 first
a compilation review on research publications and patents on
two polymers Eudragit L and Eudragit S for enteric coating were
various applications of Eudragit.
launched. It offered a synthetic polymer for film-coating of
Polymethacrylates are known with various synonyms such as
improved quality than materials such as sugar and shellac. Eudragit
Acryl-EZE, Acryl-EZE MP, Eastacryl 30D; Eudragit; Kollicoat MAE 30
based products for rapidly disintegrating and sustained release
D; Kollicoat MAE 30 DP; polymeric methacrylates. This present
coatings were added during the 1960s, expanding the widening
review focused on various grades of Eudragit which is a trademark
potential applications considerably. The introduction of aqueous
of GmbH & Co.K.G Darmastadt in Germany, first marketed in 1950s.
polymer dispersion forms of Eudragit in 1972 was a major mile-
polymerization of acrylic & methacrylic acids or their esters was
stone, making the process of coating easier, safer, more versatile
adopted to obtain Eudragit e.g. butyl ester or dimethylaminoethyl
and economical. With the development of various grades of
ester. Chemical structure of Eudragit is shown in Fig. 1. Eudragit was
Eudragit, it became possible to handle many aspects of formulation
included in USPNF, BP and PhEur. Dry powder polymer forms are
development such as film coating, granulation, direct compression,
stable at temperatures less than 30  C. Dry powders are stable for at
melt extrusion and mastery of technologies to engineer immediate
least 3 years if stored in a tightly closed container at less than 30  C.
or sustained release, as well as GI targeting, enteric coatings, pulsed
Dispersions should be stored at temperatures between 5 and 25  C
release and transdermal formulations. Hence Eudragit a versatile
and are stable for at least 18 months. Eudragits are generally
polymer for drug delivery was selected for extensive review.
regarded as nontoxic and nonirritant materials. A daily intake of
Polymethacrylates are synthetic cationic and anionic polymers
2 mg/kg body-weight in humans is regarded as essentially safe. It is
of dimethylaminoethyl methacrylates, methacrylic acid, and
included in the FDA Inactive Ingredients Guide (oral capsules and
methacrylic acid esters in varying ratios. Several types are
tablets), nonparenteral medicines licensed in the UK, Canadian list
commercially available and may be obtained as the dry powder,
of acceptable nonmedicinal ingredients.
aqueous dispersion, organic solution [1]. The most commonly used
organic phase used was a (60:40) mixture of acetone and propan-2-
ol. Polymethacrylates are primarily used as film-coating agents in 2. Literature review

A comprehensive review of literature is discussed in length


* Corresponding author. Roland Institute of Pharmaceutical Sciences, Berhampur,
760010, Ganjam, Odisha, India.
highlighting their applications. Research articles reported for each
E-mail address: drniranjanrips@gmail.com (Ch.N. Patra). grade are enlisted in tabular form. Some of those articles are dis-
Peer review under responsibility of Future University. cussed critically with special reference to eudragit.

http://dx.doi.org/10.1016/j.fjps.2017.02.001
2314-7245/© 2017 Future University. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/
licenses/by-nc-nd/4.0/).
34 Ch.N. Patra et al. / Future Journal of Pharmaceutical Sciences 3 (2017) 33e45

Table 1
Tabulation for solubility of various grades of Eudragit [1].

Grades of Eudragit Recommended solvents Solubility/Permeability

Eudragit E12,5, Acetone, alcohol Soluble in gastric fluid to pH 5


Eudragit E100,
Eudragit EPO
Eudragit L 100-55, Acetone, alcohol for L100-55 Soluble in intestinal fluid from pH 5.5
Eudragit L 30 D-55, Water
Eastacryl 30D,
Kollicoat 30D
Kollicoat 30DP
Acryl EZE
Acryl EZE MP
Eudragit L-12.5P, Acetone, alcohol Soluble in intestinal fluid from pH 6
Eudragit L-12.5,
Eudragit L 100
Eudragit S 12.5P, Acetone, alcohol Soluble in intestinal fluid from pH 7
Eudragit S 12.5,
Eudragit S 100
Eudragit FS 30D Water
Eudragit RL12.5, Acetone, alcohol High permeability
Eudragit RL100,
Eudragit RD 100
Eudragit RL PO
Eudragit RL 30D Water
Eudragit RS 12.5 Acetone, alcohol Low permeability
Eudragit RS 100
Eudragit RS PO
Eudragit RS 30D Water
Eudragit NE 30D, Water Swellable, permeable
Eudragit NE 40D

2.1. Eudragit E100, E12,5 and EPO characteristic properties of Eudragit E series. They are commonly
used in film coating, odour and taste masking, moisture and light
In this series there are three different grades of Eudragit vis-a- protection. They differ from each other in terms of their physical
vis Eudragit E100, E12,5 and EPO. All the three are cationic copol- appearance. Eudragit S100 is available in the form of granules
ymer based on dimethylaminoethyl methacrylate, butylmethacry- which consists of colourless to yellow tinged granules with a
late and methyl methacrylate. Chemically they are known as characteristic amine like odour. Eudragit E 12,5 is available in the
poly(butyl methacrylate-co-(2-dimethylaminoethyl) methacrylate- form of organic solution which is a light yellow liquid of low vis-
co-methyl methacrylate. They possess a molecular weight of cosity, clear to slightly cloudy with characteristic odour of solvent.
approximately (47,000 g/mole), alkali value (180 mg KOH/g of Eudragit EPO is available in the form of powder with a character-
polymer) and glass transition temperature (48  C). They are soluble istic amine like odour.
in gastric pH up to 5.0. Low viscosity, high pigment binding ca- A current literature review on Eudragit E 100 reveals that it has
pacity, good adhesion and low polymer weight gain are the been used in nanoparticles, microparticles, transdermal spray,
ophthalmic solution, floating drug delivery system etc as shown in
Table 2. Quinteros et al. [2] proposed a novel ophthalmic solution
based on the ionic complexation between Eudragit E 100 and
flurbiprofen. Dispersion of the drug and Eudragit complex in 0.9%
w/v sodium chloride (NaCl) increased flurbiprofen release through
an ionic exchange, providing a controlled release and more effec-
tive corneal permeation without any irritation. Paradkar et al. [3]
formulated clotrimazole transdermal spray using different ratios
of ethanol and acetone and various grades of eudragit and ethyl
cellulose. The following parameters like viscosity, drying time,
stickiness, appearance, integrity on skin and water washability
were evaluated. The desired criteria was achieved by using Eudragit
E100 and mixture of ethanol and acetone (80:20). The optimized
formulation exhibited improved drug permeation through the rat
skin and improved antifungal efficacy as evidenced from higher
zone of inhibition. Dominguez et al., [4] prepared triclosan nano-
particles suspension by the emulsification-diffusion by solvent
displacement method, using Eudragit® E 100 as polymer. Triclosan
was molecularly dispersed in the nanoparticle batches containing
Fig. 1. Chemical structure of Eudragit, For Eudragit E: R1, R3]CH3, R2]
CH2CH2N(CH3)2, R4]CH3, C4H9 For Eudragit L and Eudragit S: R1, R3]CH3, R2]H,
triclosan. Nanoparticles exhibited higher permeation compared to
R4]CH3 For Eudragit FS: R1]H, R2]H, CH3, R3]CH3, R4]CH3 For Eudragit RL and solutions and creams. Patil et al. [5] explored the application of
Eudragit RS: R1]H, CH3, R2]CH3, C2H3, R3]CH3, R4]CH2CH2N(CH3)þ3Cl For Eudragit E 100 as taste masking agent in orally disintegrating tablet
Eudragit NE 30 D and Eudragit NE 40 D: R1, R3]H, CH3, R2, R4]CH3, C2H3 For Acryl- of tramadol hydrochloride. The results demonstrated successful
EZE and Acryl-EZE MP; Eudragit L 30 D-55 and Eudragit L 100-55, Eastacryl 30 D,
masking of bitter taste.
Kllicoat MAE 30D, and Kollicoat MAE 30 DP: R1, R3]H, CH3, R2]H, R4]CH3, C2H3.
Ch.N. Patra et al. / Future Journal of Pharmaceutical Sciences 3 (2017) 33e45 35

Table 2
Reported literature on Eudragit E 100, E 12,5 and EPO.

Drug name Dosage form/delivery system Method of Preparation Applications References

Eudragit E 100
Flurbiprofen Opthalmic aqueous solution Ionic complexation Constant rate of delivery and improved [2]
permeation
Clotrimazole Transdermal spray Eutectic mixture Improved drug transport across the skin [3]
Triclosan Nanoparticles Emulsification-diffusion by solvent Improved drug delivery [4]
displacement method
Tramadol Hydrochloride Orally disintegrating tablet Mass extrusion technique Bitter taste masking [5]
Carvidilol Nanoparticles Nanoprecipitation Improved therapeutic efficacy (Faster [10]
dissolution)
Ranitidine hydrochloride Floating microspheres Solvent evaporation method Improved absorption and [11]
bioavailability
Eudragit E 12,5
* * * * *
Eudragit EPO
Clindamycin HCl Oral disintegrating tablet Drug coated to MCC beads followed by Improved pediatric and geriatric [6]
coating of eudragit EPO suspension patient compliance by taste masking.
followed by compression
Osthole Solid dispersion Hot-melt extrusion Improved dissolution rate and [12]
bioavailability
Atorvastatin Amorphous solid dispersions Direct compression Improved bioavailability by increasing [7]
compressed to orally disintegrating its gastric solubility in a stable oral
tablet disintegration tablet
Bifendate solid dispersions Hot-melt extrusion Enhanced bioavailability [13]
Meloxicam Nanoparticles Nanoprecipitation method Improved anti-inflammatory activity [8]
compared to suspension.
Andrographolide pH sensitive nanoparticle suspension Nanoprecipitation technique Improved the oral bioavailability with [14]
shorter Tmax
Aciclovir and Minoxidil liposomes High-pressure homogenization Cationic polymers had a stabilising [9]
effect
Diclofenac sodium and Polycomplex matrices Interpolyelectrolyte complexes (IPEC) Considerable pH-sensitive swelling in [15]
Theophylline between countercharged polymers acidic and neutral media
*
No literature found.

No literature was found for Eudragit 12,5 in pubmed indexed 2.2. Eudragit L 100 and 12,5
journals. An extensive review on applications of Eudragit EPO
revealed that it can be used in formulations such as solid disper- Eudragit L 100 and L 12,5 are anionic copolymers based meth-
sions, orally disintegrating tablets, nanoparticles, nanosuspensions, acrylic acid and methyl methacrylic acid. Both the polymers possess
stabilization of liposomes, superior moisture protection for solid similar molecular weight 1,25,000 g/mol, acid value 315 mg KOH/g
dosage forms etc are shown in Table 2. Cantor et al. [6] explored of polymer and glass transition temperature greater than 150  C.
taste masking potential of Eudragit EPO by formulating orally dis- Targeted drug release area for both the polymer is jejunum and
integrating tablets of clindamycin HCl. Coating of Clindamycin HCl dissolves at pH above 6. They are used for effective and stable
with Eudragit EPO suspension subsequent compression into tablet coatings with fast dissolution in the upper bowel, granulation of
showed improved pediatric and geriatric patient compliance for drug substance in powder form for controlled release, site specific
clindamycin. Salmani et al. [7] investigated solubility and drug delivery in intestine etc. The only difference between these
bioavailability enhancement potential of orally disintegrating two grades is Eudragit L 100 is available in the form of solid powder
tablet compressed from solid dispersions of atrovastatin with with a faint characteristic odour whereas Eudragit 12,5 is a organic
Eudragit EPO. Solid dispersions significantly improved the disso- solution which is colourless and clear to slightly cloudy liquid with
lution of atrovastatin. In vivo study showed. 434% more bioavail- the characteristic odour of isopropyl alcohol.
ability than plain atrovastatin tablets. Khachane et al. [8] A current review on Eudragit L 100 exhibits that it has been used
investigated the potential of Eudragit EPO nanoparticles in in various formulations such as microspheres, microsponges,
improving therapeutic efficacy of meloxicam and compared with nanoparticles, liposomes, lipotomes, tablets etc for different ap-
conventional meloxicam suspension. Meloxicam loaded eudragit plications such as enteric coating, sustain release, insulin perme-
EPO nanoparticles were prepared by nanoprecipitation method. ation, bioavailability enhancement etc as shown in Table 3. Li et al.
Improved anti-inflammatory activity with lesser ulcerogenicity was [16] filled self nanoemulsifying drug delivery systems (SNEEDS) of
observes with optimized nanoparticles. Hasanovic et al. [9] insulin into Eudragit L100 based enteric coated capsules. A pH-
improved physicochemical properties of liposomes by using dependent insulin release profile was observed. In healthy fasted
cationic polymer i.e. chitosan and Eudragit EPO. 1,2-Dipalmitoyl-sn- rats, administration of SNEDDS produced a 2.7 and 3.4 fold
glycero-3-phosphocholine (DPPC) liposomes were prepared by enhancement in the relative bioavailability and glucose reduction,
high-pressure homogenization. Zeta potential and mean particle respectively. This study showed enhanced oral absorption and ef-
size revealed that the polymeric liposomes are stable. In the pres- ficacy of insulin. Sareen et al. 2014 [17] evaluated colon specific
ence of the drugs (acyclovir and minoxidil), the polymeric lipo- drug delivery potential of Eudragit L100 by formulating micro-
somes still showed constant particle size and zeta potential. ponges of curcumin. Release studies revealed that microsponges
Moreover, the coating of liposomes with chitosan or Eudragit EPO prevented the premature release of curcumin in upper GIT and
led to higher skin diffusion for both drugs. The interaction between specifically released the drug at colonic pH. Microsponges with
the skin (negatively charged surface) and liposomes (positively Eudragit L 100 can be used as a promising drug delivery system for
charged) was the probable reason for increased skin diffusion. treatment of ulcerative colitis. Hosny et al. [18] made a novel
36 Ch.N. Patra et al. / Future Journal of Pharmaceutical Sciences 3 (2017) 33e45

approach to overcome barriers for the treatment of osteoporosis by Bendas et al. [25] attempted extrusion-spheronization followed by
formulating enteric-coated alendronate sodium (ALS) nano- spray coating for leaky enteric-coated pellets of ranitidine HCl.
liposomes. Optimized nanoliposome coated with Eudragit L 100 Pellets were prepared using Eudragit L 30 D-55, combined with
successfully resisted the release of ALS in acidic environments and soluble lactose, PEG 8000 and surfactants (span 60 (hydrophobic)
enhanced the bioavailability in rabbits. Wilson et al., [19] prepared or tween 80 (hydrophilic). Leaky enteric coated pellets allowed the
and evaluated sustain release enteric coated tablets of pan- release of some amount of drug in gastric fluid.
toprazole. The prepared tablets were dip coated using an enteric Similarly an extensive up to date review on the polymer
coating polymer such as cellulose acetate phthalate and eudragit Eudragit L100-55 suggests that this can be used in the formulations
L100. The study revealed that the prepared tablets were able to for various applications such as pH responsive drug release, taste
sustain drug release into the intestine. The enteric coated pan- masking, drug release at intestine, radioprotection etc as shown in
toprazole tablets significantly reduced ulcer formation. No litera- Table 4. Lotikar et al. [26] designed multiparticulate dosage form of
ture found for Eudragit 12,5 in pubmed indexed journals. ketoprofen by extrusion and spheronization technique. It was
based on pH-responsive dual pulse release concept. Pellets were
coated with pH sensitive Eudragit L 100-55 and Eudragit S 100 for
2.3. Eudragit L 30 D 55 and L 100-55
site-specific drug release with lag time. The dual pulse release after
a lag time of 2 and 5 h was observed. The first dose release was
Eudragit L 30 D 55 is the aqueous dispersion of anionic polymers
established in pH 1.2 for a period of 2 h, followed by pH 6.8. The
with methacrylic acid as a functional group. It is a low viscosity
second dose pellets were passed through pH 1.2, pH 6.8 followed by
liquid of white color with faint characteristic odour. It is obtainable
pH 7.5 for the rest of the study. The authors concluded that mul-
in the form of aqueous dispersion (30%) whereas eudragit L 100-55
tiparticulate dosage form of ketoprofen was able to relieve circa-
is an anionic copolymer based on methacrylic acid and ethyl
dian symptoms of rheumatoid arthritis during midnight and early
acrylate. It is a white powder with a faint characteristic odour. Both
morning. Maniruzzaman et al. [27] prepared extrudes of cationic
grades of Eudragit have molecular weight 3,20,000 g/mol, acid
model drug propranolol HCl by extrusion and spheronization
value 315 mg KOH/g of polymer and glass transition temperature
technique with the anionic polymers Eudragit L100 and Eudragit
110  C. Targeted drug release area for both is duodenum and they
L100-55. Taste masking was determined by using e tongues.
dissolve at pH of 5.5. Both the polymers are used for effective and
Intermolecular interactions as the mechanism of successful taste
stable coating with fast dissolution in the upper bowel, controlled
masking was ascertained from FT-IR spectroscopy and NMR
release, site specific drug delivery in intestine etc.
studies. Aguilar et al. [28] used polyurethane and Eudragit® L100-
An up to date literature review on the applications of Eudragit L
55 as nanofiber by belectrospinning technique. The composite
30 D 55 polymer suggests that it has been used in the formulation
mat has adequate mechanical properties and in vitro cell biocom-
of microspheres, microparticles, film coated tablets, pellets, trans-
patibility indicating that the material can be used for drug eluting
dermal film, enteric coating etc with various objectives such as
stent cover application. De Barros et al. [29] designed a laminated
improving bioavailability, drug release at intestine, sustain release
polymer film formulation for enteric delivery of live vaccine and
etc as shown in Table 4. Nair et al. [23] evaluated four different
probiotic bacteria. Eudragit L 100-55 based polymeric laminate
polymers such as Eudragit L-30 D-55, hydroxy propyl methylcel-
successfully protected dried probiotic or vaccine live bacterial cells
lulose phthalate, cellulose acetate phthalate and Acryl-EZE® by
from SGF for 2 h, and subsequently released all viable cells within
formulating enteric coated tablets of esomeprazole magnesium
60 min of transfer into simulated intestinal fluid.
trihydrate. Tablets with 5% weight gain, failed disintegration test in
0.1 N HCl media. It was observed that 8% w/w enteric coating
passed disintegration test. Methacrylic polymers (Eudragit L 30 D 2.4. Eudragit S (S-100, 12,5 and FS 30 D)
55 and Acryl EZE) exhibited better dissolution rate than the cellu-
lose polymers. Naseem et al. [24] designed transdermal films of Eudragit S 100 and S 12,5 are anionic copolymers based on
tenoxicam with Eudragit L 30D55 along with permeation en- methacrylic acid and methyl methacrylate. Eudragit S100 is solid
hancers like polyethylene glycol (PEG) and propylene glycol (PG). A substance in the form of white powder with a faint characteristic
drag effect was observed due to interaction between tenoxicam and odour. Eudragit S12,5 is a colourless and clear to slightly cloudy
Eudragit L30D-55 leading to a delay of the tenoxicam release. liquid with characteristic odour of isopropyl alcohol. Both grades

Table 3
Reported literature on Eudragit L 100 and 12,5.

Drug name Dosage form/delivery system Method of Preparation Application Reference

Oral insulin Combination of Self nanoemulsifying DDS In-situ emulsification Enhancing the oral absorption and efficacy of insulin and [16]
& enteric coated capsules eudragit L 100 as a enteric polymer.
Curcumin Microsponge for colon targeting Quasi emulsion solvent diffusion Eudragit L 100 prevented the premature release of curcumin in [17]
method upper GIT.
Lacidipine Lyophilised Lipotomes filled into enteric Thin film hydration technique Lipotomes enhanced oral bioavailability and Eudragit L 100 as a [20]
coated capsules. enteric polymer.
Dipyridamole floating alginate beads combined with the Ionic cross linking and solid Prolonged stomach retention time due to CaCO3 and modified [21]
solid dispersion dispersion technique drug release due to Eudragit L100 and RLPO.
Alendronate Enteric-coated nanoliposomes Nanotechnology Resist the release of ALS in acidic environments and enhanced [18]
sodium (ALS) the bioavailability
Pantoprazole Delayed release tablets Wet granulation method Sustained release in intestine and significant reduction in ulcer [19]
followed by enteric coating formation
Insulin Thiolated eudragit based nanoparticles Nanotechnology Facilitate insulin permeation through the intestinal epithelium. [22]
with reduced glutathione.
Eudragit L 12,5
* * * * *
*
No literature found.
Ch.N. Patra et al. / Future Journal of Pharmaceutical Sciences 3 (2017) 33e45 37

Table 4
Reported literature on Eudragit L30 D-55 and L 100-55.

Drug name Dosage form/delivery Method Application References


system

Eudragit L 30D-55
Oral Chlorea Microparticles Spray dried technique An approach to a cold chain free and effective oral cholera vaccine. [30]
vaccine
Tenoxicam Transdermal self-adhesive Casting evaporation Sustain drug release [24]
films technique
Esomeprazole Enteric coated tablet Coating Better dissolution & stable for a period of 3 months. [23]
magnesium
trihydrate
Tamsulosin Controlled-release Extrusion/ Controlled release [31]
hydrochloride capsule spheronization method
Ranitidine leaky enteric-coated Extrusion- Maintain or increase the bioavailability of drugs that have a window of absorption [25]
hydrochloride pellets spheronization followed
by spray coating
Diclofenac sodium Enteric coated pellets Fluidized-bed coating The mixture of Eudragit NE30D and Eudragit L30D-55 could be used to prepare [32]
compressed into tablets enteric pellets.
Mycoplasma Microsphere Co spray drying Oral microspheres vaccine prepared by a co-spray drying method can provide [33]
hyopneumoniae effective protection against M M. hyopneumoniae infection in pigs.
oral vaccine
Eudargit L 100e55
Ketoprofen pH-responsive dual pulse Extrusion- To relieve circadian symptoms of rheumatoid arthritis during midnight and early [26]
multiparticulate dosage spheronization & Fluid morning
form bed coating.
Propranolol HCl Taste mask formulation Hot melt extrusion Drug polymer intermolecular interactions as the mechanism of successful taste [27]
(Single screw) masking.
Amifostine Enteric microcapsules Spray drying technique Oral administration of amifostine microcapsules provided effective radioprotection [34]
compared to the bulk drug.
Omeprazole Nanoparticles Ultrasonic dispersion Nanoparticles showed a strong pH-sensitive release in vitro. [35]
and diffusion
solidification
Gemcitabine Enteric Microparticles Double emulsion Oral absorption could be increased with mucoadhesive polymer [36]
method
Domperidone Oral disintegrating tablet Direct compression Fast and pH-dependent release [37]
method
Paclitaxel Nanofiber composite mat Electrospinning process pH dependent release of paclitaxel on duodenal stent cover application. [28]
Live bacterial cells Polymer film laminate Film casting Eudragit alone successfully protected dried probiotic or vaccine LBC from SGF for [29]
as attenuated 2 h, and subsequently released all viable cells within 60 min of transfer into SIF.
vaccines
Cinnarizine Microparticles Coacervation technique pH responsive drug release [38]
Insulin Enteric nanoparticles Complex coacervation Complex coacervation process using chitosan and Eudragit L100-55 polymers may [39]
method provide a useful approach for entrapment of hydrophilic polypeptides without
affecting their conformation.

have molecular weight, acid value and glass transition temperature sustain release potential of Eudragit S100 by formulating trans-
approximately 125,000 g/mol, 190 mg KOH/g polymer and >150  C dermal patches of donepezil using various polymers along with
respectively. Eudragit S 100 is available in the form of powder. plasticizer and penetration enhancer. Eudragit S100, Eudragit E100
Eudragit S 12,5 is available in the form of organic solution (12.5%). and HPMC were used as matrix forming agents in the formulation
Both grades dissolve at pH 7.0 and used for colon targeted drug of patches. They concluded that transdermal patch can extend the
delivery. release of donepezil for many hours with enhanced bioavailability.
Eudragit FS 30D is a milky white liquid of low viscosity with a Hence Eudragit S 100 can be used to extend release of domepezil in
faint characteristic odour. It is the aqueous dispersion of an anionic transdermal patches. Li et al. [16] evaluated colon specific drug
copolymer based on methyl acrylate, methylmethacrylate and delivery potential of Eudragit S 100 based enteric coating of model
methacrylic acid. It is insoluble in acidic media, but dissolves by salt drug. Enteric coating was achieved by applying Eudragit S 100 to
formation above pH 7.0. Apart from its enteric properties, its microencapsulated 5-Flurouracil and leucovorin coloaded with
dissolution at a higher pH value allows targeted colon drug de- folate-chitosan nanoparticles. When the pH value reached the
livery. Its molecular weight, acid value and glass transition tem- soluble threshold of Eudragit S-100, a constant and slow drug
perature are approximately 2,80,000 g/mol, 70 mg KOH/g polymer release was observed. Eudragit S100 can be used for selectively
and 48  C respectively. Due to low minimum film forming tem- targeting drugs to colon in the chemotherapy of colon cancer.
perature only small amounts of plasticizer are required to get a Nandy et al. [41] formulated and characterized delayed release
smooth film formation. It is available in the form of aqueous multi particulates system of indomethacin. Microspheres were
dispersion (30%). formulated by using a novel quasi emulsion solvent diffusion
A current review on recent research publications based on technique using combination of ethyl cellulose (EC) and Eudragit RS
Eudragit S 100 is described as follows. It is used in formulation of 100/Eudragit S100 . Drug release decreased significantly (p < 0.05)
transdermal patch, nanoparticles, microparticles, microballons, with increase in amount of Eudragit polymer. Therefore this
solid dispersions and spherical crystals. It has been used for various approach suggested that the combination of EC and Eudragit S100
applications such as colon specific drug delivery, sustain release, microspheres may be useful for the delivery of maximum amount
bioavailability enhancement, improvement in micromeritic prop- of indomethacin to the colon.
erties etc as shown in Table 5. Madan et al. [40] evaluated the No literature was found for Eudragit S 12,5 in pubmed indexed
38 Ch.N. Patra et al. / Future Journal of Pharmaceutical Sciences 3 (2017) 33e45

Table 5
Reported literature on Eudragit S 100, 12,5 and FS 30 D.

Drug name Dosage form/delivery Method of Preparation Application References


system

Eudragit S 100
Donepezil Transdermal Patches Solvent casting technique Extended release, enhanced bioavailability, avoids the first [40]
pass effect
5-fluourouacil (5- Nanoparticles Ionic gelation followed by solvent evaporation Selectively targeting drugs to colon in the chemotherapy of [16]
FU) and microencapsulated with method colon cancer.
leucovorin enteric polymers
Raloxifene Nanocapsules Interfacial deposition of preformed polymer Best activity was observed for RH-loaded Eudragit S100 [44]
hydrochloride nanocapsules after 72 h
Indomethacin Multi-particulates system Novel quasi emulsion solvent diffusion Combination of EC and Eudragit S100 delivered maximum [41]
in the form of microspheres technique amount of drug to colon.
Dextromethorphan Solid dispersion (modified Solvent evaporation method Solid dispersion of drug-Eudragit S 100 to overcome the [45]
in situ gelling alginate problems of dose dumping after the rupture of the pH
formulations). dependent alginate gels.
Nizatidine Encapsulated Emulsion solvent diffusion method Sustain release and increased residence time [46]
microballoons
5-Flurouracil Enteric coated dextran Dextran Microspheres by emulsification- Eudragit S100 retard the release of drug in gastric and [47]
microspheres crosslinking method and enteric coating by oil- intestinal pH and the drug released in colon due to the
in-oil solvent evaporation method. degradation of dextran by colonic enzymes.
Peptide Val-Leu- Enteric coated Double emulsion method followed by freeze Nanoparticles almost completely released at pH 7.4 after 8 h [48]
Pro-Val-Pro-Arg nanoparticles drying reduced blood pressure for more than 30 h
(VLPVPR)
Flurbiprofen Microspheres Oil/oil emulsification method Colon specific drug delivery [49]
Mebendazole Spherical crystals Solvent change method Spherical crystals with improved micromeritic properties. [50]
Eudragit S 12,5
* * * * *
Eudragit FS 30 D
Theophyline Multiparticulate (enteric Direct compression Delayed release property was preserved. [51]
coated with FS 30 D)
compressed in to tablets
Tartrazine (model Multiple-unit tablet Film coating technique An optimal coating was obtained by mixing two acrylic [42]
substance) compressed from enteric- polymers: relatively brittle Eudragit® L30 D-55 with more
®
coated pellets flexible Eudragit FS 30 D.
Thymidine Enteric-coated HPMC Optimized coating process(fluid bed apparatus) Ready-to-use enteric-coated HPMC capsules for the use in [43]
capsules retail or hospital pharmacy or R&D sections of
pharmaceutical industry.
*
No literature found.

journals. But few articles were published on the use of Eudragit FS having a molecular weight of approximately 7,50,000 g/mol
30 D in various dosage forms such as multiparticles, tablets and whereas NM30 D have molecular weight of 6,00,000 g/mol. Glass
capsules for enteric coating as shown in Table 5. Dreu et al. [42] transition temperature (Tg) of NE 30 D and 40D are ~8  C whereas
produced multiple-unit tablet compressed from enteric-coated NM 30 D is having glass transition temperature of ~11  C. Eudragit
pellets. An optimal coating was obtained by mixing two acrylic NE 30D, NE 40 D and NM 30 D are available in the form of aqueous
polymers: relatively brittle Eudragit® L30 D-55 with more flexible dispersion 30, 40 and 30% respectively. All are highly flexible in
Eudragit® FS 30 D. The final formulation released 9% drug in acidic nature and does not require incorporation of plasticizer. They are
medium. In addition to coating, biconvex shape of tablet and pro- used in formulation of controlled release products which are in-
tective coating of Kollidon VA 64 also played a significant role in dependent of pH of gastrointestinal tract.
achieving enteric coating. Huyghebaert et al. [43] developed an An extensive review on Eudragit NE 30D revealed that it is used
alternative method for enteric coating of HPMC capsules that for modified release formulations in various dosage forms such as
avoids the sealing step before coating, resulting in ready-to-use multiparticles, microparticles, pellets, films etc as shown in Table 6.
enteric-coated capsules for the use in retail or hospital pharmacy Amrutkar et al. [52] designed multiparticulate floating drug de-
or R&D sections of pharmaceutical industry and for the production livery system of zolpidem tartarate to prolong the gastric residence
of enteric-coated heat and moisture sensitive biomaterials. The time and to improve bioavailability. The system consists of effer-
release of thymidine in 0.1 N HCl after 2 h from capsules coated vescent layer (sodium bicarbonate) and polymeric layer (Eudragit
with Eudragit L30D-55, Eudragit FS 30 D, Aqoat AS-HF and Sureteric NE 30D) membrane. In-vitro drug release of the system were
was 0.6 ± 0.03, 0.6 ± 0.3, 1.2 ± 0.2 and 7.3 ± 1.9% respectively. The dependent on Coating level of the polymeric membrane (Eudra-
alternative method was reproducible and offered a way to over- git(®) NE 30D) played a significant role in drug release. Kumaria
come the time-consuming and expensive sealing step required et al. [53] developed and evaluated Loratidine buccal films for
using the conventional coating procedure. allergic rhinitis. Polymeric buccoadhesive films of loratidine were
prepared using hydroxypropylmethyl cellulose (HPMC)-E5 and
2.5. Eudragit NE 30D, NE 40D and NM 30D K100 blend and Eudragit® NE 30D as retardant. Films were pre-
pared using solvent-casting method. Increase in Eudragit® NE 30 D
Eudragit NE 30D, NE 40D and NM 30 D are the aqueous content in the film decreased the hydration, erosion and drug
dispersion of a neutral copolymer based on ethyl acrylate and release, but enhanced the mucoadhesion time.
methyl methacrylate. These are milky white liquid of low viscosity Current literature review on Eudragit NE 40 D suggests that it is
with a faint characteristic odour. All the three grades have mini- used for various pharmaceutical applications like modified release,
mum film forming temperature of 5  C. Both NE 30D and 40 D are enhancement of bioavailability etc as bucoadhesive films and non
Ch.N. Patra et al. / Future Journal of Pharmaceutical Sciences 3 (2017) 33e45 39

Table 6
Reported literature on Eudragit NE 30 D.

Drug name Dosage form/delivery system Method of Preparation Application References

Eudragit NE 30 D
Zolpidem tartarate Multiparticulate floating drug delivery Coated with effervescent layer and Rapid floating and modified drug [52]
system (pellets) polymeric membrane release was obtained.
Loratidine Prolonged release Buccoadhesive film Solvent-casting method Mucoadhesion and release retardation [53]
was achieved with HPMC and eudragit
NE 30 D respectively.
Theophylline or cimetidine Multiparticulate DDS Extrusion-spheronization followed by Modified release [56]
coating.
Venlafaxine hydrochloride Pellets Extrusion/spheronization followed by Differences in the film micro-structure [57]
coating and surface roughness influence the
in vivo release
Tamsulosin hydrochloride Sustain Release microparticles Single-step matrix coating Optimum ratio of Aquacoat® and [58]
Eudragit® NE30D in the matrix (9:1)
provides a sustained-release
Urapidil Drug layer pellets followed by coating Centrifugal granulation and fluid bed Improvement in bioavailability [59]
coating
Eudragit NE 40 D
Prednisolone Buccoadhesive films solvent-casting method Enhanced bioavailability [54]
Miconazole nitrate Nonocclusive dermal therapeutic Matrix system In vitro control of drug release for at [55]
system least 24 h
Eudragit NM 30 D
* * * * *
*
No literature found.

occlusive dermal therapeutic systems as shown in Table 6. Kumria chemical properties of the polymers vis-a -vis eudragit RL30D and
et al. [54] prepared buccoadhesive films of prednisolone by solvent- RS30D on the release profile of ketoprofen from pellets. Extruded
casting method using hydroxyl propyl methyl cellulose (K100), and spheronized pellets were coated with 15% (w/w) polymers
Carbopol 940 and/or Eudragit® NE 40 D. Buccal route was found as a Eudragit RL 30 D and Eudragit RS 30 D. It was revealed that Eudragit
viable option for delivery of prednisolone. Minghetti et al. [55] RL 30 D has the effect to increase the initial drug release more
prepared self-adhesive matrix made of a mixture of Plastoid E significantly than RS 30D. Lingam et al. [61] formulated matrix type
35 L, an adhesive hydrophilic polymer, and eudragit NE 40 D, a multiple-unit (minitablets) floating drug delivery system for
nonadhesive hydrophobic polymer able to modify the drug release. captopril. The system consists of core units which are coated with
All systems sustained drug release for at least 24 h. No literature three successive layers vis-a-vis inner seal coat, effervescent layer
was found for Eudragit NM 30D based formulations in pubmed and an outer gas-entrapped polymeric membrane of an poly-
indexed journals. methacrylates. Eudragit RL30D and its combination formulations
exhibited floating.
2.6. Eudragit RL 30 D, RLPO, RL100 and RL 12,5 Review on Eudragit RLPO is primarily used for sustaining drug
release in diverse drug delivery systems like nanoparticles,
Eudragit RL 30 D, RLPO, RL100 and RL 12,5 are copolymers of mucoadhesive tablets and patches, solid dispersions etc as shown
ethyl acrylate, methyl methacrylate and a low content of meth- in Table 7. Singh et al. [62] investigated the effect of iron oxide in
acrylic acid ester with quaternary ammonium groups. The ammo- the development of mucoadhesive tablets of cinnarizine using
nium groups are present as salts and make the polymers Eudragit RLPO. Eudragit RLPO and iron oxide exhibited potential
permeable. RL 30D is a milky white liquid of low viscosity with a for gastroretentive and mucoadhesive drug delivery systems.
faint characteristic odour. Molecular weight of RL 30D is approxi- Pandey et al. [63] attempted site specific drug delivery by
mately 32,000 g/mol. Its minimum film forming temperature and formulating bilayered gastroretentable mucoadhesive patch
glass transition temperature are 40  C and 55  C respectively. Alkali (stomach). Both Eudragit RSPO and RLPO were used for formu-
value of RL 30D is 32.3 mg KOH per g of polymer. RL 30D is available lation of patch. Patches could control the drug release up to 12 h,
in the form of 30% aqueous dispersion. RL 30D exhibit pH depen- with mucoadhesion. Sahoo et al. [64] formulated solid dispersion
dent swelling. RL 30D is primarily used in the formulation of sus- of verapamil using Eudragit RLPO or Kollidon SR to sustain drug
tained release products. Eudragit RLPO is a solid substance available release. Extended the drug release upto 12 h was attained in case
in the form of white powder with a faint amine like odour whereas of Eudragit RLPO.
eudragit RL100 is a solid substance available in the form of col- A widespread literature review on Eudragit RL 100 revealed that
ourless, clear to cloudy granules with a faint amine like odour. it is used for controlled release and bioavailability improvement
Molecular weight, alkali value and glass transition temperature of approaches in various dosage forms such as nanoparticles, tablets,
both RLPO and RL 100 are same i.e. 32,000 g/mol, 28.1 mg KOH/g buccal films, transdermal patches, ophthalmic inserts etc as shown
polymer and 70  C respectively. RLPO and RL100 is mainly used for in Table 7. Singh et al. [65] prepared atazanavir nanoparticles
customized release profile by combination of RL and RS grades in loaded with Eudragit RL 100 to improve oral bioavailability. These
different ratios and they are also suitable for matrix structures. nanoparticles were prepared by nanoprecipitation method.
Eudragit RL 12,5 is light yellow liquid of low viscosity, clear to Eudragit L100 based nanoparticles showed improved bioavail-
slightly cloudy with a characteristic odour of solvents. RL 12,5 is ability potential. Ofokansi et al. [66] prepared ibuprofen tablets
available in the form of a 12.5% organic solution. Its molecular from interpolyelectrolyte complexes (IPECs), formed between
weight, alkali value and applications are same as RLPO. Eudragit RL100 and chitosan, by nonstoichiometric method, and
An extensive literature review on Eudragit RL 30D revealed that tablets based on the above complex by wet granulation method.
this polymer is primarily used for controlled release DDS as shown The complex was capable of preventing drug release in the stomach
in Table 7. Kibria et al. [60] investigated the effect of physico- and small intestine and helped colon specific drug delivery. Palem
40 Ch.N. Patra et al. / Future Journal of Pharmaceutical Sciences 3 (2017) 33e45

Table 7
Reported literature on Eudragit RL 30 D, RLPO, RL100 and RL 12,5.

Drug name Dosage form/delivery system Method of Preparation Application References

Eudragit RL 30D
Diltiazem HCl Matrix Tablets Dry mixing and direct compression Controlled release [69]
followed by coating with Eudragit NE
30D
Ambroxol hydrochloride Pellets Extrusion-spheronization technology Stability was dependent on storage [70]
followed by coating with Eudragit NE condition and physicochemical
30D property of the polymer.
Ketoprofen Pellet Extrusion spheronisation technique Proper selection of polymeric materials [60]
followed by coating with Eudragit Ne based on their physico-chemical
30D and RS 30D properties sustained the drug release.
Captopril Minitablets Direct compression followed by coating Only the system using Eudragit RL30D [61]
and combination of them as a gas-
entrapped polymeric membrane could
float.
Eudragit RLPO
Acyclovir Nanoparticles Nanoprecipitation technique As acyclovir: Eudragit RLPO ratio [71]
increased from 1:1.5 to 1:2, particle size
and drug entrapment increased It also
produced sustain release.
Cinnarizine Mucoadhesive tablets Simplex lattice design Eudragit RLPO and iron oxide [62]
combination showed high level
potential for fabricating gastroretentive
as well as mucoadhesive drug delivery
systems.
Lercanidipine HCl Gastroretentable mucoadhesive patch Layering technique Patches prepared using the [63]
combination of Eudragit RSPO and RLPO
could control the drug release up to
12 h
Domperidone Bilayered mucoadhesive buccal patches Solvent casting technique Bilayered mucoadhesive buccal patches [72]
with desired permeability could be
prepared
Metoprolol Solid dispersion Melting and solvent method RLPO showed higher release than RSPO. [73]
Verapamil hydrochloride Solid dispersion compressed into a Direct compression The tablet containing Eudragit RLPO has [64]
tablet extended the release rate for 12 h
Promethazine hydrochloride Solid dispersions compressed into Coevaporation and coprecipitation Eudragit RLPO coevaporates (1: 5) [74]
tablet techniques displayed extended release of drug for
12 h
Eudragit RL100
Griseofulvin Polymer-coated drug Porous hollow fiber membrane-based Coated drug particles can be potentially [75]
antisolvent crystallization used for controlled release.
Atazanavir Nanoparticles Nanoprecipitation method To improve bioavailability & in [65]
prolonged drug release
Ibuprofen Tablet with interpolyelectrolyte Wet granulation Exploited successfully for colon- [66]
complexes (IPECs), formed between targeted delivery of ibuprofen
Eudragit RL100 (EL) and chitosan (CS).
Metformin hydrochloride Matrix tablet Wet granulation technique used to sustain drug release [76]
Domperidone Buccal films Hot-melt extrusion improved bioavailability [67]
Azithromycin Opthalmic inserts Modified solvent casting method Prolonged release time and improved [68]
ocular availability.
Lercanidipine hydrochloride Transdermal patches Solvent evaporation technique Drug release sustained upto 24 h. [77]
Sulfacetamide Nanosuspension Solvent displacement method Formulation of sulfacetamide in [78]
Eudragit RL100 improve the availability
of sulfacetamide at the intraocular level.
Azelastine hydrochloride Microspheres Solvent evaporation technique Prolonged release of the drug over the [79]
period of 6 h.
Zidovudine Transdermal delivery Solvent evaporation method Increased permeation [80]
Cloricromene Nanoparticle suspensions Quasi-emulsion solvent diffusion Improves the shelf life and [81]
technique bioavailability of this drug after
ophthalmic application
Eudragit RL 12,5
* * * * *
*
No literature found.

et al. [67] prepared domperidone (DOM) hot-melt extruded (HME) RL100) showed release of drug over a 12 h in a steady and
buccal films by using combination of HPMC E5 LV or Eudragit RL100 controlled manner. No research articles found for Eudragit RL 12,5
as polymeric carriers along with some other carriers exhibited 1.5 in pubmed indexed journals.
times improved bioavailability. Thakur et al. [68] formulated the
bioerodable insert of azithromycin to prolong the release time and 2.7. Eudragit RS 30D, RSPO, RS 100 and RS 12,5
improve the ocular availability. Azithromycin insert was prepared
using hydroxyl propyl methyl cellulose (HPMC) and Eudragit Eudragit RS 30D, RSPO, RS100 and RS 12,5 is a copolymer of
RL100. The formulation (comprising of 1.5% HPMC and 3% Eudragit ethyl acrylate, methyl methacrylate and a low content of
Ch.N. Patra et al. / Future Journal of Pharmaceutical Sciences 3 (2017) 33e45 41

methacrylic acid ester with quaternary ammonium groups. The gradual sustained release of OMT for over 12 h. Kibria et al. [60]
ammonium groups are present as salts. Presence of salts makes investigated the release of ketoprofen from pellets to study the
them more permeable. Eudragit RS 30 D is a liquid of low viscosity effect of physico-chemical properties of polymers. The drug con-
with milky white color showing faint characteristic odour. Eudragit taining core pellets were prepared by extrusion spheronisation
RSPO is white powder with a faint amine like odour. Eudragits RS technique and subsequently coated with 15% (w/w) polymer load of
100 is colorless granule with a faint amine like odour. Eudragit RS the combination of Eudragit RL 30 D & Eudragit RS 30 D. It was
12,5 is a light yellow liquid of low viscosity, clear to slightly cloudy revealed that Eudragit RL 30 D has the effect to increase the initial
with a characteristic odour of the solvents. Molecular weight of drug release more significantly where as Eudragit RS 30 D has the
each of the above grades is 32,000 g/mol. Eudragit RS 30D, RSPO, effect to minimize the initial drug release but increase the terminal
RS100 and RS 12,5 are available in the form of 30% aqueous drug release more significantly.
dispersion, powder, granules and 12.5% organic solution respec- An extensive review on research publication on Eudragit RSPO
tively. All the above four grades of Eudragit are insoluble. They revealed that it is mainly used in the sustaining drug release as
exhibit low permeability with pH independent swelling. These shown in Table 8. Eudragit RSPO has been used in the formulation of
polymers are used for controlled and customized release profile by microballons, tablets, microspheres and microtablets. Porwal et al.
combination of RL and RS grades in different ratios. [83] prepared microballons of propranolol HCl by the non-aqueous
Eudragit RS 30 D is extensively used for formulation of sustain oil in oil emulsion solvent diffusion evaporation method using
release products. The current literature survey suggests that this Eudragit RSPO as polymer. The drug release from microballoons
polymer has been used in formulation of pellets, coating of pellets showed a biphasic pattern with an initial burst release, followed by
osmotically driven pellets etc as shown in Table 8. Piao et al. [82] sustained release for 12 h Abbaspour et al. [84] prepared and
developed sustained release osmotic pellet coated of oxymatrine. characterized ibuprofen pellets based on Eudragit RSPO and RLPO or
Extrusion/spheronization followed by coating with Eudragit RS 30 their combination. Eudragit RLPO compare with Eudragit RSPO
D was adopted. They found that the F3 formulation, prepared with resulted in pellets with high crushing strength; however, Eudragit
20% NaCl and an 8% coating level (Eudragit RS 30 D), showed a type did not have a significant effect on elastic modulus.
continuous NaCl-induced water influx into the pellets providing a Literature review on applications of eudragit RS100 suggests

Table 8
Reported literature on Eudragit RS 30D, RSPO, RS 100 and RS 12,5.

Drug name Dosage form/delivery system Method of Preparation Application References

Eudragit RS 30D
Oxymatrine Osmotically driven Pellets Extrusion/Spheronization followed by Gradual sustained release for 12 h [82]
fluid bed coating
Ambroxol hydrochloride Pellets Extrusion-spheronization technology Stable and sustain release formulation [70]
followed by coating
Diclofenac sodium Pellets Powder layering technology and air Retarded the drug release rate and [87]
suspension technique varied according to the type and
amount of plasticizers
Ketoprofen Pellets Extrusion and spheronisation followed Eudragit RS 30 D has the effect to [60]
by coating minimize the initial drug release but
increase the terminal drug release more
significantly.
Diclofenac sodium Pellets Roto-agglomeration Eudragit RS 30 D provided membranes [88]
successfully controlling drug release
over an extended period of 24 h
Eudragit RSPO
Propranolol hydrochloride Microballoons Non-aqueous O/O emulsion solvent Drug release showed a biphasic pattern [83]
diffusion evaporation method with an initial burst release, followed by
sustained release for 12 h
Alfuzosin hydrochloride Tablets Direct compression The release of Alfuzosin was prolonged [89]
for 20 h
Stavudine Microspheres Solvent evaporation method Sustain release [90]
Ibuprofen Pellets Extrusion-spheronization Eudragit RLPO and RSPO did not have a [84]
significant effect on elastic modulus.
Lobenzarit disodium Tablets Direct compression slower release rate [91]
Theophylline Microtablets Rotary tablet press Sustained-release [92]
Eudragit RS 100
Genistein Nanostructured lipid carrier (NLC) Melt-emulsification technique 3.3-fold increase in corneal penetration [85]
Metformin HCl and Acarbose Bbilayer tablet Solvent evaporation and cogrinding Extended release of metformin HCl for [93]
techniques 12 h from one layer
Verapamil hydrochloride Matrix tablet followed by coating Wet granulation method Coating with eudragit RS100 polymer [94]
minimized initial burst release
Terbinafine hydrochloride positively charged controlled-release Nanopreciptation method Increased drug mean residence time [95]
polymeric Nanoparticles as eye drop and improved its ocular bioavailability
four fold.
Lornoxicam matrix-type transdermal patch Solvent evaporation technique Sustain release and enhanced [86]
bioavailability
Clotrimazole Bioadhesive Vaginal tablets containing Spray drying technique Controlled intravaginal drug release [96]
microspheres
Eudragit RS 12,5
* * * * *
*
No literature found.
42 Ch.N. Patra et al. / Future Journal of Pharmaceutical Sciences 3 (2017) 33e45

that it has been used extensively in the formulation of following corneal penetration producing a 3.3-fold increase in apparent
types of dosage form vis-a-vis nanoparticle, bilayer tablet, matrix permeability coefficients was attributed to Eudragit RS100. Bavis-
tablet, transdermal patch, vaginal tablets etc as shown in Table 8. kar et al. [86] prepared matrix-type transdermal drug delivery
Zhang et al. [85] formulated nanostructured lipid carrier (NLC) system of lornoxicam with the addition of hydrophilic and hydro-
surface modified with Eudragit RS100 Model drug genistein was phobic polymers in different ratios. Transdermal patches of lor-
selected. NLC was produced using the melt-emulsification tech- noxicam were designed with ethyl cellulose:polyvinylpyrrolidone
nique followed by surface absorption of Eudragit RS 100. The and Eudragit RL 100:Eudragit RS 100 in different ratios with pro-
Eudragit RS 100 increased the surface zeta potential from 7.46 mV pylene glycol as plasticizer (5%) and tween 80 as permeation
to þ13.60 mV, by uniformly forming a spherical coating outside the enhancer using the solvent evaporation technique. It was observed
NLC surface, as shown by transmission electron microscopy images. that both the patches significantly controlled inflammation and
Particle size growth was inhibited by Eudragit RS 100. Increased showed analgesic effect from the first hour (P < 0.05). Formulations

Table 9
Patents on applications of Eudragit.

S. No Title of the patent Invention Patent Number Inventors Date References

1 Colonic delivery using zn/ The systems include pectin US 20080124279 A. Andremont H. Huguet 05/29/2008 [97]
pectin beads with a eudragit beads cross linked with zinc or
coating. any divalent cation of interest,
which beads are then coated
with Eudragit®-type polymers.
2 Ursodeoxycholic acid-synthetic The ursodeoxycholic acid- US 20120156263 J.H. Choy, G.E. Choi, M. C. Park, H. C. 06/21/2012 [98]
hydrotalcite-eudragit hybrid, synthetic hydrotalcite-Eudragit Chang
pharmaceutical composition hybrid was used for bitter-
containing the same and taste-blocking effect and
method for preparing the same improved body absorption rate
with high solubility.
3 Modified release tablet Eudragit L100-55 for said US 20070104782 S. H. Amir 02/08/2007 [99]
formulations with enhanced pharmaceutical formulation C.E. Melissa
mechanical properties which achieves a desired
hardness for tablets made from
the formulation.
4 Curcuminoid complexes with Curcuminoid-eudragit US20140271530 H. Tummala, S. Kumar 09/18/2014 [100]
enhanced stability, solubility complex, which enhance the
and/or bioavailability bioavailability of the curcumin
component.
5 Improved stabilization of Misoprostol was complexed EP0896823 C. David Tsay, 09/25/2002 [101]
misoprostol with various grades of Eudragit R. Jen
RS series, Eudragit RL series, Lin Hue In
Eudragit S, Eudragit L., The solid Lu Shu-bin
dispersions were stable 6and
showed sustain release.
6 Sustained release Controlled dissolution of the EP0322277 H. Stevens, 01/22/1992 [105]
pharmaceutical composition active principle independently M. Chariot,
of the pH, which consists of F. Arnold,
micro particles containing the G. Lewis
active principle, coated with a
mixture of ethylcellulose and
Eudragit RS.
7 Colonic delivery of metallo- Pectin beads are crosslinked US 20080199528 A. Andremont, 08/21/2008 [106]
dependent enzymes with zinc ions and the pectin H. Huguet
beads are coated with a
Eudragit® polymer.
8 Coated senna extract granules Senna extract with 20% WO/2011/014976 P. H. Jorge 10.02.2011 [102]
sennosides are granulated with
Eudragit L 100 and then coated
with Eudragit L 30 D 55
9 ketoprofen microgranules, ketoprofen micro granules of WO/2000/064432 L. C. Marechal, 11/02/2000 [103]
method for preparing same and eudragit RL and RS exhibited D.S. Pascal
pharmaceutical compositions prolonged release
10 Formulation stabilizer for The polymeric base is US 20060013880 F. Robert, R. Narayan, Z. Joseph 01/19/2006 [104]
proton pump inhibitors cholestyramine-OH, Eudragit H. Ping
EPO, chitosan, or a mixture
thereof. The composition
stabilizes the benzimidazole
derivative proton pump
inhibitor in a humid
environment
11 Oral drug delivery formulations One active substance and at US 20150250733 O. Isa 09/10/2015 [107]
least one coat comprising
Eudragit E The formulation may
be used for releasing up to
about 55% of a total dose as a
loading dose in order to manage
pain.
Ch.N. Patra et al. / Future Journal of Pharmaceutical Sciences 3 (2017) 33e45 43

A3 and B3 were found to enhance the bioavailability of lornoxicam role of Eudragit in different formulations. Hence this review
by 3.1 and 2.7 times, respectively, compared to the oral dosage manuscript can be used as ready reckoner for researchers to
form. Hence, lornoxicam can be formulated into transdermal develop Eudragit based drug delivery systems.
patches for sustain release characteristics. As far as Eudragit RS 12,5
is considered no such research article is published in any indexed Acknowledgements
research journals.
The authors are thankful to management and principal, Roland
3. Recent patents on eudragit based formulations Institute of Pharmaceutical sciences, Berhampur, India for support
and encouragement.
Recent reviews on various patents published on Eudragit based
formulation were collected. It was observed that Eudragit based
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