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Abstract: Due
to their unique features, most nanostructured lipid carriers (NLCs) in association with vegetable oils that exhibit UV filtering properties
and bioactivity could be used in many cosmetic formulations. Therefore, in this work, a new application of pomegranate seed oil (PSO) in
the cosmetic sector was developed, based on the synthesis of bioactive lipid nanocarriers loaded with various UV filters by the hot high
pressure homogenization technique. To get broad spectrum photoprotection, different UVA and UVB filters have been used (Avobenzone
- AVO, Octocrylen -OCT, Bemotrizinol - BEMT). The influence of the solid lipids combined with PSO on the particle size, physical stability
and entrapment efficiency was investigated using 8 nanocarrier systems. An improved physical stability and an appropriate size were
obtained for NLCs prepared with Emulgade, carnauba wax and PSO (e.g. -30.9-36.9 mV and 160185 nm). NLCs showed an
entrapment efficiency above 90% and assured slow release rates of UV filters, especially for BEMT (5%). The developed nanocarriers
have been formulated into safe and effective sunscreens containing low amounts of synthetic UV filters coupled with a high percent of
natural ingredients. The highest SPF of 34.3 was obtained for a cream comprising of 11% PSO and 3.7% BEMT
Keywords: Lipid nanocarriers Pomegranate seed oil Effective sunscreens Critical wavelength Release kinetics
Versita Sp. z o.o.
1. Introduction
Nanostructured lipid carriers (NLCs) are among the
most promising colloidal systems that can be readily
formulated in water-based systems and have been
intensively studied as drug delivery systems for various
lipophilic drugs due to their multiple advantages when
compared to other lipid and polymeric nanosystems
[1-3]. These nanocarriers are submicron particles,
usually with spherical shape and mean diameters ranging
between 50 and 500 nm, composed of a mixture of solid
and liquid lipids dispersed in an aqueous medium and
stabilized by the presence of surfactants [4]. These lipid
systems are safe and biodegradable carriers because
they are produced using non-toxic and non-irritating
ingredients [5]. Due to the solid nature of the lipid matrix
at body and room temperature NLCs present several
* E-mail: rl_stan2000@yahoo.com
+
The article has been presented at the 18th Romanian International Conference on Chemistry and Chemical Engineering - RICCCE18 - held in
New Montana, Sinaia, Romania on 4-7 September, 2013.
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2. Experimental procedure
2.1. Materials
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Table 1.
Composition
Tween 80
PSO%
Em%
Wax%
AVO%
OCT%
BEMT%
NLC 1
2.5
NLC 2
2.5
0.3
0.7
NLC 3
2.5
NLC 4
2.5
3.5
3.5
NLC 5
2.5
3.5
3.5
0.3
0.7
NLC 6
2.5
3.5
3.5
0.3
0.7
NLC 7
2.5
3.5
3.5
0.3
0.7
3.5
3.5
NLC 8
2.5
NE
2.5
10
0.3
0.7
NE 10
2.5
10
(1)
(2)
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(4)
first order:
log(100 % R ) = k1t 2.303
(5)
Higuchi:
%R = k2 t
(6)
KorsmeyerPeppas:
where I0 and Is are the chemiluminescence maximum for
the standard, and for the sample at t = 5 s.
The UV filters in vitro release was studied in phosphatebuffered saline, pH 5.5/ethanol (70:30, v/v), by applying
the vertical Franz glass diffusion cells (Hanson
Reasearch Corporation, USA) method at 37C and
% R = k3 n t
(7)
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Figure 1. Mean particle size and polydispersity index (PdI) of the lipid nanocarriers synthesized with different lipid matrices.
Figure 2.
Zeta potentials values of lipid nanocarriers synthesized with different lipid matrices.
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Figure 3.
Encapsulation efficiency of UV filters into the developed lipid nanocarriers synthesized with different lipid matrices.
Figure 4. Drug loading capacity of lipid matrix of the developed lipid nanocarriers synthesized with different lipid matrices.
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Figure 5.
DSC curves of free (NLC 1 and 4) and loaded NLCs (NLC 2 and 5) in comparison to their physical lipid mixtures (PM 1 and 2).
Figure 6. DSC curves of the NLCs loaded with AVO and OCT (NLC 2 and 5) in comparison to BEMT NLCs (NLC 3 and 8).
Table 2.
Sample
CI
PM 1
Em:PSO
114.4
42.8
58
100
NLC 1
88.34
38.8
55.2
77.2
NLC 2
76.42
36.7
53.9
66.8
NLC 3
84.9
38.1
54
74.2
PM 2
Em:Wax:PSO
144.1
39.4
55.2
81.8
100
NLC 4
93.42
36.8
53.3
82.7
64.8
NLC 5
98.21
34.1
51.2
81.6
68.1
NLC 6
109.7
35.6
53.8
79.8
76.1
NLC 7
132.3
35.1
53.9
80.9
91.8
NLC 8
98.11
36.9
51.1
81
68.0
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Figure 7.
The antioxidant properties of the lipid nanocarriers synthesized with various solid lipids and oil concentrations.
Figure 8. UV absorbance of free and BEMT NLCs in dispersion in comparison with reference nanoemulsion.
antioxidant properties of the oil were enhanced. In
addition, the presence of an antioxidant, the cinnamic
acid derivative, in the composition of carnauba wax has
determined a greater antioxidant activity of the NLCs
with the lipid matrix Em:Wax:PSO.
The UV filters have contributed to an improved AA of
loaded NLCs compared to those of free-NLCs, between
which the BEMT NLCs exhibited better values than
OCT_AVO NLCs.
Also, it was noticed that by increasing the oil
concentration in NLCs synthesis an enhancement of
the antioxidant activity was obtained, thus the NLC 5
(3% oil) presented an AA of 73.6% and NLC 7 (1% oil)
presented an AA of 67.8%.
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Figure 9. UV absorbance of OCT_AVO NLCs based on Em:Wax:PSO in dispersion synthesised with diferent concentrations of pomegranate
seed oil.
Figure 10. UV absorbance of BEMT NLCs dispersions and BEMT NE 10 in comparison with OCT_AVO NLCs dispersions and BEMT NE 10.
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Figure 11.
The release profiles of OCT, AVO and BEMT from the developed lipid nanocarriers.
Table 3.
c irrad I
c irrad II
NLC 1
370
368
369
NLC 2
376
371
368
NLC 3
374
371
371
NLC 4
371
355
355
NLC 5
377
372
370
NLC 6
376
373
370
NLC 7
378
373
370
NLC 8
374
371
370
Reference
OCT_AVO
376
367
368
Reference
BEMT
374
369
369
Sample
Table 4.
UV filter
OCT
Order 0
Order 1
Higuchi
Peppas
R2
0.7194
0.7529
0.9156
0.9171
2.5296
0.0127
8.0378
14.1318
AVO
0.23
R2
0.7562
0.7645
0.9484
0.9544
0.8034
0.0036
2.5341
3.7661
BEMT
0.31
R2
0.8032
0.809
0.9725
0.9749
0.6357
0.0028
1.9701
2.5603
0.38
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Figure 12. SPF values of the creams based on lipid nanocarriers synthesized with different lipid matrices exposed to UV radiation.
Figure 13.
SPF values of the cosmetic creams based lipid nanocarriers co-loaded with UV-filters (2.6% OCT and 1.1% AVO).
4. Conclusions
The use of natural ingredients is highly pursued in human
health, particularly in cosmetics, with an ongoing search
for developing efficient health products with broad
biological relevance. Safe and effective sunscreens
based on lipid nanocarriers containing low amounts
of synthetic UV filters and high amounts of natural
ingredients, which possess UV filtering properties and
bioactivity, were developed in the current work.
Lipid nanocarriers based on different lipid matrices
formed with pomegranate seed oil, with particle sizes
ranging from 130 to 280 nm and with a narrow particle
size distribution were obtained by the high pressure
homogenization technique. An improved physical
stability and a size less than 160 nm were obtained for
nanocarriers prepared with Emulgade, carnauba wax
and pomegranate seed oil. The developed NLCs based
on pomegranate seed oil showed entrapment efficiency
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Acknowledgment
The work has been funded by PN II Partnership program
in priority domains, ANCS, CNDI UEFISCDI, project
no. PN-II-PT-PCCA-132/2012.
References
[1] S. Kumar, J.K.Randhawa, Mat. Sci. Eng. C-Mater.
33, 1842 (2013)
[2] F. Tamjidi, M. Shahedi, J. Varshosaz, A. Nasirpour,
Innov. Food. Sci. Emerg. 19, 29 (2013)
[3] L. Feng, R.J. Mumper, Cancer Letters 334, 157
(2013)
[4] D. Puri, A. Bhandari, P. Sharma, D. Choudhary,
J. Global Pharma Tech. 2, 1 (2010)
[5] J. Pardeike, A. Hommoss, R.H. Mller, Int.
J. Pharmaceut. 366, 170 (2009)
[6] H.S. Jeon, J.E. Seo, M.S. Kim et al., Int. J. Pharm.
452, 311 (2013)
[7] E.B. Souto, S.A. Wissing, C.M. Barbosa,
R.H. Mller, Int. J. Pharm. 278, 71 (2004)
[8] S.A. Wissing, R.H. Mller, J Control Release 81,
225 (2002)
[9] Q. Xia, A. Saupe, R.H. Muller, E.B. Souto, Int.
J. Cosmet. Sci. 29, 473 (2007)
[10] I. Lacatusu, N. Badea, A. Murariu, D. Bojin,
A. Meghea, Mol. Cryst. Liq. Cryst. 523, 247 (2010)
[11] M. Schlumpf, K. Kypke, M. Wittassek, J. Angerer,
H. Mascher, D. Mascher, C. Vkt, M. Birchler,
W. Lichtensteiger, Chemosphere 81, 1171 (2010)
[12] S. Diaz-Cruz, M. Llorca, D. Barcelo, Trends in
Analytic Chem. 27, 873 (2008)
[13] D. Kaiser, A. Sieratowicz, H. Zielke, M. Oetken,
H. Hollert, J. Oehlmann, Environ. Pollut. 163, 84
(2012)
[14] M. Schlumpf, P. Schmid, S. Durrer et al. Toxicology
205, 113 (2004)
[15] N. Serpone, D. Dondi, A. Albini, Inorg. Chim. Acta
360, 794 (2007)
[16] P.Y. Kunz, K. Fent, Toxicol. Appl. Pharm. 234, 77
(2009)
[17] T. Wong, D. Orton, Clin. Dermatol. 29, 306 (2011)
[18] A. Varvaresou, J. Cosmet. Dermatol. 5, 53 (2006)
[19] G. Potard, C. Laugel, H. Schaefer, J.P. Marty, Skin.
Pharmacol. Appl. Skin. Physiol. 13, 336 (2000)
[20] L.R. Gaspar, P.M.B.G. Maia Campos, Int. J. Pharm.
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[40]
[41]
[42]
[43]
[44]
850
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