CONTROLLED RELEASE SYSTEMS OF

BIOPHARMACEUTICALS
ODAE FARUNIA
TAREK HADDO
2017 PHARMD CANDIDATES
 OBJECTIVES

• Define Biopharmaceuticals
• Define Controlled drug release system
• List types of Controlled drug release systems
• Discuss formulation issues for alternative forms of
antibody delivery
• Discuss the challenges in the design of injectable
formulations
• Discuss Pegylation
 BIOPHARMACEUTICALS

• Biopharmaceuticals are medical drugs produced

using biotechnology.
• These include:
• Proteins (Antibodies)
• Nucleic Acids (DNA, RNA)
CONTROLLED DRUG RELEASE SYSTEM

• Referring to the delivery at predetermined intervals

or gradually over a period of time. Helpful for
maintaining constant drug levels in the target tissues
or cells.
TYPES OF CONTROLLED DRUG RELEASE
SYSTEMS
• Dissolution controlled systems
• Diffusion controlled systems
• Dissolution and diffusion controlled release
• Water penetration controlled systems
• Chemically controlled release systems
• Hydro gels
• Ion- exchange resin controlled release systems
 FORMULATION ISSUES FOR
ALTERNATIVE FORMS OF ANTIBODY
DELIVERY
• Oral
• Respiratory tract
• Miscellaneous delivery sites of the body
• Intracellular targeting
 CHALLENGES IN THE DESIGN OF
INJECTABLE FORMULATIONS[3]
• One of the key challenges is overcoming the
instability of the biologic, caused by:
• Aggregation
• Deamination
• Isomerization
• Hydrolysis
• Oxidation
• Denaturation
• Agents developed to increase the stability of
biologics
• Trehalose
• Polysaccharides such as dextran’s.
 CHALLENGES IN THE DESIGN OF
INJECTABLE FORMULATIONS[3]
• Another issue related to biopharmaceutical drug
formulations is high and variable viscosity.
• Approaches to achieve this includes the addition of
hydrophobic salts or inorganic salts, or the addition
of lysine or arginine.
 PEGYLATION: ENGINEERING
IMPROVED BIOPHARMCEUTICALS[4]
• The technology of Polyethylene glycol (PEG)
conjugation, holds significant promise in
maintaining effective plasma concentrations of
systemically administered drugs.
• PEG chains can be conjugated to bio-therapeutics
• Increases their hydrodynamic volume, which can in turn
prolong their plasma retention time, increase their solubility
and shield antigenic determinants
 CONCLUSION

• Current biopharmaceutical drugs are primarily

aimed at extracellular targets owing to the
challenges associated with intracellular delivery
and so improving intracellular delivery could result in
new classes of biopharmaceutical drugs. Another
area for future research is the development of new
delivery devices for biopharmaceuticals drugs that
could overcome the hurdles that cannot be
addressed by new formulations.
 REFERENCES
1. "Controlling Drug Delivery." Pharmaceutics: Drug Delivery and Targeting (n.d.): 1-24. Web. 15 June 2016.
<https://www.pharmpress.com/files/docs/FT_Pharmaceutics_Drug_Delivery_sample.pdf>.
2. Daugherty, Ann L., and Randall J. Mrsny. "Formulation and Delivery Issues for Monoclonal Antibody
Therapeutics." Advanced Drug Delivery Reviews 58.5-6 (2006): 686-706. Web. 13 June 2016.
3. Mitragotri, Samir, Paul A. Burke, and Robert Langer. "Overcoming the Challenges in Administering
Biopharmaceuticals: Formulation and Delivery Strategies." Nature Reviews Drug Discovery Nat Rev Drug
Discov 13.9 (2014): 655-72. Web. 15 June 2016.
<http://www.nature.com/nrd/journal/v13/n9/full/nrd4363.html>.
4. Molineux, Graham, PhD. "Wiley Online Library." Wiley Online Library. N.p., 15 June 2016. Web. 29 June
2016. <http://onlinelibrary.wiley.com/>.