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One-Step Preparation of Poly-Lactic-Co-Glycolic-Acid Microparticles to Prevent the Initial Burst Release of Encapsulated Water-Soluble Proteins
Drug Formulation Department, Central Research Laboratories, Kaken Pharmaceutical Co., Ltd. Shizuoka, Japan; Department of Pharmaceutical Engineering, Graduate School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
Drug Formulation Department, Central Research Laboratories, Kaken Pharmaceutical Co., Ltd. Shizuoka, Japan
Department of Pharmaceutical Engineering, Graduate School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
Department of Pharmaceutical Engineering, Graduate School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
Department of Pharmaceutical Engineering, Graduate School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
- 1 Drug Formulation Department, Central Research Laboratories, Kaken Pharmaceutical Co., Ltd. Shizuoka, Japan; Department of Pharmaceutical Engineering, Graduate School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
- 2 Drug Formulation Department, Central Research Laboratories, Kaken Pharmaceutical Co., Ltd. Shizuoka, Japan
- 3 Department of Pharmaceutical Engineering, Graduate School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
- 4 Department of Pharmaceutical Engineering, Graduate School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
- 5 Department of Pharmaceutical Engineering, Graduate School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
Pharmacology & Pharmacy·Volume 04 (2013)·Pages 578–583·Published 8 November 2013·DOI10.4236/pp.2013.48083
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Abstract
An initial burst is often observed during the release of active pharmaceutical ingredients (APIs) from poly-lactic-coglycolic-acid (PLGA) microparticles (MPs) which have been prepared by the emulsion-solvent evaporation method. Herein, we describe the development of a simple one-step coating method that suppresses the initial burst release process. This new method involves coating the PLGA-MPs with PLGA, with the coating process being performed through the phase separation of PLGA on the surface of PLGA-MPs using the emulsion-solvent evaporation method. Bovine serum albumin (BSA) was encapsulated in the PLGA-MPs as a model API. The coated MPs were spherical in shape with no pores on their smooth surface, whereas the non-coated PLGA-MPs had porous surfaces. An in vitro release study showed that the residual levels of BSA in the coated and non-coated PLGA-MPs after 1 h were about 99 % and 16% of the original loads, respectively. The one-step coating method therefore represents a useful method for preparing PLGA-MPs that do not give an initial burst release of proteinaceous APIs.
KeywordsPoly-Lactic-Co-Glycolic-AcidMicroparticleSuppression of Initial Burst ReleaseCoatingBovine Serum Albumin
- R. A. Jain, “The Manufacturing Techniques of Various Drug Loaded Biodegradable Poly(Lactide-Co-Glycolide) (PLGA) Devices,” Biomaterials, Vol. 21, No. 23, 2000, pp. 2475-2490. http://dx.doi.org/10.1016/S0142-9612(00)00115-0
- P. I. P. Park, M. Makoid and S. Jonnalagadda, “The Design of Flexible Ciprofloxacin-Loaded PLGA Implants Using a Reversed Phase Separation/Coacervation Method,” European Journal of Pharmaceutics and Biopharmaceutics, Vol. 77, No. 2, 2011, pp. 233-239. http://dx.doi.org/10.1016/j.ejpb.2010.11.014
- K. Andreas, R. Zehbe, M. Kazubek, K. Grzeschik, N. Sternberg, H. Baumler, H. Schubert, M. Sittinger and J. Ringe, “Biodegradable Insulin-Loaded PLGA Microspheres Fabricated by Three Different Emulsification Techniques: Investigation for Cartilage Tissue Engineering,” Acta Biomaterialia, Vol. 7, No. 4, 2011, pp. 1485-1495. http://dx.doi.org/10.1016/j.actbio.2010.12.014
- C. B. Weldon, J. H. Tsui, S. A. Shankarappa, V. T. Nguyen, M. Ma, D. G. Anderson and D. S. Kohane, “Electrospun Drug-Eluting Sutures for Local Anesthesia,” Journal of Controlled Release, Vol. 161, No. 3, 2012, pp. 903-909. http://dx.doi.org/10.1016/j.jconrel.2012.05.021
- T. Niwa, H. Takeuchi, T. Hino, M. Nohara and Y. Kawashima, “Biodegradable Submicron Carriers for Peptide Drugs: Preparation of dl-Lactide/Glycolide Copolymer (PLGA) Nanospheres with Nafarelin Acetate by a Novel Emulsion-Phase Separation Method in an Oil System,” International Journal of Pharmaceutics, Vol. 121, No. 1, 1995, pp. 45-54. http://dx.doi.org/10.1016/0378-5173(95)00002-Z
- S. Mao, J. Xu, C. Cai, O. Germershaus, A. Schaper and T. Kissel, “Effect of WOW Process Parameters on Morphology and Burst Release of FITC-Dextran Loaded PLGA Microspheres,” International Journal of Pharmaceutics, Vol. 334, No. 1-2, 2007, pp. 137-148. http://dx.doi.org/10.1016/j.ijpharm.2006.10.036
- Y. Yamaguchi, M. Takenaga, A. Kitagawa, Y. Ogawa, Y. Mizushima and R. Igarashi, “Insulin-Loaded Biodegradable PLGA Microcapsules: Initial Burst Release Controlled by Hydrophilic Additives,” Journal of Controlled Release, Vol. 81, No. 3, 2002, pp. 235-249. http://dx.doi.org/10.1016/S0168-3659(02)00060-3
- C. Engineer, J. Parikh and A. Raval, “Effect of Copolymer Ratio on Hydrolytic Degradation of Poly (Lactideco-glycolide) from Drug Eluting Coronary Stents,” Chemical Engineering Research and Design, Vol. 89, No. 3, 2011, pp. 328-334. http://dx.doi.org/10.1016/j.cherd.2010.06.013
- S. Xie, S. Wang, L. Zhu, F. Wang and W. Zhou, “The Effect of Glycolic Acid Monomer Ratio on the Emulsifying Activity of PLGA in Preparation of Protein-Loaded SLN,” Colloids and Surfaces B: Biointerfaces, Vol. 74, No. 1, 2009, pp. 358-361. http://dx.doi.org/10.1016/j.colsurfb.2009.08.005