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Updated: Apr 27, 2026

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Impact of microparticle formulation approaches on drug burst release: a level A IVIVC
Rania A H Ishak1, Nahed D Mortada, Noha M Zaki
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University , Cairo , Egypt.
Aim:
To study the effect of poly(d,l-lactic-co-glycolic acid) (PLGA) microparticles (MPs) preparation techniques on particle physical characterization with special emphasis on burst drug release.
Methods:
A basic drug clozapine was used in combination with acid-terminated PLGA. Two approaches for MP preparation were compared; the in situ forming microparticle (ISM) and the emulsion-solvent evaporation (ESE) methods using an experimental design. The MPs obtained were compared according to their physical characterization, burst release and T80%. An in vivo pharmacokinetic study with in vitro-in vivo correlation (IVIVC) was also performed for the selected formula.
Results:
Both methods were able to sustain drug release for three weeks. ISM produced more porous particles and was not effective as ESE for controlling burst release. A good IVIVC (R(2) = 0.9755) was attained when injecting the selected formula into rats.
Conclusion:
MPs prepared with ESE showed a minimum burst release and a level A IVIVC was obtained when administered to rats.
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