197
Views
6
CrossRef citations to date
0
Altmetric
Research Article

Impact of microparticle formulation approaches on drug burst release: a level A IVIVC

, , , &
Pages 674-684 | Received 05 Oct 2013, Accepted 31 Mar 2014, Published online: 25 Jun 2014
 

Abstract

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 (R2 = 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.

Acknowledgements

The authors wish to express their thanks to the staff members of the pharmacology and toxicology department, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt, for their assistance in performing the in vivo study. The authors would also like to acknowledge PURAC Biochem, Apex Pharma and Sedico companies for supplying PLGA, clozapine and celecoxib, respectively, for this work.

Log in via your institution

Log in to Taylor & Francis Online

PDF download + Online access

  • 48 hours access to article PDF & online version
  • Article PDF can be downloaded
  • Article PDF can be printed
USD 65.00 Add to cart

Issue Purchase

  • 30 days online access to complete issue
  • Article PDFs can be downloaded
  • Article PDFs can be printed
USD 721.00 Add to cart

* Local tax will be added as applicable

Related Research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.