Abstract

This study was aimed at improving dissolution rate and sustained release of progesterone by varying copolymer composition and polymer: drug ratio of PLGA. Drug-loaded particles were prepared using electrohydrodynamic atomization. The effects of polymer: drug ratio and copolymer composition on particle properties and in vitro drug-release profile were investigated. The physical form of the generated particles was determined via X-ray powder diffraction (XRPD) and Fourier transform infrared spectroscopy (FTIR). Drug release in vitro was found to be dependent on copolymer composition, where the release rate increased with decreased lactide content of PLGA. Particles produced with solutions of copolymer (75:25) had elongated shapes. In general, the obtained results indicated that the prepared microparticles were ideal carriers for oral administration of progesterone offering great potential to improve the dissolution rate of drugs that suffer from low aqueous solubility.

Highlights

  • In the development of oral formulations, the aqueous solubility of the drug plays a key role in the extent of drug absorption [1]

  • Long term sustained drug delivery systems can be obtained using biodegradable particles, in which progesterone can be administered via depot injection [15] and released for a prolonged period of time

  • The effects of PLGA concentration and copolymer composition were evaluated by particle characterization and drug-release behavior in this study

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Summary

Introduction

In the development of oral formulations, the aqueous solubility of the drug plays a key role in the extent of drug absorption [1]. A previous study reveals that the dissolution rate of poorly water-soluble drug can be enhanced by incorporating it into a polymeric matrix thereby inducing its amorphous state [14], again making this a preferable oral delivery technique. Long term sustained drug delivery systems can be obtained using biodegradable particles, in which progesterone can be administered via depot injection [15] and released for a prolonged period of time. The medication is deposited in a localized mass via intramuscularly, subcutaneously or intradermal injection This offers advantages over long-term daily injection which can compromise patient compliance

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