Effect of tricaprin on the physical characteristics and in vitro release of etoposide from PLGA microspheres

Abstract

The purpose of this article is to examine the effects of tricaprin on the physical characteristics and in vitro release of etoposide from poly (lactic-co-glycolic acid) microspheres. The microspheres were synthesized through the use of a single-emulsion solvent-extraction procedure. Samples from each batch of microspheres were then analyzed for size distribution, drug loading efficiency, surface characteristics, in vitro release, and in vitro degradation of microspheres. Microsphere batches were synthesized using three different etoposide concentrations (15%, 10%, and 5% w/w) with tricaprin concentrations of 25% and 50%. The incorporation of 50% tricaprin significantly increased (p<0.05) the size of the microspheres for all three etoposide concentrations in comparison to microspheres prepared without tricaprin (control). The percentage of tricaprin used did not significantly affect the drug loading efficiency of the microspheres. The addition of tricaprin was shown to significantly increase (p<0.05) the in vitro release of etoposide from the microspheres prepared with all three concentrations of etoposide and the two different tricaprin percentages. Examination of the surface characteristics of the tricaprin loaded microspheres showed a dimpled surface with what appeared to be pockets of tricaprin dispersed throughout. In the in vitro degradation study, the tricaprin microspheres grew very porous as the degradation time increased, but they still retained a recognizable structure even after 30 days of degradation. © 2002 Elsevier Science Ltd. All rights reserved.