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Published on: July 23, 2016
Study of gamma-irradiation effects on aciclovir poly(D,L-lactic-co-glycolic) acid microspheres for intravitreal
Concepción Martínez-Sancho1, Rocío Herrero-Vanrell, Sofía Negro
1Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Plaza Ramon y Cajal sn, Universidad Complutense de Madrid, 28040 Madrid, Spain.
Abstract:
Gamma-irradiation effects on aciclovir poly(D,L-lactic-co-glycolic) acid (PLGA) microspheres, with gelatin as additive, were studied. Microspheres with a 2:2:10 aciclovir:gelatin:polymer ratio were prepared by the solvent evaporation method and sterilised by gamma-irradiation at a dose of 25 kGy. Loading efficiency, morphology (particle size analysis, scanning electron microscopy (SEM)), physical chemistry (infrared (IR) absorption spectrophotometry, differential scanning calorimetry (DSC), X-ray diffraction and gel permeation chromatography (GPC)) and in vitro release assays for 73 days were performed to evaluate the sterilisation effect on microsphere characteristics. After gamma-irradiation, no surface changes were observed by SEM. Microparticle mean diameter and aciclovir loading efficiency were not affected by gamma-ray exposition. IR spectroscopy, DSC and X-ray diffraction showed no modification of the bulk properties of the microspheres or their components. The controlled release profiles of aciclovir-loaded microspheres for 73 days were not altered upon exposure to gamma-irradiation. GPC measurements showed a decrease in molecular weight of the polymer. The sterilisation method is adequate because microspheres underwent no change after exposition to gamma-irradiation. These favourable properties of the aciclovir-loaded microspheres make them a suitable system for the intravitreal treatment of herpes virus infections, in an animal model.
