Photolysis of three antiviral drugs acyclovir, zidovudine and lamivudine in surface freshwater and seawater.

Photodegradation is an important elimination process for many pharmaceuticals in surface waters. In this study, photodegradation of three antiviral drugs, acyclovir, zidovudine, and lamivudine, was investigated in pure water, freshwater, and seawater under the irradiation of simulated sunlight. Results showed that zidovudine was easily transformed via direct photolysis, while acyclovir and lamivudine were mainly transformed via indirect photolysis. We found that in freshwater, nitrate enhanced the photodegradation of the three antiviral drugs, bicarbonate promoted the photodegradation of acyclovir, and dissolved organic matter (DOM) accelerated the photolysis of acyclovir and lamivudine. In seawater, the photolysis of acyclovir was not susceptible to Cl(-), Br(-) and ionic strength; however, the photolysis of zidovudine was inhibited by Cl(-) and Br(-), and the photolysis of lamivudine was enhanced by Cl(-), Br(-) and ionic strength. Second-order reaction rate constants for the three antiviral drugs with (1)O2 (k1O2) and OH (kOH) were also measured. These results are important for fate and ecological risk assessment of the antiviral drugs in natural waters.

Study of gamma-irradiation effects on aciclovir poly(D,L-lactic-co-glycolic) acid microspheres for intravitreal administration.

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.