Tran Thi Hai Yen*, Nguyen Tran Linh, Vu Thi Thu Giang and Hoang Lan Anh Pages 271 - 279 ( 9 )
Objectives: Acyclovir (ACV) is an antiviral drug, which requires frequent dosing regimen because of poor oral bioavailability and short half-life. In this study, ACV nanoparticles were formulated using ammonium methacrylates copolymers such as Eudragit RS 100 (Eud RS) and Eudragit RL 100 (Eud RL) to prolong release drug, and increase bioavailability.Methods: ACV loaded nanoparticles were prepared by the solvent replacement technique and then were characterized by particle size, distribution, entrapment efficiency, differential scanning calorimeter, transmission electron microscope, and in-vitro drug release. Results: It was found that as drug:polymer ratio changed from 1:2 to1:5, particle size and drug entrapment efficiency increased significantly. ACV– Eud RS loaded nanoparticles had a larger mean diameter of 363 nm in comparison to 200 nm of ACV- Eud RL nanoparticles. DSC results showed that in the prepared ACV-Eud RS nanoparticles, the drug was presented in the amorphous phase and may have been molecularly dispersed in the polymer matrix, but in the ACV-Eud RL nanoparticles, the drug was presented in the particles and homogeneously dispersed in the polymeric matrix. The entrapment efficiency of AVC-Eud RS nanoparticles was higher than that of ACV-Eud RL nanoparticles. In vitro drug release study showed that the ratios of released drug from ACV-Eud RS nanoparticles in the range from 58±3.8 to 62.9 ±4.6%, which was lower than those from ACVEud RL nanoparticles, in the range from 73.3±4.9 to 77.9±2.9%. The release was found to follow the Weibull model with a Fickian diffusion mechanism for both ACV-Eud RS and ACV- Eud RL nanoparticles. Conclusion: These results suggest that ACV nanoparticles based on Eud RS100 and Eud RL100 could prolong the release of the drug.
Polymer nanoparticles, acyclovir, prolonged-release, nanoprecipitation, Eudragit RS 100, Eudragit RL 100.
Hanoi University of Pharmacy, Department of Pharmaceutics, 13-15 Le Thanh Tong str., Hoankiem District, Hanoi, Hanoi University of Pharmacy, Department of Pharmaceutics, 13-15 Le Thanh Tong str., Hoankiem District, Hanoi, Hanoi University of Pharmacy, Department of Pharmaceutics, 13-15 Le Thanh Tong str., Hoankiem District, Hanoi, Saint Paul Hospital, Hanoi