Title:Polymeric Nanoparticles Loaded with Acyclovir: Formulation, Characterization and In-Vitro Drug Prolonged-Release Study
VOLUME: 10 ISSUE: 3
Author(s):Tran Thi Hai Yen*, Nguyen Tran Linh, Vu Thi Thu Giang and Hoang Lan Anh
Affiliation: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
Keywords:Polymer nanoparticles, acyclovir, prolonged-release, nanoprecipitation, Eudragit RS 100,
Eudragit RL 100.
Abstract:
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
ACV-Eud 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 ACVEud
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.
