Development and optimisation of mucoadhesive nanoparticles of acyclovir using design of experiments approach.
The aim of our study was to improve the bioavailability of acyclovir (ACV) by delivery of mucoadhesive nanoparticles (NPs) and controlled delivery of drug at its absorption window. Central composite design was used by which the effects of independent variables (gelatin and Pluronic F-68) on various responses such as particle size, polydispersity index, entrapment efficiency, loading efficiency, drug release and mucoadhesive strength were studied. The optimised formulation was evaluated for morphology, stability, pharmacokinetic and gastrointestinal tracking. The optimised NPs were found to be nearly spherical. Changes in characteristics of NPs were not significant after six months of accelerated stability studies. In vivo mucoadhesion study showed significant retention of mucoadhesive NPs in upper gastro-intestinal tract for more than 12 h. Pharmacokinetic study in rats revealed that mucoadhesive NPs could maintain relatively steady plasma concentration of ACV for more than 10 h. The AUC0-∞ and mean residence time of optimised formulation (7527.9 ng h/mL and 12.09 h) were significantly high than tablet dispersion (3841.13 ng h/mL and 7.97 h).
a Department of Pharmaceutics , Oriental College of Pharmacy , Bhopal , Madhya Pradesh , India .
Ankit Anand
AA
Kharia
Akhlesh Kumar
AK
Singhai
D000212:Acyclovir / Q000008:administration & dosage*; D000284:Administration, Oral; D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage; D019540:Area Under Curve; D001682:Biological Availability; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004353:Drug Evaluation, Preclinical; D005780:Gelatin / Q000737:chemistry; D008297:Male; D050997:Nanomedicine / Q000379:methods; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D013607:Tablets
D000998:Antiviral Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D013607:Tablets; D020442:Poloxamer; D005780:Gelatin; D000212:Acyclovir
Acyclovir; central composite design; gastoretention; gelatin; mucoadhesion; pharmacokinetics