Development and optimisation of mucoadhesive nanoparticles of acyclovir using design of experiments approach

Abstract

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 AUC_0–∞ 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).

• Acyclovir
• central composite design
• gastoretention
• gelatin
• mucoadhesion
• pharmacokinetics

Acknowledgements

Authors wish to express their deep sense of gratitude to Modern Laboratories (Indore) and SAIL, RGPV (Bhopal) for providing gift sample of drug and determination of particle size distribution, respectively. The authors also thank Professor Bhupinder Singh Bhoop, University Institute of Pharmaceutical Sciences (UIPS), PU, Chandigarh, India, and Dr. Jayant Yadav, Alliance Medicare Pvt. Ltd. (Bhopal, India) for discussing technical issues and collaborative work.

Declaration of interest

The authors report no declarations of interest.