Abstract

ATORVASTATIN LOADED NANOSPONGES –A NOVEL STRATEGIC APPROACH FOR ENHANCED BIOAVIALABILITY

Keerthi Priya Dharshini M.*, Jyothshna Devi K., Shilpaja C. and Umasankar K.

ABSTRACT

Introduction: Nanosponges are three dimensional, solid, porous, biocompatible adaptable drug delivery systems that can entrap both hydrophilic and hydrophobic drugs and conquer the problem of drug toxicity and poor bioavailability. Aim and objective: Atorvastatin, a hypolipidemic drug encounters the major problem of poor oral bioavailability. Hence, the objective of the present study was to develop and characterize an optimal stable nanosponge formulation of Atorvastatin (AT) with solvent evaporation method and aimed to increase its bioavailability. Results and discussion: All the prepared formulations were subjected for various evaluation studies. The entrapment efficiency of all the formulations (AF1 – AF9) was found to be in the range of 71.56±0.78 to 93.36±0.55%. Amongst all the formulations AF8 shows high entrapment efficiency of 93.36±0.55%. The average particle size ranges from 530.3 nm to 758.5 nm which increasing with increase in concentration of polymer. SEM images of optimized formulation AF8 showed nanosponges were spherical and uniform with no drug crystals on the surface. By the end of 12th hour, AF8 formulation shown complete drug release and was found to be 99.23%. The release kinetics of the optimized formulation was best fitted into Higuchi model and showed zero order drug release with super case 2 transport mechanism. Stability studies indicated there was no significant change in the invitro dissolution profile of optimized formulation at storage condition of 40°C ± 2°C / 75 ± 5% RH after 3 months. Conclusion: With the revealed results of different evaluation parameters, it is confirmed that, for highly lipophilic drug like Atorvastatin, nanosponge approach would be possible alternative delivery system to conventional oral formulation to improve its bioavailability.

Keywords: Nanosponges, Controlled release, Targeted release, Atorvastatin, Colloidal size.