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ISSN 2063-5346
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Formulation and In-Vitro Evaluation of Clopidogrel Bisulphate Nanosuspension using Box Behnken Design.

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Toravi Harita1, Maimuna Fatima1, SVVM Lakshmi2 , Preeti P. Kulkarni1, Sreeja Reddy1, R. Geetha1, Dr. K. Latha1
» doi: 10.48047/ecb/2023.12.10.743

Abstract

In the current study an endeavour was made to formulate Clopidogrel Bisulphate (CLB) nanosuspension for enhancing aqueous solubility of CLB which displays poor bioavailability (<50%) by utilizing nanoprecipitation method, using Polyvinyl alcohol (PVA) as stabilizer optimized by polymer screening studies using different polymers with degree of precipitation as deciding factor. Box-Behnken design was used for optimization of CLB nanosuspension with temperature, drug: polymer and solvent:antisolvent as independent factors and %Drug release as a dependent factor, resulting in 13 formulation runs. Based on responses formulation was optimized (30oC Temperature, 1:4 Drug:Polymer and 1:30 Solvent:Antisolvent). The 13 formulations were assessed for viscosity, drug content and drug entrapment which were in range of 2.01- 4.43cps, 61.2- 86.3% and 81.12- 90.36% respectively. All formulations were found to redisperse within seconds with no lag time. Optimized formulation showed entrapment efficiency of 89.5% with drug release of 88.4% at 90 min. which is close to the value predicted by design. Optimized formulation was likewise evaluated for - particle size, zeta potential and polydispersibility index (PDI) prior to and after subjecting to probe and bath sonication. Particle size was 2334 d.nm, 4.306 d.nm, 4.808 d.nm, zeta potential was 0.940mV, 2.14mV, 0.511mV and PDI was 0.410, 0.487, 0.369 respectively. Optimized formulation demonstrated a 2-fold increase compared to the pure drug. Other evaluation tests performed include viscosity and drug content which were identified to be 2.12cps and 89.78% respectively. The evaluation results indicate that the attempt for enhancement of aqueous solubility of CLB by nanonization technique was successful.

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