Published:  Feb 27, 2017DOI: 10.7324/JAPS.2017.70213
The present study was aimed to formulate nanosuspensions using high pressure homogenization (HPH), a top down technique for enhancement of dissolution rate and solubility of clopidogrel using Pluronic F127 as stabilizer. Clopidogrel is categorized as a BCS class II agent having oral bioavailability less than 50%. The formulation scheme was generated by Box- Behnken design of response surface methodology. The formulated nanosuspensions were assessed on particle size, polydispersity index, and zeta potential. Three formulations were selected based on different predicted particle size with manipulation of parameters using response optimizer. The selected formulations were checked on percentage of bias in between predicted value and observed value and evaluated based on drug content, drug entrapment efficiency and in vitro dissolution study. The formulation was optimized based on the smallest particle size and highest percentage of in vitro cumulative drug release. Formulation FF3 was selected as optimized formulation which attributed to the smallest particle size (478.1 nm) and the highest % CDR in both 0.1 N HCl (98.37%) and phosphate buffer (48.67%). The optimized formulation has shown a significant 2 folds enhancement in dissolution rate in 0.1 N HCl and 10 folds improvement in pH 6.8 phosphate buffers with 0.1% w/v Tween 80 compared to pure drug suspension.
Qureshi MJ, Phin FF, Patro S. Enhanced Solubility and Dissolution Rate of Clopidogrel Nanosuspension: Formulation via High Pressure Homogenization Technique and Optimization Using Box Behnken Design Response Surface Methodology. J App Pharm Sci, 2017; 7 (02): 106-113.
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