Abstract

The objective of this research work was to increase the dissolution and bioavailability of C. sativum extract in order to increase its therapeutic applications. To achieve this goal, nanosuspensions of ethanolic extract of C. sativum were prepared with six different stabilizers afterwards other formulation conditions were optimized with response surface methodology (RSM). Dimensions and morphology of optimized nanosuspension was determined by employing atomic force microscopy (AFM) and scanning electron microcopy. Based on the initial stabilizer screening study, sodium lauryl sulphate was selected as stabilizer for the development of nanosuspension of C. sativum. Optimization study by RSM recommended 1% concentration of stabilizer, antisolvent/solvent ratio of 15:1 and stirring time of 2hrs to formulate optimum nanosuspension of C. sativum. Under optimum conditions, nanosuspension of C. sativum with mean particle size 72.08 nm, polydispersity index 0.408 and zeta potential of 55 mV was successfully developed. Optimized nanosuspension showed almost 2.6 folds enhanced dissolution rate and greater plasma concentration of quercetin in nanosuspension administrated rats as compared to coarse suspension. AFM study demonstrated homogenous and narrow distribution of C. sativum nanoparticles with approximate size of 5–7 nm in height and 200–500 nm in width. It was concluded from the current research that fabrication of nanosuspension of C. sativum was an economical approach to increase its oral bioavailability.

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