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ISSN 2063-5346
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BOX BEHNKEN DESIGN BASED FORMULATION OPTIMIZATION AND CHARACTERIZATION OF GALLIC ACID LOADED PHYTOSOMES

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Rashita Makkar, Tapan Behl, Sukhbir Singh, Neelam Sharma, Abhishek Chauhan, Hardeep Singh Tuli
» doi: 10.31838/ecb/2023.12.4.170

Abstract

The current investigation aims to synthesize gallic acid (GA) based phytosomes formulation using phosphatidylcholine by solvent evaporation technique with the prime objective of dissolution enhancement of GA. Box-Behnken Design was used to analyze the effect of drug: lipid concentration (X1), reflux time (X2) and reflux temperature (X3) on dependent variables i.e. entrapment efficiency (Y1), yield % (Y2) and drug loading (Y3) using Design-expert software. The fourier transform infrared spectroscopy and x-ray diffraction (XRD) studies confirmed the absence of any incompatibilities between the drug-polymer and indicated successful incorporation of GA in optimized phytosome. It was determined that the quadratic model was distinctive to best describe the statistical analysis of GA loaded phytosomes on the basis of its insignificant p-value (p > 0.05) for lack of fit analysis and significant p-value for model (p < 0.05). The quadratic equation for response variables were: Y1= 60.48+15.48X1-0.4650 X2-1.96 X3-0.0975X1X2+1.90 X1X3-1.54 X2X3+14.35X1²- 0.9220X2²+0.2655X3²; Y2 = +55.99+15.43X1-0.4375X2-1.98X3-0.2025X1X2+1.69X1X3- 1.58X2X3+14.11X1²-0.9450X2² + 0.2225X3² and Y3=15.12-0.8525X1-0.1062X 2 - 0.5713X3+0.0050X1X2+0.6400X1X3-0.3875X2X3+3.81X1²-0.2938 X2²+0.1313X3². The formulation and processing conditions for optimized GAP were 1:3 of drug: lipid (w/w), reflux time of 3.8 hours and reflux temperature of 80°C with desirability function of 0.861. The finalized batch of GA phytosomes showed entrapment efficiency of 91.63%, process yield of 86.65% and drug loading of 18.48%. The study established that phytosomes produced an increase in dissolution of GA by 1.97- fold, 1.63-fold, 1.38-fold and 1.86-fold at 1, 2, 6 and 24 hours, respectively. The in-vitro dissolution profile of GAP confirmed that in concurrent to dissolution rate enhancement, the phytosomes demonstrated sustained release pattern till 24 hours. The current research conclusively demonstrated that phytosomes hold an enormous potential role as drug delivery design to enhance the dissolution of phytoconstituents in conjunction with sustained behaviour.

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