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Design Development and Statistical Optimization of Capecitabine Loaded PH Sensitive Nanoparticle for Colon Targeted Delivery: Cell line study
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| Author:
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SONIA PANDEY, S.M.VIJAYENDRA SWAMY, ANIL BHANDARI, AKSHAY KOLI , ARTI GUPTA , JITENDRA SINGH YADAV
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| Abstract:
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Drug based polymeric nanoparticle (NP) formulations have gained considerable attention over the past decade for their use in various drug formulations. NPs have been shown to increase bioavailability, decrease side effects of highly toxic drugs, and prolong drug release. The present study aimed to statistically optimize a colon specific formulation of capecitabine(CAP) for the treatment of colon cancer.A 32 full factorial design was used for optimization. The independent variables employed were drug: Eudragit S100 and % of PVA, each at three levels.The evaluated responses were particle size,% entrapment efficiency,PDI and cumulative drug release (% CDR) at 10 hr. The optimized formulation was also evaluated for cytotoxic potential using HT-29 human colon cancer cell lines. The prepared nanoparticles were almost spherical in shape, as determined by SEM. The nanoparticles with varied size 80–125.3 nm, 17.58–68.59% of entrapment efficiency andupto 52% controlled released were obtained at the end of 10 hr. The optimum formulation (B6) consisted of Drug: Eudragits100 ratio (1:10) and (0.3) % of PVA was found to fulfill the maximum requisite of the formulation. At a concentration of 50µg/ml - 500µg/ml % cytotoxicity potential of optimized formulation gets increased. The particle size and encapsulation efficiencies depended on the concentration of %PVAand drug: Eudragit S100 in the blend. These data also demonstrated the efficacy of these nanoparticles for controlling the capecitabine(CAP) release profile.
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Nanoparticles, Capecitabine, Eudragir S 100, PVA, Colonic delivery
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