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Current Drug Delivery


ISSN (Print): 1567-2018
ISSN (Online): 1875-5704

Research Article

Cell Line and Augument Cellular Uptake Study of Statistically Optimized Sustained Release Capecitabine Loaded Eudragit S100/PLGA(poly(lacticco- glycolic acid)) Nanoparticles for Colon Targeting

Author(s): Sonia Pandey*, Sanganala Mattha Vijayendra Swamy, Udhshu Mansha Ubaid Ulla, Arti Gupta, Hetal Patel and Jitendra Singh Yadav

Volume 14, Issue 6, 2017

Page: [887 - 899] Pages: 13

DOI: 10.2174/1567201813666160817150621

Price: $65


Background: Capecitabine, an anti cancer drug, has a very short drug elimination half-life (0.49 to 0.89 h). High doses and absence of targeting ability in the colon region may lead to more side effects to the patients with colon cancer.

Purpose: To develop and optimize sustained release nanoparticles for effective treatment of colon cancer.

Methods: Eudragit S100-PLGA(poly (lactic-co-glycolic acid)) nanoparticles were prepared by a double emulsification, solvent evaporation method followed by high-pressure homogenisation evaluated and the particles were evaluated for surface morphology, particle size analysis, polydispersity index, drug content, % entrapment efficiency and in vitro drug release. To optimize the batch a 32 full factorial design was applied. The optimized batch was evaluated for cytotoxicity and cellular uptake study.

Results and Discussion: The optimized formulation exhibited 179.25 nm mean particle size, 71.27% of drug entrapment efficiency and 81.824% drug release up to 72 h. When the concentration of capecitabine was increased from 50-500 μg/ml, the % cytotoxicity of nanoparticles and capecitabine (pure drug) increased from 8.5 to 97.70% and 2.7 to 82.23%, respectively. As per a cellular uptake study, the optimized nanoparticles were completely uptaken by HT 29 adenocarcinoma cells within 2 to 4 h.

Conclusion: Optimized Eudragit S100-PLGA nanoparticles are a promising delivery system for colon targeting.

Keywords: Cytotoxicity, controlled release, capecitabine, factorial design, nanoparticles, targeting.

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