Sonia Pandey1, Sanganala Mattha Vijayendra Swamy2, Udhshu Mansha Ubaid Ulla3, Arti Gupta1, Hetal Patel1, Jitendra Singh Yadav4.
Abstract
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
Entities:
Keywords:
Cytotoxicity; capecitabine; controlled release; factorial design; nanoparticles; targeting
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Year: 2017
PMID： 27538461 DOI： 10.2174/1567201813666160817150621
Source DB: PubMed Journal: Curr Drug Deliv ISSN： 1567-2018 Impact factor: 2.565