Title: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
Volume: 14
Issue: 6
Author(s): Sonia Pandey*, Sanganala Mattha Vijayendra Swamy, Udhshu Mansha Ubaid Ulla, Arti Gupta, Hetal Patel and Jitendra Singh Yadav
Affiliation:
- Department of Pharmaceutics, Maliba Pharmacy College, Bardoli Mahuva Road, Dist. Surat, Gujarat 394350,India
Keywords:
Cytotoxicity, controlled release, capecitabine, factorial design, nanoparticles, targeting.
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.