Cytotoxicity and Pharmacokinetic Studies of PLGA Based Capecitabine Loaded Nanoparticles

Background: Colorectal cancer ranked fourth as devastating cancer globally based on statistical death analysis. The major challenge for treating colorectal cancer is to target the drug to the specific site of the colon. Purpose: The main objective of the present research was to develop PLGA based nanoparticles to target and sustain the drug release at the colon for effective treatment of colorectal cancer. The significance of using Eudragit S100 was to prevent drug release in the stomach and small intestine whereas the significance of PLGA is to sustain drug release by its mucoadhesion property. Methods: Nanoparticles were prepared by modified nanoprecipitation method and the cytotoxicity study was performed by MTT assay. Results: From the cytotoxicity study it was found that Capecitabine loaded PLGA based nanoparticles had more capacity to inhibit HT 29 cell lines than that of the pure drug for all concentrations (10 to 0.0001). Pharmacokinetic (PK) study for the aqueous suspension of Capecitabine and optimized formulation ratified the results of in vitro study. The Area under the curve (AUC) for nanoparticles formulation was found to be twice more than the pure drug indicating better bioavailability. Conclusion: The PLGA based nanoparticles can be better targeted to colon for effective treatment of colorectal cancer.