Optimization of Capecitabine Loaded Polymeric Nanoparticles for Colon Targeted Drug Delivery

Abstract

The study set out to develop and assess Capecitabine-loaded nanoparticles for the treatment of colon cancer. An exhaustive screening and optimisation design were applied to scrutinise all possible parameters during the preparation of nanoparticles. The Box-Behnken design was used to optimise the nano formulation by incorporating it in the State Ease Design Expert 13 Trial Version. Capecitabine-loaded pectin nanoparticle (CPN) was prepared by the ionic gelation method using a cross-linker, i.e., tripolyphosphate (TPP). FTIR analysis of the nanoparticle formulation showed no interaction between the drug and excipients. The results of the optimised Capecitabine nanoparticles were as follows: particle size of 239.42 nm, zeta potential of 17.5 mV, and 100 nm SEM images. Thermal analysis and PXRD results were found to be within the acceptable range. The cumulative drug release of the Capecitabine-loaded nanoparticles was found to be more than 80% after 8 hours. The MTT assay was used to evaluate the percentage of inhibition of the Capecitabine nanoparticle formulation on the Caco-2 cell line, resulting in a notable rate of cell death within 48 hours and decreased cell viability. Stored samples were evaluated for stability screening such as particle size, entrapment efficiency, drug release in 0.1 HCl and 7.4 PBS, and drug content at one-month intervals. The formulation remained stable at 25°C/60% RH and 40°C/75°RH under accelerated conditions after 6 months. According to the results of the current study, colon cancer cells are resistant to the effects of capecitabine-loaded nanoparticles.