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Capecitabine encapsulated chitosan succinate-sodium alginate macromolecular complex beads for colon cancer targeted delivery: in vitro evaluation

Sinha, Priyanka, Udhumansha, Ubaidulla, Rathnam, Grace, Ganesh, Mani, Jang, Hyun Tae
International journal of biological macromolecules 2018 v.117 pp. 840-850
alginates, apoptosis, calcium chloride, chitosan, colon, colorectal neoplasms, drugs, electrostatic interactions, experimental design, in vitro studies, ionization, neoplasm cells, pH, response surface methodology, succinic acid, toxicity testing
The present study aims to investigate the efficacy of the novel biopolymeric complex multiparticulate system consisting of chitosan succinate and alginate for the capecitabine-targeted delivery to colon cancer. A Box-Behnken design was used to optimize the CS-SA beads by considering the effect of three factors: CS (A;X1), CaCl2 (B;X2), and SA (C;X3), on the response variables Y1 (EE), Y2 (Size), and Y3 (Release). The results of response surface plots allowed an optimized bead to be identified with high drug EE and maximum drug release at colon. The swelling index showed that the beads reached a maximum good swelling at pH 7.4, and nil or little swelling at acidic pH, which proves that the beads completely protect the release of drug. The in vitro release portrayed a maximum release at pH 7.4, due to the large swelling force that was created by electrostatic repulsion between the ionized carboxylic acid groups of the CS-SA network. In vitro cytotoxicity assay (MTT) of CS-SA beads shows inhibition of the proliferation of HT-29 tumour cell to induce apoptosis over a longer period of time. The above results show that CS-SA beads prolong the release of CP in the colonic region, and also enhance antitumor efficacy.