In-vitro and in-vivo evaluation of polymeric microsphere formulation for colon targeted delivery of 5-fluorouracil using biocompatible natural gum katira

Saumen Karan; Souvik Debnath; Ketousetuo Kuotsu; Tapan Kumar Chatterjee

doi:10.1016/j.ijbiomac.2020.04.129

In-vitro and in-vivo evaluation of polymeric microsphere formulation for colon targeted delivery of 5-fluorouracil using biocompatible natural gum katira

Int J Biol Macromol. 2020 Apr 23:158:922-936. doi: 10.1016/j.ijbiomac.2020.04.129. Online ahead of print.

Authors

Saumen Karan¹, Souvik Debnath², Ketousetuo Kuotsu³, Tapan Kumar Chatterjee⁴

Affiliations

¹ Division of Pharmacology, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India.
² Division of Pharmacology, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India; Department of Basic Medical Sciences, Purdue University, USA.
³ Division of Pharmaceutics, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India.
⁴ Division of Pharmacology, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India; Department of Pharmaceutical Science and Technology, JIS University, Kolkata, India. Electronic address: tkchatterjee_81@rediffmail.com.

PMID: 32335117
DOI: 10.1016/j.ijbiomac.2020.04.129

Abstract

The aim was to develop oral site-specific rate-controlled anticancer drug delivery to pacify systemic side-effects and offer effective and safe therapy for colon cancer with compressed dose and duration of treatment. The double emulsion solvent evaporation method was employed. To check functionality, DAPI-staining and in-vivo anticancer study of Ehrlich Ascites Carcinoma bearing mice was tested. Histopathology of liver and kidney and Cell morphology of EAC cell was also performed. Formulated and optimized polymeric microsphere of 5-FU showed excellent physicochemical features. In-vitro, DAPI results pointed drug-treated groups displayed the prominent feature of apoptosis. The percentage of apoptotic of entrapped drug played in a dose-dependent manner. Significant decreases in EAC liquid tumors and increased life span of treated mice were observed. Rate of variation of cell morphology was more in 5-FU loaded microsphere than 5-FU injection. Hematological and biochemical parameter's and Histopathology of liver and kidney resulted that due to control released formulation have slow release rate, that gives less trace on liver and kidney function. Finally, we foresee that polymeric microsphere of 5-FU applying natural gum katira could be an assuring micro-carrier for active colon targeting delivery tool with augmented chemotherapeutic efficacy and lowering side effect against colon cancer.

Keywords: 5-Fluorouracil; Colon cancer; Colon targeted drug delivery; DAPI staining; Ehrlich ascites carcinoma (EAC) cell.