Original scientific paper

https://doi.org/10.2478/acph-2013-0033

Preparation and evaluation of chitosan based thermoreversible gels for intraperitoneal delivery of 5-fluorouracil (5-FU)

BHAVESH P. DEPANI ; Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (E),
ANUJA A. NAIK ; Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (E),
HEMA A. NAIR ; Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (E),

Abstract

Sterile thermoreversibly gelling systems based on chitosan-glycerol phosphate were developed for intraperitoneal delivery of the antineoplastic agent 5-FU. The formulation was evaluated for gelling characteristics and in vitro drug release. Drug free gels were evaluated for in vitro cytotoxicity in L-929 mouse fibroblast cells. Drug loaded gels were subjected to acute toxicity studies in Swiss albino mice via intraperitoneal route and efficacy studies via intratumoral injections in subcutaneous colon carcinoma bearing BALB/c mice. The formulations gelled reversibly in 8 min at 37 oC and provided prolonged release of the drug. Drug free systems showed dose dependent cytotoxicity in fibroblast cells, while in vivo studies revealed a 2.8 fold increase in LD50 of 5-FU administered intraperitonealy as the developed system. Tumor volume measurements showed comparable efficacy of 5-FU administered as gel and commercial injection with greatly improved safety profile of the former as adjudged from mortality and body weight measurements.

Keywords

chitosan; glycerophosphate; thermoreversible gels; intraperitoneal; 5-fluorouracil

Hrčak ID:

110456

URI

https://hrcak.srce.hr/110456

Publication date:

31.12.2013.

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