Development and characterization of chitosan-polycarbophil interpolyelectrolyte complex-based 5-fluorouracil formulations for buccal, vaginal and rectal applicationReport as inadecuate




Development and characterization of chitosan-polycarbophil interpolyelectrolyte complex-based 5-fluorouracil formulations for buccal, vaginal and rectal application - Download this document for free, or read online. Document in PDF available to download.

DARU Journal of Pharmaceutical Sciences

, 20:67

First Online: 25 October 2012Received: 15 June 2012Accepted: 08 August 2012

Abstract

Background of the studyThe present investigation was designed with the intention to formulate versatile 5-fluorouracil 5-FU matrix tablet that fulfills the therapeutic needs that are lacking in current cancer treatment and aimed at minimizing toxic effect, enhancing efficacy and increasing patient compliance. The manuscript presents the critical issues of 5-FU associate with cancer and surpasses issues by engineering novel 5-FU matrix tablets utilizing chitosan- polycarbophil interpolyelectrolyte complex IPEC.

MethodsPrecipitation method is employed for preparation of chitosan and polycarbophil interpolyelectrolyte complex IPEC followed by characterization with Fourier transform infrared spectroscopy FT-IR, Differential Scanning calorimeter DSC and X-ray Diffraction XRD. 5-FU tablets were prepared by direct compression using IPEC. Six formulations were prepared with IPEC alone and in combination with chitosan, polycarbophil and Sodium deoxycholate. The formulations were tested for drug content, hardness, friability, weight variation, thickness, swelling studies, in vitro drug release buccal, vaginal and rectal pH, ex vivo permeation studies, mucoadhesive strength and in vivo studies.

ResultsFT-IR studies represent the change in spectra for the IPEC than single polymers.DSC study represents the different thermo gram for chitosan, polycarbophil and IPEC whereas in X-ray diffraction, crystal size alteration was observed. Formulations containing IPEC showed pH independent controlled 5-FU without an initial burst release effect in buccal, vaginal and rectal pH. Furthermore, F4 formulations showed controlled release 5-FU with highest bioadhesive property and satisfactory residence in both buccal and vaginal cavity of rabbit. 3% of SDC in formulation F6 exhibited maximum permeation of 5-FU.

ConclusionThe suitable combination of IPEC, chitosan and polycarbophil demonstrated potential candidate for controlled release of 5-FU in buccal, vaginal and rectal pH with optimum swelling approaching zero order release.

KeywordsChitosan Polycarbophil Interpolyelectrolyte complex pH independent drug release Electronic supplementary materialThe online version of this article doi:10.1186-2008-2231-20-67 contains supplementary material, which is available to authorized users.

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Author: Mohamed S Pendekal - Pramod K Tegginamat

Source: https://link.springer.com/







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