Journal Article

Chemotherapeutic potential of alginate–chitosan microspheres as anti-tubercular drug carriers

Rajesh Pandey and G. K. Khuller

in Journal of Antimicrobial Chemotherapy

Published on behalf of British Society for Antimicrobial Chemotherapy

Volume 53, issue 4, pages 635-640
Published in print April 2004 | ISSN: 0305-7453
Published online April 2004 | e-ISSN: 1460-2091 | DOI: http://dx.doi.org/10.1093/jac/dkh139
Chemotherapeutic potential of alginate–chitosan microspheres as  anti-tubercular drug carriers

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Objectives: This study was designed to develop alginate–chitosan microspheres as drug carriers to reduce dose/dosing frequency in the management of tuberculosis (TB), which otherwise demands prolonged chemotherapy.

Methods: Alginate–chitosan microspheres encapsulating three frontline anti-tuberculous drugs (ATDs), rifampicin, isoniazid and pyrazinamide, were formulated. A therapeutic dose and a half-therapeutic dose of the microsphere-encapsulated ATDs were orally administered to guinea pigs for pharmacokinetic/chemotherapeutic evaluations, respectively.

Results: The drug encapsulation efficiency ranged from 65% to 85% with a loading of 220–280 mg of drug per gram microspheres. Administration of a single oral dose of the microspheres to guinea pigs resulted in sustained drug levels in the plasma for 7 days and in the organs for 9 days. The half-life and mean residence time of the drugs were increased 13- to 15-fold by microsphere encapsulation, along with an enhanced relative/absolute bioavailability. The sustained release and increase in bioavailability were also observed with a sub-therapeutic dose of the microspheres. In Mycobacterium tuberculosis H37Rv-infected guinea pigs, administration of a therapeutic dose of microspheres spaced 10 days apart produced a clearance of bacilli equivalent to conventional treatment for 6 weeks. The most important observation, however, was the documentation of therapeutic benefit with a half-therapeutic dose of the microspheres administered weekly.

Conclusion: Alginate–chitosan microspheres hold promise as a potential natural polymer-based oral ATD carrier for better management of TB.

Keywords: Keywords: tuberculosis, polymers, bioavailability, chemotherapy

Journal Article.  4157 words.  Illustrated.

Subjects: Medical Oncology ; Critical Care

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