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Development and in vitro characterization of 5-flurouracilloaded, colon-targeted drug delivery system


Hina Raza
Nazar Muhammad Ranjha
Asif Mahmood
Farooq Azam
Rai Muhammad Sarfraz
Zermina Rashid

Abstract

Purpose: To prepare chondroitin sulphate–polyvinyl alcohol cross-linked microcapsules (miCAPs) for controlled delivery of 5-flurouracil (5-FU) in cancer patients.

Method: Nine different miCAP formulations were prepared using emulsion cross-linking procedure. The formulations were evaluated for their physicochemical properties, complex formation, stability at variable temperatures, safety, as well as drug-loading and drug-release characteristics. The effects of glutaraldehyde (GA), polymer concentration and stirring speed on 5-FU release at various pH were also assessed.

Results: One of the miCAP formulations (miCAP-1) was adjudged the most suitable based on its particle size, high drug loading (75.3 %, p = 0.034), and high entrapment efficiency (85.2 %, p = 0.031). Best-fit drug release model was Higuchi model based on regression coefficient value (R2) while drug release mechanism was Fickian.

Conclusion: Highly stable, crosslinked, amorphous and drug delivery system has been successfully developed. The delivery system is potentially suitable for acid-sensitive therapeutic moieties and where controlled release is desired.

Keywords: Emulsion cross-linking, Colon-specific delivery, 5-Flurouracil, Glutaraldehyde, Kinetic models


Journal Identifiers


eISSN: 1596-9827
print ISSN: 1596-5996