Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

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

Hina Raza¹ , Nazar Muhammad Ranjha¹, Asif Mahmood², Farooq Azam², Rai Muhammad Sarfraz³, Zermina Rashid⁴

¹Department of Pharmacy, Bahauddin Zakariya University, Multan; ²Institute of Pharmacy, Physiology and Pharmacology, University of Agriculture, Faisalabad; ³Faculty of Pharmacy, University of Sargodha, 4Department of Pharmacy, Women University, Multan, Pakistan.

For correspondence:- Hina Raza Email: hinaaitzaz01@gmail.com Tel:+923057905890

Accepted: 18 January 2018 Published: 28 February 2018

Citation: Raza H, Ranjha NM, Mahmood A, Azam F, Sarfraz RM, Rashid Z. Development and in vitro characterization of 5-flurouracil-loaded, colon-targeted drug delivery system. Trop J Pharm Res 2018; 17(2):195-204 doi: 10.4314/tjpr.v17i2.1

© 2018 The authors.
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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