Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Formulation and evaluation of topical halofuginone gel using a novel ex vivo model

Awatef Sassi^1,2 , Balcem Kacem³, Amel Hassairi¹, Mehdi Jaidane¹, Saad Saguem¹

¹Metabolic Laboratory of Biophysics and Applied Occupational and Environmental Toxicology, Faculty of Medicine, University of Sousse; ²Faculty of Science of Bizerte, Zarzouna; ³Chemical, Pharmacological and Pharmaceutical Drug Development, Faculty of Pharmacy, Monastir, Tunisia.

For correspondence:- Awatef Sassi Email: awatefsassi@yahoo.com Tel:+216992882691

Accepted: 20 April 2018 Published: 28 May 2018

Citation: Sassi A, Kacem B, Hassairi A, Jaidane M, Saguem S. Formulation and evaluation of topical halofuginone gel using a novel ex vivo model. Trop J Pharm Res 2018; 17(5):755-760 doi: 10.4314/tjpr.v17i5.1

© 2018 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..

Abstract

Purpose: To formulate and study the kinetics of delivery and retention of three halofuginone (HF) gels via different wall layers of an ex vivo model mimicking urethral tissue.

Methods: Three HF hydrogels (a, b and c) of the same concentration (0.03 % w/v) incorporating different levels of sodium carboxymethyl cellulose (Na-CMC), were prepared. The viscosity of the different gels was studied at 37 °C and at room temperature. The release of HF from these hydrogels and its diffusion into urethral tissue were evaluated using a new ex vivo model mimicking human urethral tissue. The amount of HF was determined by HPLC method.

Results: The release of HF increased with increasing viscosity and duration of contact. Gel c showed the best drug release after 2 h of diffusion, with 65.7 % HF in the wall of the ureter. The model showed a uniform distribution of the drug throughout the ureter tissue. In comparison, HF was not detected in the receiver compartment until 2 h.

Conclusion: Topical HF gel application is a suitable solution for the potential treatment of urethral stricture and/or recurrence. The formulation and characterization of the ureter model should facilitate the development of new therapeutics for urethral diseases.

Keywords: Halofuginone gel, Urethra, Wall diffusion, Urethral stenosis