Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Development and In vitro Evaluation of Betahistine Adhesive-Type Transdermal Delivery System

Ashish A Heda¹ , Aravind R Sonawane¹, Gautam H Naranje¹, Vijay G Somani², Prashant K Puranik¹

¹Department of Pharmaceutics, Government College of Pharmacy, Osmanpura, Aurangabad (M.S.); ²Themis Laboratories, R&D Centre, Thane, Mumbai, India.

For correspondence:- Ashish Heda Email: aaheda@rediffmail.com Tel:+919890360133

Received: 26 January 2010 Accepted: 16 September 2010 Published: 23 December 2010

Citation: Heda AA, Sonawane AR, Naranje GH, Somani VG, Puranik PK. Development and In vitro Evaluation of Betahistine Adhesive-Type Transdermal Delivery System. Trop J Pharm Res 2010; 9(6):516-524 doi: 10.4314/tjpr.v9i6.1

© 2010 The authors.
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Abstract

Purpose: To develop a transdermal betahistine (BTH) delivery system using different pressure sensitive adhesives (PSAs) including acrylics, polyisobutylene and styrenic rubber solution.

Methods: Formulations were prepared by solvent casting and adhesive transfer method. PSAs - acrylate vinylacetate (AVA), hydrophilic acrylate (HA), acrylic non-curing (ANC), polyisobutylene (PIB), and tackified styrenic rubber solution (TSR) - were evaluated for their suitability in terms of miscibility, maximum drug loading, effect on tack property and in vitro permeation through excised guinea pig skin. Furthermore, one of the PSAs was tested in relation to effect of penetration enhancers on tack property, in vitro permeation, in vivo patch adhesion performance and stability.

Results: Only formulations prepared with AVA and HA were stable. Increased drug loading in these PSAs significantly reduced tack. In vitro permeation data across guinea pig skin demonstrated that BTH flux from from the formulation containing HA (F1) was significantly (p < 0.001) higher than that containing AVA (F2). Formulations containing 2 % enhancer showed good tack. Specifically, the formulation containing 2 % oleic acid as enhancer not only showed the highest permeation but also good tack property, non-irritancy for up to 36 h and stability under accelerated conditions.

Conclusion: The formulation containing HA as the PSA and 2 % oleic acid as enhancer demonstrated a good potential for further development to an adhesive-type transdermal delivery system for BTH.

Keywords: Meniereâ€™s syndrome, Transdermal delivery, Betahistine, Pressure-sensitive adhesives, Penetration enhancers