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A novel transdermal nanoethosomal gel of betahistine dihydrochloride for weight gain control: in-vitro and in-vivo characterization

Authors El-Menshawe SF, Ali AA, Halawa AA, Srag El-Din AS

Received 22 June 2017

Accepted for publication 18 October 2017

Published 28 November 2017 Volume 2017:11 Pages 3377—3388

DOI https://doi.org/10.2147/DDDT.S144652

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Amy Norman

Peer reviewer comments 3

Editor who approved publication: Dr Sukesh Voruganti

Shahira F El-Menshawe,1 Adel Ahmed Ali,1 Abdelkhalk Ali Halawa,2 Ahmed SG Srag El-Din2

1Department of Pharmaceutics and Industrial Pharmacy, Beni-Suef University, Beni-Suef, 2Department of Pharmaceutics and Clinical Pharmacy, Nahda University, Beni-Suef, Egypt

Background: Betahistine dihydrochloride (BDH) is a histamine analog used to control weight gain, with short elimination half-life and gastric irritation as side effects.
Objective: The aim of the current investigation is to formulate and optimize a topical BDH ethosomal gel for weight gain control.
Materials and methods: Box–Behnken design was applied to study the effect of independent variables: phosphatidylcholine (PC), propylene glycol (PG), and ethanol on vesicle size; entrapment efficiency; % drug release; and flux. The morphology and zeta potential of the optimized formulation were evaluated. The % drug release, flux, and pharmacodynamics of the optimized formulation gel were studied.
Results: The size and entrapment efficiency percent had a direct positive relationship with the concentration of PC and negative relationship with ethanol and PG. The % drug release and flux decreased with increasing PC and PG, while ethanol enhanced both responses. Regression modeling indicated a good correlation between dependent and independent variables, where F16 was chosen as the optimized formulation. F16 showed well-defined spherical vesicles and zeta potential of −24 mV, and % release from the gel exceeded 99.5% over 16 h with the flux of 0.28 mg/cm2/h. Food intake and weight gain of rats were significantly decreased after transdermal application of the BDH ethosomal gel when compared with control, placebo, and BDH gel. The histopathological findings proved the absence of inflammation and decrease in adipose tissue.
Conclusion: Results obtained showed a significant, sustained transdermal absorption of BDH ethosomal gel and, consequently, a decrease in food intake and weight gain.

Keywords:
Box–Behnken design, regression modeling, neural histamine, pharmacodynamics, obesity

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