J Appl Biomed 16:192-197, 2018 | DOI: 10.1016/j.jab.2017.12.003

Influence of skin permeation enhancers on the transdermal delivery of palonosetron: An in vitro evaluation

Anroop B. Naira,*, Shery Jacobb, Bandar E. Al-Dhubiaba, Rakan Naser Alhumama
a King Faisal University, College of Clinical Pharmacy, Department of Pharmaceutical Sciences, Al-Ahsa, Saudi Arabia
b Gulf Medical University, College of Pharmacy, Department of Pharmaceutical Sciences, Ajman, United Arab Emirates

It is proposed that the low skin permeation potential of palonosetron could be enhanced by the inclusion of chemical permeation enhancers. The objective of this study is to evaluate the influence of various chemical enhancers on the transdermal permeation of palonosetron. Different drugs in adhesive transdermal patches (F1-F5) were prepared using five pressure sensitive adhesives; Duro-Tak 87-4098, Duro-Tak 87-2074, Duro-Tak 87-900A, Duro-Tak 87-9301 and Duro-Tak 87-2287. Patches prepared using Duro-Tak 87-9301 (F5) was further combined with four well-known chemical enhancers. The influence of permeation enhancers (propylene glycol, diethylene glycol monoethyl ether, Tween 80 and oleic acid) on the transdermal flux was evaluated ex vivo. Release of the drug from fabricated patches was carried out for a period of 6 h. Greater amount of drug (12% w/w) was incorporated in the patches prepared using Duro-Tak 87-9301 (F5). Incorporation of skin permeation enhancers significantly (P < 0.001) improves the transdermal flux of palonosetron. Among the permeation enhancers, propylene glycol (5% w/w) shows highest permeation (53.12 ± 5.62 μg/cm2/h), which is ∼4 folds higher than control. Biphasic drug release was noticed in the prepared patches and the rate of release was relatively high with patch F7. This study reveals that the optimized transdermal system with propylene glycol as permeation enhancers can provide effective therapeutic level of palonosetron.

Keywords: Palonosetron; Transdermal; Adhesive; Enhancers; Release

Received: July 21, 2017; Revised: October 30, 2017; Accepted: December 12, 2017; Published: August 1, 2018  Show citation

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Nair AB, Jacob S, Al-Dhubiab BE, Naser Alhumam R. Influence of skin permeation enhancers on the transdermal delivery of palonosetron: An in vitro evaluation. J Appl Biomed. 2018;16(3):192-197. doi: 10.1016/j.jab.2017.12.003.
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