Evaluation of β-blocker Gel and Effect of Dosing Volume for Topical Delivery

Although topical administration of β-blockers is desired because of the improved therapeutic efficacy and reduced systemic adverse effects compared with systemic administration in the treatment of infantile hemangioma, the permeation of β-blockers across skin under finite dose conditions has not bee...

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Bibliographic Details
Published in:	Journal of pharmaceutical sciences 2015-05, Vol.104 (5), p.1721-1731
Main Authors:	Zhang, Qian, Chantasart, Doungdaw, Kevin Li, S.
Format:	Article
Language:	eng
Subjects:	Administration, Topical Adrenergic beta-Antagonists - administration & dosage Adrenergic beta-Antagonists - pharmacokinetics Adult Aged diffusion Dose-Response Relationship, Drug Drug Delivery Systems - methods Drug Evaluation, Preclinical - methods finite dose Gels - administration & dosage Gels - pharmacokinetics hemangioma Humans Male Middle Aged occlusion Organ Culture Techniques partition coefficient percutaneous skin Skin Absorption - drug effects Skin Absorption - physiology stability topical Young Adult β-blocker
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Summary:	Although topical administration of β-blockers is desired because of the improved therapeutic efficacy and reduced systemic adverse effects compared with systemic administration in the treatment of infantile hemangioma, the permeation of β-blockers across skin under finite dose conditions has not been systematically studied and an effective topical β-blocker formulation for skin application is not available. The present study evaluated the permeation of β-blockers propranolol, betaxolol, and timolol across human epidermal membrane (HEM) from a topical gel in Franz diffusion cells in vitro under various dosing conditions. The effects of occlusion and dosing volume on percutaneous absorption of β-blockers from the gel were studied. The permeation data were compared with those of finite dose diffusion theory. The results showed that skin permeation of β-blockers generally could be enhanced two to three times by skin occlusion. The cumulative amounts of β-blockers permeated across HEM increased with increasing dosing volume. An adequate fit was obtained between the theoretical curve and experimental permeation data, indicating that the experimental results of the gel are consistent with finite dose diffusion theory. In conclusion, the findings suggest the feasibility of using topical gels of β-blockers for infantile hemangioma treatment and topical application with skin occlusion is preferred.
ISSN:	0022-3549 1520-6017