Percutaneous absorption enhancement of leuprolide.

Abstract:

:Chemical enhancers and vehicles were tested for their ability to improve the percutaneous absorption of leuprolide, a nonapeptide (luteinizing hormone releasing hormone analogue; MW 1209.4). In vitro permeabilities in nude mouse, snake, and cadaver skin were evaluated in either Franz diffusion cells or a Bronaugh flow-through system using an HPLC assay. Skin irritation caused by the formulations was evaluated in the rabbit. The chemical enhancer systems investigated strongly enhanced skin penetration of leuprolide. Maximum permeability enhancement of leuprolide acetate can be achieved with a nonirritating formulation containing ethanol, menthol, camphor, methyl salicylate, urea, and hydrogel. The in vitro permeability in nude mouse skin was 10 or 100 times higher than that obtained in cadaver skin, depending on the type of enhancer that was used in the formulation. Snake skin was at least 10 times less permeable than cadaver skin in this study. However, the effects of chemical enhancers on skin permeability were highly dependent on the skin model. Further, the in vitro permeability of leuprolide in the base form was 10 times higher than in the acetate form with the enhancers.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Lu MY,Lee D,Rao GS

doi

10.1023/a:1015860324161

subject

Has Abstract

pub_date

1992-12-01 00:00:00

pages

1575-9

issue

12

eissn

0724-8741

issn

1573-904X

journal_volume

9

pub_type

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