Format

Send to

Choose Destination
See comment in PubMed Commons below
AAPS PharmSciTech. 2013 Mar;14(1):294-300. doi: 10.1208/s12249-012-9915-z. Epub 2013 Jan 10.

Development and evaluation of α-asarone transdermal patches based on hot-melt pressure-sensitive adhesives.

Author information

1
Sir Run Run Shaw Hospital, College of Medicine, Zhejiang University, Hangzhou, People's Republic of China.

Abstract

A hot-melt, pressure-sensitive adhesive (HMPSA) based on styrene-isoprene-styrene was prepared, and its compatibility with various transdermal penetration enhancers was investigated. The effect of penetration enhancers on the adhesion properties of HMPSA was also studied. A drug-in-adhesive patch was formulated using α-asarone as a model drug, and penetration enhancers were screened by an in vitro transdermal study across excised pig skin. The pharmacokinetics in rabbits was also studied. The results show that HMPSA was miscible with most penetration enhancers (azone, menthol, isopropyl myristate, 1-methyl-pyrrolidinone, N,N-dimethylformamide, oleic acid), apart from propylene glycol. Penetration enhancers had a plasticizer-like effect that decreased the peel strength and shear strength of HMPSA. A combination of 1% oleic acid and 4% menthol had the highest in vitro penetration rate and was selected for patch preparation. The patch formulation was optimized by replacing some of the plasticizer by penetration enhancers to achieve good adhesion and effective transdermal flux. The final patch showed a high efficiency, with a relative bioavailability of 1,494%. This suggests that HMPSA may be a promising material for drug-delivery patches.

PMID:
23307595
PMCID:
PMC3581663
DOI:
10.1208/s12249-012-9915-z
[Indexed for MEDLINE]
Free PMC Article
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Springer Icon for PubMed Central
    Loading ...
    Support Center