Design and Evaluation of a Monolithic Drug-in-Adhesive Patch for Testosterone Based on Styrene–Isoprene–Styrene Block Copolymer

The purpose of the present study was to design and evaluate a monolithic drug-in-adhesive patch with a novel pressure-sensitive adhesive (PSA) matrix based on styrene–isoprene-styrene (SIS) block copolymer. Testosterone was selected as the model drug. The orthogonal array design for ternary mixtures...

Full description

Saved in:
Bibliographic Details
Published in:Journal of pharmaceutical sciences 2013-07, Vol.102 (7), p.2221-2234
Main Authors: Ma, Jianfang, Wang, Chengxiao, Luo, Huafei, Zhu, Zhuangzhi, Wu, Yubo, Wang, Hao
Format: Article
Language:English
Subjects:
adhesive properties
Administration, Cutaneous
Androgens - administration & dosage
Androgens - pharmacokinetics
Animals
Female
permeability
pharmacokinetics
Polystyrenes - chemistry
pressure-sensitive adhesive
Rats
Rats, Sprague-Dawley
skin
Skin - metabolism
Skin Absorption
stability
styrene–isoprene–styrene block copolymer
Terpenes - chemistry
testosterone
Testosterone - administration & dosage
Testosterone - pharmacokinetics
transdermal drug delivery
Transdermal Patch
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The purpose of the present study was to design and evaluate a monolithic drug-in-adhesive patch with a novel pressure-sensitive adhesive (PSA) matrix based on styrene–isoprene-styrene (SIS) block copolymer. Testosterone was selected as the model drug. The orthogonal array design for ternary mixtures was employed to optimize the amounts of SIS, C-5 hydrocarbon resin, and liquid paraffin. The drug release percentage, water vapor permeability, adhesive properties were chosen as response variables. The patch formulation was optimized by investigating the effects of the drug loading capacity, the type, and amount of permeation enhancer on the adhesive properties and skin permeation. The compositions of the optimal matrix were: 120 g of SIS copolymer, 120 g of C-5 hydrocarbon resin, 60 g of liquid paraffin. An optimized formulation with maximum skin permeation and acceptable adhesive properties was developed incorporating 2% testosterone and 6% isopropyl myristate. No significant differences for in vitro release, skin permeation, and in vivo absorption were observed between the optimal formulation and Testopatch®. The stability evaluation showed that the patches were stable at 25°C/60% relative humidity for 6 months. The result indicated that SIS copolymer was a suitable and compatible polymer for the development of PSA. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:2221–2234, 2013
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.23576