title: A drug-in-adhesive matrix based on thermoplastic elastomer: evaluation of percutaneous absorption, adhesion, and skin irritation.
abstract: A novel drug-in-adhesive matrix was designed and prepared. A thermoplastic elastomer, styrene-isoprene-styrene (SIS) block copolymer, in combination with tackifying resin and plasticizer, was employed to compose the matrix. Capsaicin was selected as the model drug. The drug percutaneous absorption, adhesion properties, and skin irritation were investigated. The results suggested that the diffusion through SIS matrix was the rate-limiting step of capsaicin percutaneous absorption. [SI] content in SIS and SIS proportions put important effects on drug penetration and adhesion properties. The chemical enhancers had strong interactions with the matrix and gave small effect on enhancement of drug skin permeation. The in vivo absorption of samples showed low drug plasma peaks and a steady and constant plasma level for a long period. These results suggested that the possible side effects of drug were attenuated, and the pharmacological effects were enhanced with an extended therapeutic period after application of SIS matrix. The significant differences in pharmacokinetic parameters produced by different formulations demonstrated the influences of SIS copolymer on drug penetrability. Furthermore, the result of skin toxicity test showed that no skin irritation occurred in guinea pig skin after transdermal administration of formulations.
authors.affiliation: School of Pharmacy, East China University of Science and Technology, Shanghai, 200237, China.
authors.forename: ChengXiao
authors.initials: C
authors.lastname: Wang
authors.forename: Ran
authors.initials: R
authors.lastname: Liu
authors.forename: XiuZhen
authors.initials: X
authors.lastname: Tang
authors.forename: Wei
authors.initials: W
authors.lastname: Han
mesh_terms: D000269:Adhesives / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D002070:Butadienes / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D002211:Capsaicin / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004058:Diffusion; D020724:Elastomers / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D045782:Hemiterpenes / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D007509:Irritants / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D008297:Male; D010420:Pentanes / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D010539:Permeability; D010968:Plasticizers / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D011108:Polymers / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000187:drug effects* / Q000378:metabolism; D012869:Skin Absorption; D020058:Styrene / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity
chemical_list: D000269:Adhesives; D002070:Butadienes; D020724:Elastomers; D045782:Hemiterpenes; D007509:Irritants; D010420:Pentanes; D010968:Plasticizers; D011108:Polymers; C005059:isoprene; D020058:Styrene; D002211:Capsaicin