Formulation and characterization of a captopril ethyl ester drug-in-adhesive-type patch for percutaneous absorption.
BACKGROUND
The ethyl ester of captopril has been shown to exhibit enhanced permeation across human skin compared to the parent drug. A drug-in-adhesive patch formulation of a captopril ethyl ester was therefore developed for optimum drug release.


METHODS
A wide range of transdermal patches were prepared using two commercially available bioadhesive polymers. Investigational screening was conducted on the patches using microscopy, texture profile analysis, and infrared spectroscopy. Drug release profiles of suitable patches were obtained using both polydimethylsiloxane (Silastic) and porcine skin in vitro.


RESULTS
Diffusion results across Silastic showed a gradual plateau in flux with increased drug loading that may be attributable to intramolecular interactions while flux across porcine skin was seen to increase with increasing patch thickness and attained a therapeutic level.


CONCLUSIONS
This study demonstrated that adhesion and drug loading are significant factors in optimizing a topical patch formulation for the delivery of a captopril prodrug.
Gullick
Darren R
DR
School of Pharmacy and Biomedical Sciences, University of Portsmouth, Portsmouth, UK.
Pugh
W John
WJ
Ingram
Matthew J
MJ
Cox
Paul A
PA
Moss
Gary P
GP
D000268:Adhesiveness; D000269:Adhesives; D000279:Administration, Cutaneous; D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000032:analysis / Q000737:chemistry* / Q000493:pharmacokinetics; D002216:Captopril / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000032:analysis / Q000737:chemistry / Q000493:pharmacokinetics; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D004058:Diffusion; D004129:Dimethylpolysiloxanes / Q000737:chemistry; D016503:Drug Delivery Systems; D004952:Esters; D010539:Permeability; D011108:Polymers; D011355:Prodrugs / Q000008:administration & dosage* / Q000032:analysis / Q000737:chemistry* / Q000493:pharmacokinetics; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013055:Spectrophotometry, Infrared; D034421:Sus scrofa; D013997:Time Factors
D000269:Adhesives; D000959:Antihypertensive Agents; D004129:Dimethylpolysiloxanes; D004952:Esters; D011108:Polymers; D011355:Prodrugs; C553091:captopril ethyl ester; D002216:Captopril