title: Formulation and characterization of a captopril ethyl ester drug-in-adhesive-type patch for percutaneous absorption.
abstract: 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.
authors.affiliation: School of Pharmacy and Biomedical Sciences, University of Portsmouth, Portsmouth, UK.
authors.forename: Darren R
authors.initials: DR
authors.lastname: Gullick
authors.forename: W John
authors.initials: WJ
authors.lastname: Pugh
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Ingram
authors.forename: Paul A
authors.initials: PA
authors.lastname: Cox
authors.forename: Gary P
authors.initials: GP
authors.lastname: Moss
mesh_terms: 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
chemical_list: D000269:Adhesives; D000959:Antihypertensive Agents; D004129:Dimethylpolysiloxanes; D004952:Esters; D011108:Polymers; D011355:Prodrugs; C553091:captopril ethyl ester; D002216:Captopril