Effect of the composition of lecithin/n-propanol/isopropyl myristate/water microemulsions on barrier properties of mice skin for transdermal permeation of tetracaine hydrochloride: in vitro.
Effect of composition of lecithin water-in-oil and oil-in-water microemulsion on in vitro transdermal permeation of tetracaine hydrochloride was studied on mice model. The results were compared with an aqueous solution of tetracaine hydrochloride (2.7 mg/ml). In vitro skin flux and permeability coefficients were obtained using the Franz diffusion cell. Differential scanning calorimetry (DSC), transmission electron microscopy (TEM) and confocal laser scanning microscopy (CLSM) were used to study the mechanism of action of the microemulsion. Micrographs of TEM and CLSM studies were analyzed by using Image Pro Plus image software. Skin flux of tetracaine hydrochloride was found to be dependent on the composition of lecithin/n-propanol/isopropyl myristate/water microemulsions. At lower Km ratio (i.e. 0.5:1 and 0.8:1) of microemulsion, the rate of permeation of tetracaine hydrochloride was higher when compared to the microemulsion of higher Km ratio (1:1 and 1.5:1). Image analysis of TEM micrograph, 6h after application of lecithin microemulsion, showed 3.5+/-0.75-fold (p<0.001) increase in the intercellular space in the epidermis and 3.8+/-0.4-fold (p<0.001) enhancement in upper dermis. CLMS results show that sweat gland and hair follicles also provided path for permeation of the drug through the skin.
Changez
Mohammad
M
Centre for Biomedical Engineering, Indian Institute of Technology, New Delhi 110016, India. ach2k@yahoo.com
Varshney
Manoj
M
Chander
Jadish
J
Dinda
Amit Kumar
AK
D000433:1-Propanol / Q000737:chemistry*; D000279:Administration, Cutaneous; D000779:Anesthetics, Local / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D002152:Calorimetry, Differential Scanning; D002463:Cell Membrane Permeability / Q000187:drug effects*; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D004655:Emulsions / Q000008:administration & dosage / Q000737:chemistry*; D008297:Male; D051379:Mice; D008832:Microchemistry; D018613:Microscopy, Confocal; D046529:Microscopy, Electron, Transmission; D015394:Molecular Structure; D009226:Myristates / Q000737:chemistry*; D010713:Phosphatidylcholines / Q000737:chemistry*; D012867:Skin / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D013748:Tetracaine / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D014867:Water / Q000737:chemistry
D000779:Anesthetics, Local; D004337:Drug Carriers; D004655:Emulsions; D009226:Myristates; D010713:Phosphatidylcholines; D014867:Water; D013748:Tetracaine; C008205:isopropyl myristate; D000433:1-Propanol