Transdermal permeation of tetracaine hydrochloride by lecithin microemulsion: in vivo.
In vivo transdermal permeation of tetracaine hydrochloride encapsulated in lecithin water-in-oil and oil-in-water microemulsion was studied. The effect of the composition of the lecithin microemulsion on analgesic response of tetracaine hydrochloride was evaluated on Wistar rats by tail flick method. To find out the toxicity of lecithin/n-propanol/isopropyl myristate/water/tetracaine hydrochloride microemulsion histopathological and irritation response were measured in Swiss mice. Time course studies were also conducted for the biochemical response of microemulsion by measuring catalase, glutathione and lipid peroxidation levels of the treated mice skin. The analgesic response was found to be dependent on the drug concentration and composition of the systems. The histopathological, irritation and biochemical findings reveal that lecithin/n-propanol/isopropyl myristate/water/tetracaine hydrochloride microemulsion is a safe carrier for transdermal drug delivery systems. Confocal laser scanning microscopy observation indicated that sweat gland and hair follicle also provided the path for transdermal permeation of lecithin/n-propanol/isopropyl myristate/water microemulsion.
Centre for Biomedical Engineering, Indian Institute of Technology, Delhi, Hauz Khas, New Delhi 110016, India. ach2k@yahoo.com
Mohammad
M
Changez
Jagdish
J
Chander
Amit Kumar
AK
Dinda
D000433:1-Propanol / Q000737:chemistry; D000279:Administration, Cutaneous; D000779:Anesthetics, Local / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D000818:Animals; D002374:Catalase / Q000032:analysis; D004337:Drug Carriers / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D004655:Emulsions / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D015227:Lipid Peroxidation / Q000187:drug effects; D008297:Male; D008315:Malondialdehyde / Q000032:analysis; D051379:Mice; D018613:Microscopy, Confocal; D009226:Myristates / Q000737:chemistry; D010146:Pain / Q000188:drug therapy / Q000473:pathology; D010539:Permeability / Q000187:drug effects; D010713:Phosphatidylcholines / Q000737:chemistry; D011506:Proteins / Q000032:analysis; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000737:chemistry / Q000187:drug effects* / Q000201:enzymology / Q000378:metabolism; D023422:Skin Irritancy Tests; D012997:Solvents / Q000008:administration & dosage / Q000493:pharmacokinetics; D013347:Subcellular Fractions / Q000737:chemistry; D013748:Tetracaine / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D014867:Water / Q000737:chemistry
D000779:Anesthetics, Local; D004337:Drug Carriers; D004655:Emulsions; D009226:Myristates; D010713:Phosphatidylcholines; D011506:Proteins; D012997:Solvents; D014867:Water; D013748:Tetracaine; C008205:isopropyl myristate; D008315:Malondialdehyde; D000433:1-Propanol; D002374:Catalase