ABSTRACT
This study was designed to investigate the influence of volatile oil pretreated skin on in vitro permeation from films containing ionized and dodecylamine ion-paired diclofenac sodium (DS). The involvement of skin cholesterol was investigated to determine its possible role in enhancing the permeation of ion-paired DS. Cardamom oil produced the maximum (10 x) in vitro permeation enhancement for ion-paired DS. The carrageenan induced rat paw oedema reduction (up to 12 hr) by cardamom oil was comparable to that of diclofenac injection (s c). Leaching of cholesterol from excised skin in addition to increased partition coefficient following volatile oil skin pretreatment appears to be responsible for in vitro permeation enhancement of DS. Whereas, a mild barrier perturbation effect due to altered cholesterol levels following pretreatment with volatile oils appears to increase the permeation of ion-paired DS across viable skin, thereby producing significant reduction of carrageenan induced paw oedema.
Subject(s)
Administration, Cutaneous , Animals , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Biomarkers/analysis , Cholesterol/metabolism , Diclofenac/pharmacokinetics , Edema/chemically induced , Epidermis/metabolism , Male , Oils, Volatile/pharmacology , Permeability , Rats , Rats, Inbred Strains , Rats, Wistar , Skin/metabolism , Skin Absorption/drug effects , Solubility , Pharmaceutical Vehicles/pharmacokineticsABSTRACT
The management of diabetic hypertension requires meticulous selection of agents in the antihypertension armamentorium. There may be several associated factors to be considered while treating a hypertensive diabetic. These include hyperglycemia, dyslipidemia, proteinuria, left ventricular hypertrophy and heart failure to name a few. Losartan is the first of a new class of agents in the list of antihypertensive drugs. By its selective angiotension II receptor (subtype AT1) blocking action it is postulated to bring about a more complete inhibition of the renin-angiotensin system. Thus, it might produce all the benefits of angiotensin converting enzyme (ACE) inhibitor therapy with the freedom from cough so commonly seen with the use of ACE inhibitors. This review attempts to analyze the possible benefits of losartan therapy in diabetes.