The Physicochemical Characterization and In Vitro In Vivo Evaluation of Natural Surfactants-based Emulsions as Vehicles for Diclofenac Diethylamine

• Published in: Drug development and industrial pharmacy Vol. 33; no. 3; pp. 221 - 234
• Main Authors: Vu ini -Milankovi, Nada, Savi, Sne ana, Vuleta, Gordana, Vu ini, Slavica
• Format: Journal Article
• Language: English
• Published: Colchester Informa UK Ltd 01-03-2007; Taylor & Francis
• Subjects: Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics; Biological and medical sciences; Cetearyl alcohol & cetearyl glycoside; Chemistry, Pharmaceutical - methods; Diclofenac - administration & dosage; Diclofenac - pharmacokinetics; Diclophenac diethylamine release; Diethylamines - administration & dosage; Diethylamines - pharmacokinetics; Droplet size analysis; Emulsions; Fatty Alcohols - chemistry; General pharmacology; Glucosides - chemistry; Humans; Liquid Crystals; Liquid-crystalline gel network; Medical sciences; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Rheology; Skin Absorption; Sorbitan stearate & sucrose cocoate; Stearates - chemistry; Surface-Active Agents - chemistry; Prostaglandin-endoperoxide synthase; Sorbitan stearate & sucrose cocoate; Vehicle(excipient); Diclophenac diethylamine release; Droplet size analysis; Emulsifier; Surfactant; Diclofenac; Cetearyl alcohol & cetearyl glycoside; Colloidal gel; Formulation; Pharmaceutical technology; Enzyme; Rheology; Enzyme inhibitor; Liquid-crystalline gel network; Amphiphilic compound; In vitro; Non steroidal antiinflammatory agent; In vivo; Arylacetic acid derivatives; Analgesic; Sorbitan stearate; Dosage form; Antipyretic; Oxidoreductases; Physicochemical properties
• ISSN: 0363-9045; 1520-5762
• DOI: 10.1080/03639040601150179

ABSTRACTTwo sugar-based emulsifiers, cetearyl alcohol & cetearyl glycoside and sorbitan stearate & sucrose cocoate, known as potential promoters of lamellar liquid crystals gel phases, were investigated in order to formulate an optimal vehicle for amphiphilic drug-diclofenac diethylamine (DDA).
Physico-chemical characterization and study of vehicle's physical stability were performed. Then, the in vitro DDA liberation profile, dependent on the mode of drug incorporation to the system, and the in vivo, short-term effects of chosen samples on skin parameters were examined.
Droplets size distribution and rheological behavior indicated satisfying physical stability of both types of vehicles. Unexpectedly, the manner of DDA incorporation to the system had no significant influence on DDA release. In vivo study pointed to emulsion's favorable potential for skin hydration and barrier improvement, particularly in cetearyl glycoside-based vehicle.