Advanced formulation and pharmacological activity of hydrogel of the titrated extract of C. asiatica.
Titrated extract of Centella asiatica (TECA) contains three principal ingredients, asiaticoside (AS), asiatic acid (AA), and madecassic acid (MA). These components are known to be clinically effective on systemic scleroderma, abnormal scar formation, and keloids. However, one problem associated with administration of TECA is its low solubility in aqueous as well as oil medium. In this study, various nonionic surfactants and bile salts as anionic surfactant were tested and screened for solubilizing TECA with a view to developing topical hydrogel type of ointment which is stable physicochemically, and has better pharmacological effects. When TECA was incorporated into various nonionic surfactant systems, labrasol had the most potent capacity for solubilizing TECA. In cases of bile salt systems, Na-deoxycholate (Na-DOC) had foremost solubilizing capacity, even more than labrasol. In differential scanning calorimetric study, the peaks of AA, MA, AS and Na-DOC disappeared at the coprecipitate of 1% TECA and 1% Na-DOC, suggesting the optimum condition of Na-DOC for solubilizing TECA. When the physicochemical stability of hydrogel containing this mixture was assessed, it was stable at room temperature for at least one month. Pharmacologically it significantly decreased the size of wound area at the 9th day when applied to the wound area of rat dorsal skin. Taken together, solubility of TECA was dramatically improved by using nonionic and anionic surfactant systems, and Na-DOC was found to be the most effective solubilizer of TECA in formulating a TECA-containing hydrogel typed ointment. Moreover this gel was considered to be applicable to clinical use for wound healing effect.
Hong
Soon-Sun
SS
Department of Pharmaceutics, College of Pharmacy, Seoul National University, Seoul 151-742, Korea.
Kim
Jong-Ho
JH
Li
Hong
H
Shim
Chang-Koo
CK
D000818:Animals; D002152:Calorimetry, Differential Scanning; D028041:Centella / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D004339:Drug Compounding; D004355:Drug Stability; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate / Q000737:chemistry*; D008297:Male; D015394:Molecular Structure; D009824:Ointments; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000187:drug effects / Q000293:injuries; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*; D017186:Titrimetry; D014945:Wound Healing / Q000187:drug effects
D009824:Ointments; D010936:Plant Extracts; D013501:Surface-Active Agents; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate