title: Formulation parameters influencing the physicochemical characteristics of rosiglitazone-loaded cationic lipid emulsion.
abstract: To enhance the solubility of rosiglitazone, rosiglitazone-loaded cationic lipid emulsion was formulated using cationic lipid DOTAP, DOPE, castor oil, tween 20, and tween 80. The formulation parameters in terms of droplet size were optimized focused on the effect of the cationic lipid emulsion composition ratio on drug encapsulating efficiency, in vitro drug release, and cellular uptake of the rosiglitazone-loaded emulsion. Droplet sizes of a blank cationic emulsion and a rosiglitazone-loaded cationic emulsion ranged between 195-230 nm and 210-290 nm, respectively. The encapsulation efficiency of the rosiglitazone-loaded emulsion was more than 90%. The rosiglitazone-loaded cationic emulsion improved in vitro drug release over the drug alone and showed a much higher cellular uptake than rosiglitazone alone. Moreover, drug loading in cationic emulsions increased cellular uptake of rosiglitazone in insulin-resistant HepG2 cells more than the normal HepG2 cells. Taken together, these results indicate that cationic lipid emulsions could be a potential delivery system for rosiglitazone and could enhance its cellular uptake efficiency into target cells.
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea.
authors.forename: Enkhzaya
authors.initials: E
authors.lastname: Davaa
authors.forename: Jeong-Sook
authors.initials: JS
authors.lastname: Park
mesh_terms: D001692:Biological Transport; D006528:Carcinoma, Hepatocellular / Q000378:metabolism; D002368:Castor Oil / Q000737:chemistry; D002412:Cations; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D004355:Drug Stability; D004655:Emulsions; D005229:Fatty Acids, Monounsaturated / Q000737:chemistry; D056945:Hep G2 Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000378:metabolism; D007333:Insulin Resistance; D008055:Lipids / Q000737:chemistry*; D008113:Liver Neoplasms / Q000378:metabolism; D053758:Nanoparticles; D010316:Particle Size; D010714:Phosphatidylethanolamines / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D000644:Quaternary Ammonium Compounds / Q000737:chemistry; D000077154:Rosiglitazone; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods; D045162:Thiazolidinediones / Q000737:chemistry* / Q000378:metabolism
chemical_list: D002412:Cations; D004337:Drug Carriers; D004655:Emulsions; D005229:Fatty Acids, Monounsaturated; D007004:Hypoglycemic Agents; D008055:Lipids; D010714:Phosphatidylethanolamines; D011136:Polysorbates; D000644:Quaternary Ammonium Compounds; D013501:Surface-Active Agents; D045162:Thiazolidinediones; D000077154:Rosiglitazone; C020888:1,2-dielaidoylphosphatidylethanolamine; D002368:Castor Oil; C070046:1,2-dioleoyloxy-3-(trimethylammonium)propane