title: Preparation and evaluation of liposome-encapsulated codrug LMX.
abstract: A novel codrug (LMX) consisting of Lamivudine and Ursolic acid has been shown to possess the dual action of anti-hepatitis B virus activity and hepatoprotective effects against acute liver injury in vivo. Because of the limited water solubility of LMX, our aims were to design and optimize a liposomal formulation that could facilitate its in vivo administration, and to estimate the potential of LMX-loaded liposomes as oral or intravenous delivery system. In this work, LMX-loaded liposomes were prepared by the thin film hydration method coupled with sonication. LMX-loaded liposomes showed spherical morphology under transmission electron microscope (TEM) analysis. The mean particle size of liposomes was about 210 nm, and the drug entrapment efficiency was more than 90%. Stability data indicated that lyophilized liposomes were stable for at least 6 months at 4 °C. In vitro drug release profile of LMX-loaded liposomes showed a sustained release profile of LMX and an initial mild burst was observed. The relative bioavailability of LMX-loaded liposomes was 1074.8% compared with LMX suspension after oral administration, and 135.2% relative to 50% alcohol solution after intravenous (i.v.) administration. These results indicated that LMX-loaded liposomes were valued to develop as a practical preparation for oral or i.v. administration.
authors.affiliation: School of Chemistry and Chemical Engineering, Southeast University, Nanjing 210096, PR China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Zhong
authors.forename: Jing
authors.initials: J
authors.lastname: Wang
authors.forename: Yao
authors.initials: Y
authors.lastname: Wang
authors.forename: Bin
authors.initials: B
authors.lastname: Wu
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001682:Biological Availability; D004338:Drug Combinations; D004339:Drug Compounding; D004355:Drug Stability; D007408:Intestinal Absorption / Q000187:drug effects; D019259:Lamivudine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008081:Liposomes; D010316:Particle Size; D020011:Protective Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D014315:Triterpenes / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000097245:Ursolic Acid
chemical_list: D000998:Antiviral Agents; D004338:Drug Combinations; D019259:Lamivudine; D008081:Liposomes; D020011:Protective Agents; D014315:Triterpenes; D000097245:Ursolic Acid