In vitro and in vivo evaluation of mPEG-PLA modified liposomes loaded glycyrrhetinic acid.
In order to prolong the in vivo residence of glycyrrhetinic acid, a liposomes with surface modified by methoxy poly(ethyleneglycol) (mPEG)-PLA was prepared for the first time. The liposomes (C-LP) and long-circulating liposomes (LC-LP) were prepared by film-dispersion method using soybean phospholipid/cholesterol mixture (1:0.5 mol/mol), containing 5% (w/w) sodium deoxycholate, and 2% (w/w) mPEG-PLA (only for LC-LP). The diameter of LC-LP was 243.3+/-17.1 nm. The pharmacokinetics behaviors of the conventional injection and liposomes (C-LP and LC-LP) were compared after a single intravenous injection to rats. Pharmacokinetic parameters were calculated based on a two-compartment open model analysis. LC-CP had a 1.7-fold longer residence time (MRT), a 2.75-fold larger AUC and a 0.4-fold lower clearance compared with conventional injection, respectively. These results combined suggested that the LC-CP had a well-improved residence in rats.
Lu
Yang
Y
Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, PR China.
Li
Juan
J
Wang
Guangji
G
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002784:Cholesterol / Q000737:chemistry; D003692:Delayed-Action Preparations; D003840:Deoxycholic Acid / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D006034:Glycyrrhetinic Acid / Q000008:administration & dosage / Q000493:pharmacokinetics*; D007275:Injections, Intravenous; D008081:Liposomes; D008297:Male; D010743:Phospholipids / Q000737:chemistry; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013025:Glycine max / Q000737:chemistry
D000893:Anti-Inflammatory Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008081:Liposomes; D010743:Phospholipids; D011091:Polyesters; C492425:methoxy poly(ethylene glycol)-poly(lactide); D003840:Deoxycholic Acid; D011092:Polyethylene Glycols; D002784:Cholesterol; D006034:Glycyrrhetinic Acid