Curcumin-loaded PLGA-PEG-PLGA triblock copolymeric micelles: Preparation, pharmacokinetics and distribution in vivo.
The aim of this study was to assess the potential of new copolymeric micelles to modify the pharmacokenetics and tissue distribution of Curcumin (CUR), a hydrophobic drug. In the present study, a poly (d,l-lactide-co-glycolide)-b-poly(ethylene glycol)-b-poly(d,l-lactide-co-glycolide) (PLGA-PEG-PLGA) copolymer was synthesized and characterized by (1)H NMR, gel permeation chromatography and FTIR analysis. The CUR-loaded PLGA-PEG-PLGA micelles were prepared by dialysis method and the physicochemical parameters of the micelles such as zeta potential, size distribution and drug encapsulation were characterized. The pharmacokinetics and biodistribution of CUR-loaded micelles in vivo were evaluated. The results showed that the zeta potential of CUR-loaded micelles was about -0.71mV and the average size was 26.29nm. CUR was encapsulated into PLGA-PEG-PLGA micelles with loading capacity of 6.4±0.02% and entrapment efficiency of 70±0.34%. The plasma AUC((0-)(∞)), t(1/2α), t(1/2β) and MRT of CUR micelles were increased by 1.31, 2.48, 4.54 and 2.67 fold compared to the CUR solution, respectively. The biodistribution study in mice showed that the micelles decreased drug uptake by liver and spleen and enhanced drug distribution in lung and brain. These results suggested that PLGA-PEG-PLGA micelles would be a potential carrier for CUR.
Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, China.
Zhimei
Z
Song
Runliang
R
Feng
Min
M
Sun
Chenyu
C
Guo
Yan
Y
Gao
Lingbing
L
Li
Guangxi
G
Zhai
D000818:Animals; D003474:Curcumin / Q000493:pharmacokinetics*; D004337:Drug Carriers / Q000737:chemistry*; D057927:Hydrophobic and Hydrophilic Interactions; D007668:Kidney / Q000737:chemistry; D019344:Lactic Acid / Q000138:chemical synthesis / Q000737:chemistry*; D008099:Liver / Q000737:chemistry; D051379:Mice; D008823:Micelles; D015394:Molecular Structure; D010316:Particle Size; D011092:Polyethylene Glycols / Q000138:chemical synthesis / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000138:chemical synthesis / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
D004337:Drug Carriers; D008823:Micelles; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D003474:Curcumin