Preparation and evaluation of folate-modified cationic pluronic micelles for poorly soluble anticancer drug.
The aim of this study was to construct novel targeting polymeric micelles. Folate-Poly (ethylenimine)-Pluronic copolymers were synthesized. A paclitaxel (PTX)-loaded mixed micelles consisting of Folate-Poly (ethylenimine)-Pluronic and Pluronic L121 copolymers have been developed. The mixed micelles showed nano-sized spherical morphology. The solubilization capacity of the mixed micelles was higher than Folate-Poly (ethylenimine)-Pluronic micelles because L121 has high solubilization capacity. MTT colorimetric test revealed that PTX in Folate-Poly (ethylenimine)-Pluronic micelles demonstrated the maximum anticancer activity. Pluronic-poly (ethylenimine) micelles and folate-modified Pluronic-poly(ethylenimine) micelles showed a marked increase of cellular accumulation compared with Pluronic P123 micelles. The biodistribution and retention of intravenously (i.v.) administered micelles to rats were determined. Folate-Poly (ethylenimine)-Pluronic micelles demonstrated enhanced pulmonary retention in rats after injection when compared to Pluronic P123 micelles.
Institute of Biochemical and Biotechnological Drugs, School of Pharmaceutical Science, Shandong University, Jinan, Shandong Province, China.
Wei
W
Xu
Yanan
Y
Cui
Peixue
P
Ling
Ling-bing
LB
Li
D000818:Animals; D002412:Cations; D002626:Chemistry, Pharmaceutical; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005492:Folic Acid / Q000138:chemical synthesis* / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D007275:Injections, Intravenous; D008823:Micelles; D011060:Poloxalene / Q000138:chemical synthesis* / Q000494:pharmacology; D020442:Poloxamer / Q000138:chemical synthesis* / Q000494:pharmacology; D011094:Polyethyleneimine / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D012995:Solubility; D014018:Tissue Distribution / Q000187:drug effects / Q000502:physiology
D002412:Cations; D008823:Micelles; D020442:Poloxamer; C464484:pluronic block copolymer P123; D011094:Polyethyleneimine; D011060:Poloxalene; D005492:Folic Acid