title: Folated synperonic-cholesteryl hemisuccinate polymeric micelles for the targeted delivery of docetaxel in melanoma.
abstract: The objective of this study was the synthesis of folic acid- (FA-) targeted polymeric micelles of Synperonic PE/F 127-cholesteryl hemisuccinate (PF127-Chol) for specific delivery of docetaxel (DTX). Targeted or nontargeted micelles loaded with DTX were prepared via dialysis method. The effects of processing variables on the physicochemical properties of targeted micelles were evaluated using a full factorial design. After the optimization of the polymer/drug ratio, the organic solvent type used for the preparation of the micelles, and the temperature of dialyzing medium, the in vitro cytotoxicity and cellular uptake of the optimized micelles were studied on B16F10 melanoma cells by flow cytometry and fluorescent microscopy. The anticancer efficacy of DTX-loaded FA-PF127-Chol was evaluated in mice bearing melanoma tumor. Optimized targeted micelles had the particle size of 171.3 nm, zeta potential of -7.8 mV, PDI of 0.325, and a high encapsulation efficiency that released the drug within 144 h. The MTT assay indicated that targeted micelles carrying DTX were significantly more cytotoxic, had higher cellular uptake, and reduced the tumor volume significantly more than the nontargeted micelles and the free drug. FA-PF127-Chol could be, therefore, a promising biomaterial for tumors overexpressing folate receptors.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan 81746 73461, Iran.
authors.forename: Jaleh
authors.initials: J
authors.lastname: Varshosaz
authors.affiliation: Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan 81746 73461, Iran.
authors.forename: Somayeh
authors.initials: S
authors.lastname: Taymouri
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Isfahan University of Medical Sciences, Isfahan 81746 73461, Iran.
authors.forename: Farshid
authors.initials: F
authors.lastname: Hassanzadeh
authors.affiliation: Applied Physiology Research Center, Isfahan University of Medical Sciences, Isfahan 81746 73461, Iran.
authors.forename: Shaghayegh Haghjooy
authors.initials: SH
authors.lastname: Javanmard
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Isfahan University of Medical Sciences, Isfahan 81746 73461, Iran.
authors.forename: Mahboobeh
authors.initials: M
authors.lastname: Rostami
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D045744:Cell Line, Tumor; D002788:Cholesterol Esters / Q000737:chemistry*; D000077143:Docetaxel; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods; D005492:Folic Acid / Q000737:chemistry*; D056945:Hep G2 Cells; D006801:Humans; D008546:Melanoma, Experimental / Q000178:diet therapy*; D051379:Mice; D008823:Micelles; D010316:Particle Size; D011108:Polymers / Q000737:chemistry*; D043823:Taxoids / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D002788:Cholesterol Esters; D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; D043823:Taxoids; D000077143:Docetaxel; D005492:Folic Acid; C013440:cholesteryl succinate
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