Improved therapeutic effect of folate-decorated PLGA–PEG nanoparticles for endometrial carcinoma

• Published in: Bioorganic & medicinal chemistry 2011-07, Vol.19 (13), p.4057-4066
• Main Authors: Liang, Changyan, Yang, Yuebo, Ling, You, Huang, Yueshan, Li, Tian, Li, Xiaomao
• Format: Article
• Language: English
• Subjects: Animals; Antineoplastic agents; Antineoplastic Agents - administration & dosage; Antineoplastic Agents - chemistry; Antineoplastic Agents - toxicity; Biological and medical sciences; Cell Line, Tumor; Drug Carriers - chemistry; Drug targeting; Endometrial carcinoma; Endometrial Neoplasms - drug therapy; Female; Folate receptor; Folic Acid - chemistry; General aspects; Humans; Lactic Acid - chemistry; Medical sciences; Mice; Mice, Nude; Nanoparticles - chemistry; Nanoparticles - toxicity; Paclitaxel; Paclitaxel - administration & dosage; Paclitaxel - chemistry; Paclitaxel - toxicity; Pharmacology. Drug treatments; PLGA nanoparticles; Polyglycolic Acid - chemistry; Transplantation, Heterologous
• ISSN: 0968-0896; 1464-3391
• DOI: 10.1016/j.bmc.2011.05.016

Folate (FOL) mediated poly-lactide-co-glycolide–polyethylene glycol nanoparticles (FOL–PEG–PLGA NPs) bearing paclitaxel (PTX) were prepared for the effective delivery of drug to endometrial carcinoma. The FOL-targeted PTX NPs showed a greater cytotoxicity against HEC-1A cancer cells in vitro and in vivo. These results suggest that the novel FOL–PEG–PLGA NPs could be a potential delivery system with excellent therapeutic efficacy for targeting the drugs to cancer cells. Folate (FOL) mediated poly–lactide-co-glycolide–polyethylene glycol nanoparticles (FOL–PEG–PLGA NPs) bearing paclitaxel (PTX) were prepared for the effective delivery of drug to endometrial carcinoma. The average size, zeta potential and encapsulation efficiency of FOL-targeted NPs were found to be around 220 nm, −30.43 mV and 95.6%. Cellular uptake was observed. The accumulation of FOL-targeted NPs depends on dual effects of passive and active targeting. The FOL-targeted PTX NPs showed a greater cytotoxicity against HEC-1A cancer cells in vitro and in vivo, which might be induced by apoptosis. H&E staining did not showed apparent tissue damage to liver and kidney of the mice after injecting NPs intravenously. These results suggest that the novel FOL–PEG–PLGA NPs could be a potential delivery system with excellent therapeutic efficacy for targeting the drugs to cancer cells.