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Preparation and in vitro evaluation of actively targetable nanoparticles for SN-38 delivery against HT29 cell lines

Pedram Ebrahimnejadac, Rassoul DinarvandadCorresponding Author Informationemail address, Abolghasem Sajadib, Mahmoud Reza Jaafaric, Ali Reza Nomaniae, Ebrahim Azizide, Mazda Rad-Malekshahia, Fatemeh Atyabiad

Received 20 February 2009; received in revised form 26 September 2009; accepted 2 October 2009. published online 16 October 2009.
Accepted Manuscript

Abstract 

SN-38 (7-ethyl-10-hydroxycamptothecin) is the active metabolite of irinotecan, which is 100-1000 folds more cytotoxic than irinotecan. Nonetheless extreme hydrophobicity of SN-38 has prevented its clinical use. One way of improving the solubility and stability of SN-38 is to formulate the drug into nanoparticles. Folic acid has been widely employed as a targeting moiety for various anti-cancer drugs. For folate-receptor-targeted anti-cancer therapy, SN-38 nanoparticles were produced employing poly-lactide-co-glycolide–polyethylene glycol–folate (PLGA-PEG-FOL) conjugate by emulsification/solvent evaporation method. The FOL-conjugated di-block copolymer was synthesized by coupling the PLGA-PEG-NH2 di-block copolymer with an activated folic acid. The conjugates were used for the formation of SN-38 NPs with an average size of 200 nm in diameter. The SN-38 targeted nanoparticles showed a greater cytotoxicity against HT-29 cancer cells than SN-38 non-targeted nanoparticles. These results suggested that folate-targeted nanoparticles could be a potentially useful delivery system for SN-38 as an anticancer agent.

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a Novel Drug Delivery Systems Lab, Dept of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, PO Box 14155-6451, Iran

b Pharmacological Research Centre of Medicinal Plants, Faculty of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran

c Biotechnology Research Centre, Faculty of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran

d Medical Nanotechnology Research Centre, Tehran University of Medical Sciences, Tehran, Iran

e Pharmacology Research Lab., Dept of Toxicology-Pharmacology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

Corresponding Author InformationCorresponding author. Rassoul Dinarvand, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, PO Box 14155-6451, Iran. Fax: +98 21 66959055.

PII: S1549-9634(09)00191-9

doi:10.1016/j.nano.2009.10.003

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