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  • Title: Etoposide-loaded biodegradable amphiphilic methoxy (poly ethylene glycol) and poly (epsilon caprolactone) copolymeric micelles as drug delivery vehicle for cancer therapy.
    Author: Mohanty AK, Dilnawaz F, Mohanty C, Sahoo SK.
    Journal: Drug Deliv; 2010 Jul; 17(5):330-42. PubMed ID: 20370380.
    Abstract:
    Amphiphilic diblock copolymers composed of methoxy poly ethylene glycol (MePEG) and poly epsilon caprolactone (PCL) were synthesized for the formation of micelles by ring opening mechanism using stannous octoate as a catalyst. The effects of the molecular weight of MePEG and the copolymer ratio on the properties of micelles were investigated by Nuclear Magnetic Resonance ((1)H-NMR), Fourier Transform Infrared Spectroscopy (FT-IR), and Gel Permeation Chromatography (GPC). The diblock copolymers were self-assembled to form micelles and their hydrophobic core was used for the encapsulation of the anti-cancer drug (etoposide) in aqueous solution. The sizes of micelles were less than 250 nm with a narrow size distribution with monodispersed unimodal pattern. Differential Scanning Calorimetric (DSC) thermogram was done for etoposide-loaded micelles to understand the crystalline nature of the drug after entrapment. A drug loading capacity up to 60% (w/w) with an entrapment efficiency of 68% was achieved as determined by reverse phase high performance liquid chromatography (RP-HPLC). In vitro release kinetics showed a biphasic release pattern of etoposide for 2 weeks. The cytotoxic efficacy of the etoposide-loaded micelles demonstrated greater anti-proliferative activity (IC(50) = 1.1 microg/ml) as compared to native drug (IC(50) = 6.3 microg/ml) in pancreatic cancer cell line MIA-PaCa-2. Thus, etoposide-loaded MePEG/PCL block copolymeric micelles can be used as an efficient drug delivery vehicle for pancreatic cancer therapy.
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