title: Etoposide-loaded biodegradable amphiphilic methoxy (poly ethylene glycol) and poly (epsilon caprolactone) copolymeric micelles as drug delivery vehicle for cancer therapy.
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.
authors.affiliation: Institute of Life Sciences, Nalco Square, Chandrasekharpur, Bhubaneswar, Orissa, India.
authors.forename: Anjan K
authors.initials: AK
authors.lastname: Mohanty
authors.forename: Fahima
authors.initials: F
authors.lastname: Dilnawaz
authors.forename: Chandana
authors.initials: C
authors.lastname: Mohanty
authors.forename: Sanjeeb K
authors.initials: SK
authors.lastname: Sahoo
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000494:pharmacology; D002152:Calorimetry, Differential Scanning; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid; D003460:Crystallization; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D005047:Etoposide / Q000008:administration & dosage* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D008823:Micelles; D008970:Molecular Weight; D010190:Pancreatic Neoplasms / Q000188:drug therapy / Q000473:pathology; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008823:Micelles; D011091:Polyesters; C439611:methoxy poly(ethylene glycol-co-epsilon-caprolactone); D011092:Polyethylene Glycols; D005047:Etoposide