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Year : 2019  |  Volume : 14  |  Issue : 4  |  Page : 293-307

Preparation and optimization of polymeric micelles as an oral drug delivery system for deferoxamine mesylate: in vitro and ex vivo studies

1 School of Pharmacy; Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, I.R, Iran
2 School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, I.R, Iran

Correspondence Address:
Behzad Sharif Makhmal Zadeh
School of Pharmacy; Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, I.R
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Source of Support: None, Conflict of Interest: None

DOI: 10.4103/1735-5362.263554

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Deferoxamine mesylate (DFO) is administered as a slow subcutaneous or intravenous infusion due to its poor oral bioavailability and lack of dose proportionality. The aim of the present study was to prepare and optimize polymeric micelles containing DFO, as an oral drug delivery system for increasing permeability and oral bioavailability. Based on a full factorial design with three variables in two levels, eight polymeric micelle formulations were made using film hydration method. Two polymers including 0.1% of carbomer 934 and Poloxamer® P 407 and two blends of surfactant + co-surfactant including 1 and 2 fold of critical micelle concentration of Labrafil® + Labrasol® and Tween 80 + Span 20 were used to prepare polymeric micelles. The effect of variables on particle size (PS), entrapment efficiency (EE), drug release, thermal behavior, in vitro iron bonding and ex vivo rat intestinal permeability were evaluated. The PS of polymeric micelles was less than 83 nm that showed 80% EE with continuous drug release pattern. The change in type of polymer from carbomer to Ploxamer® significantly increased drug release. All polymeric micelles increased the iron-bonding ability of DFO compared to control. This could be due to surfactants that can play an important role in this ability. Polymeric micelles increased drug permeability through intestine more than 2.5 folds compared to control mainly affected by polymer type. Optimized polymeric micelle consists of Tween 80 and Span 20 with 1.35 folds of critical micelle concentration and Poloxamer® demonstrated 97.32% iron bonding and a 3-fold increase in permeation through the rat intestine compared with control.

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