The effect of Ibuprofen–DEAE-Dextran nanoconjugates (surfactant solubilization) on the thermal properties and in vitro drug release kinetics of ibuprofen

Adeola T. Kola-Mustapha1 and Amos O. Abioye2.

Faculty of Pharmaceutical Sciences, University of Ilorin, Ilorin, Nigeria1; Leicester School of Pharmacy, De Montfort University, Leicester, UK2. *Corresponding author: Adeola T. Kola-Mustapha,Email: atkmusty@yahoo.com, +2348033475485

 

ABSTRACT

Background: It has become increasingly desirable to overcome the low aqueous solubility of drug candidates and develop more novel and innovative formulation approaches to increase the dissolution rate of the poorly soluble drugs; due to significant difficulties presented by Active Pharmaceutical Ingredients (APIs) in drug product design and development. This work focused on the effect of stable amorphous ibuprofen-DEAE-Dextran nanoconjugates formulated in earlier studies via surfactant solubilization technique (organic solvent free process) on its physicochemical and drug release characteristics.

Methods: The nanoparticles were characterised via the Fourier Transform Infra-red (FTIR), Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA), drug release profile and kinetics.

Results: The FTIR spectroscopic analysis revealed electrostatic, hydrophobic and hydrogen bonding interaction between solubilized ibuprofen and the cationic polymer (DEAE-Dextran) to form a new product (an amide). The DSC of the nanoconjugates exhibited broad and diffuse melting peaks which confirmed that the Ibuprofen-DEAE-Dextran nanoconjugates exist in amorphous state. Isothermal stability was suggested due to the disappearance of thermal decomposition peak of ibuprofen at 237.51 °C also disappeared in all the nanoconjugates. The TGA thermograms of the nanoconjugates exhibited two steps of weight loss profile due to the loss of free water and decomposition of the nanoconjugates.  Marked enhancement of drug release was achieved by the nanoconjugates. The major mechanism of drug release from the nanoconjugates was by anomalous diffusion.   Conclusions: This study therefore demonstrates the improved drug release profile of amorphous Ibuprofen-DEAE-Dextran nanoconjugates with potential application in the delivery of poorly soluble drug.

Key Words: Ibuprofen, surfactant solubilization, DEAE-Dextran, nanoconjugate and poorly soluble drug

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