Formulation and physical characterization of Ibuprofen-DEAE-Dextran nanoconjugates via surfactant solubilization
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Date
2015
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Publisher
West African Journal of Pharmacy
Abstract
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 focuses on the formulation of novel amorphous ibuprofen-polymer nanoconjugates based on the polymer-drug complexation in order to improve its physical and dissolution characteristics without the use of toxic organic solvents. Ibuprofen-polymer nanoconjugates were prepared using surfactant solubilization technique. A remarkably high loading capacity was achieved ranging from 89.05 to 96.34%. The size of ibuprofen (2.87 µm) was reduced significantly in the presence of 2.0 x10-3 mM of Diethylaminoethyl Dextran (DEAE-Dextran) to 122.17 nm. 5.0 x 10-4 mM of chitosan also reduced the size of ibuprofen from 2872.12 to 10.70 nm (268-fold reduction). 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). 1H and 13C NMR analysis confirmed the conjugation between ibuprofen and each of the cationic polymers as well as the confirming that they did exist in amorphous state as multiple complexes. The TGA thermograms of the binary nanoconjugates exhibited one step degradation profile compared with the physical mixture formation of a new amide product. DSC thermal analysis showed that the nanoconjugates exhibited new broad and diffuse peaks which exhibited two steps. Marked enhancement of drug release was achieved by the surfactant solubilization techniques compared with the ibuprofen control.
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Keywords
Ibuprofen, Surfactant solubilization, DEAE-Dextran, Nanoconjugate