Browsing by Author "Abioye, Amos"
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Item The effect of Ibuprofen-DEAE-Dextran nanoconjugates (surfactant solubilization) on the thermal properties and in vitro drug release kinetics of ibuprofen(Nigerian Journal of Pharmacy, 2015) Kola-Mustapha, Adeola Tawakalitu; Abioye, AmosBackground: 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 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.Item Formulation and physical characterization of Ibuprofen-DEAE-Dextran nanoconjugates via surfactant solubilization(West African Journal of Pharmacy, 2015) Kola-Mustapha, Adeola Tawakalitu; Abioye, AmosIt 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.