Browsing by Author "Kola-Mustapha, Adeola Tawakalitu"

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    Antifungal Screening of Ceiba petandra and Lannea kerstingii Stem Bark Extract Cream Formulations
    (Journal of Pharmaceutical Sciences and Pharmacy Practice, 2014) Kola-Mustapha, Adeola Tawakalitu; Aremu, Olusola; Njinga, Stan; Ayotunde, Hameedat
    Aim: Evaluation of the potential application of Ceiba petandra and Lannea kerstingii creams in the management of topical dermatophytic infections. Methodology: Antifungal activities of methanolic extract of Ceiba petandra, ethyl acetate extract of Lannea kerstingii stem barks, their combinations and their cream formulations were studied by the agar well diffusion method. Clinical isolates of Trichophyton rubrum and Trichophyton mentagrophytes were used as test organisms, while modified Aqueous Cream (BP) was used as the cream base. The extracts were incorporated into modified aqueous cream at concentrations 0.4, 0.8, 1.6, 2.4 and 3.2% w/w. Griseofulvin and ketoconazole cream were used as reference antifungal agents. Results: Extracts of Ceiba petandra, Lannea kerstingii and their combinations exhibited significant levels of antifungal activity (p < 0.05) against the test dermatophytes. Diameters of inhibition zones ranged from 11.00 ± 0.29 mm to 24.30 ± 0.02 mm for the extracts and 3.00 ± 0.82 mm to 26.33 ± 0.94 mm for the cream formulations, as extract concentrations increased from 0.4 to 3.2% w/w. More inhibitory activities were exerted against Trichophyton rubrum compared to Trichophyton mentagrophytes. Conclusion: Stem bark extracts of Ceiba petandra and Lannea kerstingii and their cream formulations possess useful antifungal activities against some causative agents of dermatophytoses.
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    Characterization of Ceiba petandra and Lannea kerstingii Stem Bark Extract Creams
    (Journal of Pharmaceutical and Health Sciences (Islamic Azad University Tehran Iran, Pharmaceutical Sciences Branch), 2017) Aremu, Olusola Isaac; Kola-Mustapha, Adeola Tawakalitu; Ayotunde, Hameedat Taiye
    Aim: Formulation of extracts of Ceiba petandra and Lannea kerstingii into creams. Methodology: The stem barks of Ceiba petandra and Lannea kerstingii were extracted using methanol and ethyl acetate respectively. The obtained extracts and their combinations were formulated into creams using modified Aqueous Cream BP base at concentrations ranging from 0.4 to 3.2% w/w. Physical and chemical characteristics of the creams such as stability, viscosity, pH, diffusion, irritancy and elegancy were evaluated. Ketoconazole cream was used as the reference product. Results: Creams prepared with each extract alone exhibited good characteristics in terms of spreadability, non-irritancy, stability and diffusivity. Creams formulated with Ceiba petandra were most stable, with pH ranges of 6.21 to 7.13. Those formulated with Lannea kerstingi were more acidic. Creams formulated with the combinations of the two extracts exhibited some levels of incompatibility, which increased with increasing extract concentrations. The rate of diffusion of extracts from cream base increased with time and was generally more at 37 °C as compared to that at 25 °C. Conclusion: Cream formulations of the stem bark extracts of Ceiba petandra and Lannea kerstingii but not their combinations using Aqueous Cream Base (BP) possesses good characteristics.
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    Characterization of Ceiba petandra and Lannea kerstingii Stem Bark Extract Creams
    (2017) Aremu, Olusola Isaac; Kola-Mustapha, Adeola Tawakalitu; Ayotunde, Taiye Hameedat
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    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, Amos
    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 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.
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    Evaluation of Terminalia macroptera (Combretaceae) Guill. & Perr stem bark extract incorporated into an emulgel for the potential management of rheumatoid arthritis
    (Elsevier, 2023) Kola-Mustapha, Adeola Tawakalitu; Taiwo, Suleiman Olubusayomi; Isiaka, Abimbola Rofiat; Amao, Sherifat Omowunmi; Ishola, Ismail O.; Ghazali, Yusuf Oluwagbenga; Usman, Sukurat Olasumbo
    Abstract: Background: Rheumatoid Arthritis (RA) is a chronic disease which causes inflammation and damage to the joint. The goals of treatment are to stop inflammation, relieve symptoms, improve physical function and overall well-being. The purpose of this study was to evaluate Terminalia macroptera stem bark (TMB) ethanol extract and formulate it into an herbal emulgel (TME) for the potential management of RA. Methods: Phytochemical analysis and anti-inflammatory activity of TMB were first evaluated using standard analytical methods and complete Freund's adjuvant (CFA) induced arthritis model in rats respectively. Post-formulation, physical characterization of the carbopol 940 based herbal emulgels (TME) and the reduction in the induced rat paw sizes by the herbal emulgels were evaluated using diclofenac emulgel as the positive control. Results: Phytochemical screening revealed the presence of flavonoids, tannins, terpenoids, saponins, and alkaloids. Inflammatory activity of the extract gave the highest percentage inhibition with TMB (50 mg/kg). The formulated herbal emulgels had good spreadability, extrudability, pH ranging from 4.5±0.2 to 6.9±0.4 and viscosity ranging from 0.36 ± 0.20 to 8.37 ± 0.65 Pas at 6 rpm and 0.26 ± 0.01 to 10.67±0.96 Pas at 12 rpm. TME emulgel significantly (p < 0.05) reduced oedema formation and arthritic index induced by complete Freund's adjuvant in rats. TME showed dose-dependent anti-inflammatory activity comparable with commercial diclofenac emulgel. Conclusion: TMB showed an excellent inhibitory activity on the induced paw of the test animals which makes it a suitable candidate in a topical herbal emulgel formulation (TME) for the potential use in the management of RA.
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    Ex vivo skin permeation and retention studies on chitosan-ibuprofen-gellan ternary nanogel prepared by in situ ionic gelation technique – a tool for controlled transdermal delivery of ibuprofen
    (International Journal of Pharmaceutics, 2015-07) Abioye, Amos Olusegun; Issah, Sureya; Kola-Mustapha, Adeola Tawakalitu
    The chemical potentials of drug-polymer electrostatic interaction have been utilized to develop a novel ternary chitosan-ibuprofen-gellan nanogel as controlled transdermal delivery tool for ibuprofen. The ternary nanogels were prepared by a combination of electrostatic nanoassembly and ionic gelation techniques. The electrostatic and hydrophobic interactions as well as hydrogen bonding between ibuprofen and chitosan were confirmed with FTIR, while DSC, TGA and SEM confirmed the physical state, thermal and morphological characteristics, respectively. The ex vivo delivery of ibuprofen onto and across the skin was evaluated based on system specific drug release parameters such as steady state permeation rate, permeability coefficient, permeability enhancement ratio, skin/gel partition coefficient, diffusion coefficient, lag time and release rate constant and mechanisms of release were determined using mathematical models. Interaction between ibuprofen and chitosan produced new spherical eutectic nanoconjugates with remarkable decrease in particle size of ibuprofen from 4580 (length-to-breadth aspect ratio) to a minimum of 14.15 nm (324-times), and thermally stable amorphous characteristics. The nanogels exhibited significant elastic and pseudoplastic characteristics dictated by the concentration of chitosan with maximum swelling capacity of 775% w/w at 6.55 mM chitosan compared with 281.16 and 506.50% for plain gellan and control ibuprofen hydrogel, respectively. Chitosan enhanced the skin penetration, permeability and the rate of transdermal release of ibuprofen by a factor of 4, dictated by the extent of ibuprofen-chitosan ionic interaction and its concentration. The major mechanism of ibuprofen release through the pig skin was drug diffusion however drug partition and matrix erosion also occurred. It was evident that ternary nanogels are novel formulations with potential application in controlled transdermal delivery of ibuprofen.
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    Formulation and physical characterization of Ibuprofen-DEAE-Dextran nanoconjugates via surfactant solubilization
    (West African Journal of Pharmacy, 2015) Kola-Mustapha, Adeola Tawakalitu; Abioye, Amos
    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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    Thermodynamic Changes Induced by Intermolecular Interaction Between Ibuprofen and Chitosan: Effect on Crystal Habit, Solubility and In Vitro Release Kinetics of Ibuprofen
    (Pharmaceutical Research, 2016-02) Abioye, Amos Olusegun; Armitage, Rachel; Kola-Mustapha, Adeola Tawakalitu
    The direct impact of intermolecular attraction between ibuprofen and chitosan on crystal behaviour, saturated solubility and dissolution efficiency of ibuprofen was investigated in order to expand the drug delivery strategy for ibuprofen. METHODS: Amorphous nanoparticle complex (nanoplex) was prepared by controlled drug-polymer nanoassembly. Intermolecular attraction was confirmed with surface tension, conductivity measurements and FTIR spectroscopy. The nanoplex was characterized using DSC, TGA and SEM. The in vitro release kinetics and mechanism of drug release were evaluated using mathematical models. RESULTS: The cmc of ibuprofen decreased significantly in the nanoplex (1.85 mM) compared with pure ibuprofen (177.62 mM) suggesting a remarkable affinity between the chitosan and ibuprofen. The disappearance of ibuprofen melting peak in the nanoplex and the broadened DSC endothermic peaks of the nanoplex indicate formation of eutectic amorphous product which corresponded to higher saturated solubility and dissolution velocity. Ibuprofen (aspect ratio 5.16 ± 1.15) was converted into spherical nanoparticle complex with particle size of 14.96 ± 1.162-143.17 ± 17.5247 nm (36-345 folds reduction) dictated by chitosan concentration. Pure ibuprofen exhibited burst release while the nanoplexes showed both fast and extended release profiles. DE increased to a maximum (81.76 ± 2.1031%) with chitosan concentrations at 3.28 × 10-3 g/dm3, beyond which retardation occurred steadily. Major mechanism of drug release from the nanoplex was by diffusion however anomalous transport and super case II transport did occur. CONCLUSION: Ibuprofen-chitosan nanoplex exhibited combined fast and extended release profile dictated by chitosan concentration. This study demonstrated the potential application of drug-polymer nanoconjugate design in multifunctional regulated drug delivery.