Browsing by Author "Kola-Mustapha, Adeola T"
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Item Development of aqueous ternary nanomatrix films: A novel ‘green’ strategy for the delivery of poorly soluble drugs(International Journal of Pharmaceutics (Elsevier), 2016) Kola-Mustapha, Adeola T; Armitage, David; Abioye, Amos OAqueous polymeric films have potentially great values in drug development, particularly in controlled drug release and taste masking strategies. However, the progressive polymer-particle coalescence that occurs randomly during film formation, curing and storage may render the film less permeable leading to erratic and unpredictable drug release profile. The focus of this study was to investigate the impacts of the in situ formation of polymer-drug nanoconjugate, at the interfacial nano-domains of two oppositely charged polymers, on the mechanism of film formation and to prepare aqueous ternary polymer-drug polymer nanomatrix films as a novel green strategy for the delivery of ibuprofen, a model poorly soluble drug. Composite and Layer-by-Layer films were prepared by aqueous casting technique using the concept of combined polymer-drug self-assembly and polyelectrolyte complexation. The plain and drug-loaded nanomatrix films were characterized using SEM, AFM, FTIR, DSC and TGA. Ibuprofen formed spherical core-shell microstructures (4.55 – 9.73 mm) in gellan film. However, in the presence of cationic dextran (Ddex), nanoconjugates (61.49 ± 5.97 – 447.52 ± 37.51 nm) were formed within the core of the film matrix. The composite films exhibited reduced tensile strength and lower elastic modulus with optimal conjugation efficiency of 98.14 ± 1.19%, which correlates with higher dissolution efficiency (99.76%) compared to 47.37% in layer-by-layer (LbL) films, dictated by Ddex concentration. Generally, the mechanism of drug release was by Fickian diffusion, however anomalous transport or polymer relaxation was also observed at higher concentration of Ddex. This study demonstrated the potential application of aqueous drug-loaded nanomatrix films as controlled drug delivery strategy for ibuprofen, a model poorly soluble drugItem Formulation and Characterization of Gellan–DEAE-Dextran Polyelectrolyte Complex Hydrogels(West African Journal of Pharmacy (West African Postgraduate College of Pharmacists), 2016) Kola-Mustapha, Adeola T; Abioye, Amos O.Background: There is a need to formulate hydrogels via direct physical interaction to circumvent the use of crosslinker which can affect the integrity of the entrapped drug in the hydrogel. Objective: The aim of this study is to formulate and characterize plain polyelectrolyte complex (PEC) hydrogels prepared by physical interaction between gellan gum and oppositely charged DEAE-Dextran. Method: Gellan-DEAE-Dextran (GDD) PEC hydrogels were prepared by polyelectrolyte complexation of gellan and DEAE-Dextran. The GDD-PEC hydrogels were characterized using Scanning Electron Microscopy (SEM), Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and Thermogravimetric Analysis (TGA). Their swelling kinetics and rheological properties were also evaluated. Results: Morphological characteristics analysed by SEM of plain gellan (G) hydrogel showed strand-like smooth compact structured surface while the GDD-PEC hydrogels exhibited crinkled rough surfaces. The shifts and disappearances in peaks shown in the FTIR spectra, suggested an interaction between gellan and DEAE-Dextran. DSC showed that the gellan and DEAE-Dextran merged into a single endothermic melting peak between 99.8 and 115.3 °C in the GDD-PEC hydrogels. Their TGA showed that the plain gellan (G) hydrogel was able to withstand more heat when compared to the GDD-PEC hydrogels. The GDD-PEC hydrogels exhibited pseudoplastic and elastic characteristics based on the concentration of DEAE-Dextran. The addition of DEAE-Dextran to GDD-PEC hydrogels significantly increased (p < 0.05, n = 4) their swelling ratio when compared to the plain gellan (G) hydrogel. Conclusion: GDD-PEC hydrogels were successfully formulated and characterized. This formulation has the potential for use in transdermal drug delivery systems.Item Polymer-Drug Nanoconjugate – An Innovative Nanomedicine: Challenges and Recent Advancements in Rational Formulation Design for Effective Delivery of Poorly Soluble Drugs(Pharmaceutical Nanotechnology (Betham Science), 2016) Abioye, Amos Olusegun; Chi, George Tangyie; Kola-Mustapha, Adeola T; Ruparelia, Ketan; Beresford, Ken; Aroo, RandolphBackground: Over the last four decades, the use of water soluble polymers in rational formulation design has rapidly evolved into valuable drug delivery strategies to enhance the safety and therapeutic effectiveness of poorly soluble drugs, particularly anticancer drugs. Novel advances in polymer chemistry have provided new generations of well defined polymeric architectures for specific applications in polymer-drug conjugate design. However, total control of crucial parameters such as particle size, molecular weight distribution, polydispersity, localization of charges, hydrophilic-lipophilic balance and non site-specific coupling reactions during conjugation has been a serious challenge. Objective: This review briefly describes the current advances in polymer-drug nanoconjugate design and various challenges hindering their transformation into clinically useful medicines. Method: Existing literature was reviewed. Results: This review provides insights into the significant impact of covalent and non-covalent interactions between drug and polymer on drug loading (or conjugation) efficiency, conjugate stability, mechanism of drug release from the conjugate and biopharmaceutical properties of poorly soluble drugs. The utility values and application of Quality by Design principles in rational design, optimization and control of the Critical Quality Attributes (CQA) and Critical Process Parameters (CPP) that underpin the safety, quality and efficacy of the nanoconjugates are also presented. Conclusion: It was apparent that better understanding of the physicochemical properties of the nanoconjugates as well as the drug-polymer interaction during conjugation process is essential to be able to control the biodistribution, pharmacokinetics, therapeutic activity and toxicity of the nanoconjugates which will in turn enhance the prospect of successful transformation of these promising nanoconjugates into clinically useful nanomedicines.