Jones E., Ojewole E., Kalhapure R., Govender T.
Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa
Jones, E., Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa; Ojewole, E., Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa; Kalhapure, R., Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa; Govender, T., Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa
Drug delivery via the buccal route has emerged as a promising alternative to oral drug delivery. Didanosine (DDI) undergoes rapid degradation in the gastrointestinal tract, has a short half-life and low oral bioavailability, making DDI a suitable candidate for buccal delivery. Recent developments in buccal drug delivery show an increased interest toward nano-enabled delivery systems. The advantages of buccal drug delivery can be combined with that of nanoparticulate delivery systems to provide a superior delivery system. The aim of this study was to design and evaluate the preparation of novel nano-enabled films for buccal delivery of DDI. Solid lipid nanoparticles (SLNs) were prepared via hot homogenization followed by ultrasonication and were characterized before being incorporated into nano-enabled monolayered multipolymeric films (MMFs). Glyceryl tripalmitate with Poloxamer 188 was identified as most suitable for the preparation of DDI-loaded SLNs. SLNs with desired particle size (PS) (201nm), polydispersity index (PDI) (0.168) and zeta potential (-18.8mV) were incorporated into MMFs and characterized. Conventional and nano-enabled MMFs were prepared via solvent casting/evaporation using Eudragit RS100 and hydroxypropyl methylcellulose. Drug release from the nano-enabled films was found to be faster (56% versus 20% in first hour). Conventional MMFs exhibited higher mucoadhesion and mechanical strength than nano-enabled MMFs. SLNs did not adversely affect the steady state flux (71.63±13.54μg/cm2h versus 74.39±15.95μg/cm2h) thereby confirming the potential transbuccal delivery of DDI using nano-enabled MMFs. Nano-enabled buccal films for delivery of DDI can be successfully prepared, and these physico-mechanical studies serve as a platform for future formulation optimization work in this emerging field. © 2014 Informa Healthcare USA, Inc.
citric acid triethyl ester; cyclosporin A; didanosine; eudragit rs; hydroxypropylmethylcellulose; methanol; paromomycin; placebo; poloxamer; pravastatin; solid lipid nanoparticle; testosterone; tripalmitin; water; zidovudine; anti human immunodeficiency virus agent; didanosine; lipid; nanoparticle; poloxamer; polymer; triacylglycerol; tripalmitin; animal experiment; antiviral therapy; article; cheek mucosa; controlled study; cross linking; dispersion; domestic pig; drug design; drug penetration; drug screening; drug solubility; drug stability; drug synthesis; evaporation; lipid analysis; lipid solubility; melting point; mucoadhesion; nanoemulsion; nonhuman; particle size; pH; photon correlation spectroscopy; polymerization; porcine model; room temperature; steady state; sustained drug release; tensile strength; Young modulus; zeta potential; adhesion; buccal drug administration; chemistry; comparative study; drug delivery system; HIV Infections; human; medicinal chemistry; permeability; ultrastructure; Adhesiveness; Administration, Buccal; Anti-HIV Agents; Chemistry, Pharmaceutical; Didanosine; Drug Delivery Systems; Elastic Modulus; HIV Infections; Humans; Lipids; Nanoparticles; Particle Size; Permeability; Poloxamer; Polymers; Tensile Strength; Triglycerides
