Sustained Release of Poorly Water-Soluble Drug from Hydrophilic Polymeric Film Sandwiched Between Hydrophobic Layers. 2018

Bhavesh D Kevadiya, and Lu Zhang, and Rajesh N Davé
Department of Chemical, Biochemical, and Pharmaceutical Engineering, New Jersey Institute of Technology, Newark, New Jersey, USA.

This proof-of-concept study explores the feasibility of using a drug-loaded hydrophilic polymeric layer sandwiched between two hydrophobic layers for improving film drug load while achieving sustained release of poorly water-soluble drug. Such films having total thickness in range ~ 146-250 μm were prepared by slurry-based casting using hydrophilic hydroxypropyl methylcellulose (HPMC) as matrix layer containing fenofibrate (FNB) as the model drug, encased between two very thin rate-limiting layers of 10 μm each of hydrophobic poly-ɛ-caprolactone (PCL). Film precursor slurry consisted of HPMC with plasticizer and water along with micronized FNB powders, which were dry-coated with hydrophilic silica. Characterization techniques demonstrated the presence of homogeneously dispersed crystalline FNB in films. The films are very thin and hence two-dimensional; hence, average drug load per unit area in range ~ 5 to ~ 9 mg/cm2 could be achieved by altering the thickness of the drug matrix layer. Drug amount and drug content uniformity were measured through assay of ten circular samples ~ 0.712 cm2 in area punched out using a circular-shaped punch tool. Drug release rate was investigated using USP IV flow-through cell and surface dissolution imaging system. Thinner films followed Fickian diffusion, and thicker films followed non-Fickian anomalous diffusion. Overall, the application of middle layer thickness could be used as a tool to manipulate drug load without the need for altering its formulation or precursor preparation by changing its thickness, hence achieving relatively high drug loading yet having sustained release of drug.

UI MeSH Term Description Entries
D011108 Polymers Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS). Polymer
D003692 Delayed-Action Preparations Dosage forms of a drug that act over a period of time by controlled-release processes or technology. Controlled Release Formulation,Controlled-Release Formulation,Controlled-Release Preparation,Delayed-Action Preparation,Depot Preparation,Depot Preparations,Extended Release Formulation,Extended Release Preparation,Prolonged-Action Preparation,Prolonged-Action Preparations,Sustained Release Formulation,Sustained-Release Preparation,Sustained-Release Preparations,Timed-Release Preparation,Timed-Release Preparations,Controlled-Release Formulations,Controlled-Release Preparations,Extended Release Formulations,Extended Release Preparations,Slow Release Formulation,Sustained Release Formulations,Controlled Release Formulations,Controlled Release Preparation,Controlled Release Preparations,Delayed Action Preparation,Delayed Action Preparations,Formulation, Controlled Release,Formulations, Controlled Release,Prolonged Action Preparation,Release Formulation, Controlled,Release Formulations, Controlled,Sustained Release Preparation,Timed Release Preparation,Timed Release Preparations
D006118 Griseofulvin An antifungal agent used in the treatment of TINEA infections. Fulvicin-U-F,Grifulvin V,Gris-PEG,Grisactin,Grisefuline,Fulvicin U F,FulvicinUF,Gris PEG,GrisPEG
D012995 Solubility The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Solubilities
D014867 Water A clear, odorless, tasteless liquid that is essential for most animal and plant life and is an excellent solvent for many substances. The chemical formula is hydrogen oxide (H2O). (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) Hydrogen Oxide
D014961 X-Ray Diffraction The scattering of x-rays by matter, especially crystals, with accompanying variation in intensity due to interference effects. Analysis of the crystal structure of materials is performed by passing x-rays through them and registering the diffraction image of the rays (CRYSTALLOGRAPHY, X-RAY). (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) Xray Diffraction,Diffraction, X-Ray,Diffraction, Xray,Diffractions, X-Ray,Diffractions, Xray,X Ray Diffraction,X-Ray Diffractions,Xray Diffractions
D016503 Drug Delivery Systems Systems for the delivery of drugs to target sites of pharmacological actions. Technologies employed include those concerning drug preparation, route of administration, site targeting, metabolism, and toxicity. Drug Targeting,Delivery System, Drug,Delivery Systems, Drug,Drug Delivery System,Drug Targetings,System, Drug Delivery,Systems, Drug Delivery,Targeting, Drug,Targetings, Drug
D053758 Nanoparticles Nanometer-sized particles that are nanoscale in three dimensions. They include nanocrystaline materials; NANOCAPSULES; METAL NANOPARTICLES; DENDRIMERS, and QUANTUM DOTS. The uses of nanoparticles include DRUG DELIVERY SYSTEMS and cancer targeting and imaging. Nanocrystalline Materials,Nanocrystals,Material, Nanocrystalline,Materials, Nanocrystalline,Nanocrystal,Nanocrystalline Material,Nanoparticle
D057927 Hydrophobic and Hydrophilic Interactions The thermodynamic interaction between a substance and WATER. Hydrophilic Interactions,Hydrophilic and Hydrophobic Interactions,Hydrophilicity,Hydrophobic Interactions,Hydrophobicity,Hydrophilic Interaction,Hydrophilicities,Hydrophobic Interaction,Hydrophobicities,Interaction, Hydrophilic,Interaction, Hydrophobic,Interactions, Hydrophilic,Interactions, Hydrophobic
D065347 Hypromellose Derivatives Polymeric compounds that contain repeating units of hydroxypropyl methylcellulose. The properties of hypromellose polymers can vary greatly and are defined by their molecular weight, the percentage of hydroxyl groups, the percentage of hydroxypropyl groups, and viscosity measurements. They are found a broad variety of commercial products such as FOOD ADDITIVES; EXCIPIENTS; and LUBRICANTS. HPMC 2910,HPMC-K-100 M,Hydroxypropyl Methylcellulose,Hydroxypropylmethylcellulose,Hypromellose,K-8515,K8515,MHPC Polymer,Methocel E,Methoxyhydroxypropylcellulose,Methyl Hydroxypropyl Cellulose,Methyl-hydroxypropyl-cellulose,Derivative, Hypromellose,Derivatives, Hypromellose,HPMC K 100 M,HPMCK100 M,Hypromellose Derivative,K 8515

Related Publications

Bhavesh D Kevadiya, and Lu Zhang, and Rajesh N Davé
September 2008, Acta pharmaceutica (Zagreb, Croatia),
Bhavesh D Kevadiya, and Lu Zhang, and Rajesh N Davé
July 2007, Chemical & pharmaceutical bulletin,
Bhavesh D Kevadiya, and Lu Zhang, and Rajesh N Davé
May 2018, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences,
Bhavesh D Kevadiya, and Lu Zhang, and Rajesh N Davé
January 1982, Biomaterials,
Bhavesh D Kevadiya, and Lu Zhang, and Rajesh N Davé
August 2020, Pharmaceutical research,
Bhavesh D Kevadiya, and Lu Zhang, and Rajesh N Davé
December 2003, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences,
Bhavesh D Kevadiya, and Lu Zhang, and Rajesh N Davé
April 2017, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V,
Bhavesh D Kevadiya, and Lu Zhang, and Rajesh N Davé
May 2000, Journal of controlled release : official journal of the Controlled Release Society,
Copied contents to your clipboard!