Nano-sized solid dispersions based on hydrophobic-hydrophilic conjugates for dissolution enhancement of poorly water-soluble drugs. 2017

Ha T T Dinh, and Phuong H L Tran, and Wei Duan, and Beom-Jin Lee, and Thao T D Tran
International University, Vietnam National University, Ho Chi Minh City, Vietnam.

The aim of this study was to investigate hydrophilic-hydrophobic conjugates as new carriers for nano-sized solid dispersions (SDs). The amphiphilic conjugates were prepared via an esterification reaction between hydroxypropyl methylcellulose (HPMC) and zein. Four formulations of conjugates were investigated with different ratios of zein to HPMC (1:5, 1:10, 1:20, and 1:40). Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy and particle size analyses were performed to characterize and optimize the formulation for SD. Isradipine and prednisolone were chosen as poorly water-soluble drugs for SD using the conjugate as a carrier. Dissolution tests, particle size analyses, powder X-ray diffraction and FTIR were conducted to determine the dissolution enhancement and its mechanism. The conjugate formed small particles as a self-assembled carrier. Although the SD with isradipine or prednisolone showed a small increase in particle size, the dissolution rate of those drugs in SD increased significantly compared to pure drugs. The interaction between the drug and conjugate was attributed to the formation of small particles and changes to the drug crystallinity. This study demonstrated that the hydrophilic-hydrophobic conjugate is a promising material for SD, with the potential of reducing drug particles to nano size in addition to promoting drug amorphousness or molecular interactions.

UI MeSH Term Description Entries
D004337 Drug Carriers Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers. Drug Carrier
D004951 Esterification The process of converting an acid into an alkyl or aryl derivative. Most frequently the process consists of the reaction of an acid with an alcohol in the presence of a trace of mineral acid as catalyst or the reaction of an acyl chloride with an alcohol. Esterification can also be accomplished by enzymatic processes. Esterifications
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
D013535 Suspensions Colloids with liquid continuous phase and solid dispersed phase; the term is used loosely also for solid-in-gas (AEROSOLS) and other colloidal systems; water-insoluble drugs may be given as suspensions. Suspension
D015028 Zein A group of alcohol-soluble seed storage proteins from the endosperm of corn.
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
D065546 Drug Liberation Release of drugs from DOSAGE FORMS into solution. Drug Dissolution,Drug Release,Dissolution, Drug,Liberation, Drug,Release, Drug

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