Purpose: In this work, the three most common formulation methods used to prepare solid dispersion (SD) such as spray-drying, solvent casting method, and freeze-drying, have been compared in order to investigate their capability in increase the most drug dissolution profile. Methods: Three formulation strategies have been used to prepare a mixture of Polyvinyl-Alcohol (PVA) and Maltodextrin (MDX) as SD loaded with three model poorly soluble drugs: Olanzapine, Dexamethasone and Triamcinolone acetonide. The formulations obtained have been analysed and compared in term of drugs particle size, drug-loading capacity, surface homogeneity, and dissolution profile enhancement. Physical-chemical characterization has been conducted on both drugs molecules and obtained formulations by thermal analysis and infrared spectroscopy.Result: The polymers used were able to increase drugs saturation solubility. The formulation strategies effected the drugs particles size, and solvent casting method resulted to give more
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This study unravels a formulation made of food‐based microparticles (MPs) able to control the release of quercetin, a natural anticancer compound, which activity is only limited by its poor aqueous solubility and consequent low bioavailability. To solve this issue, a spray‐dried micro delivery system was developed using a bench mini spray dryer B290 Buchi. The resulting MPs were only manufactured with food‐derived ingredients such as whey proteins and milk, avoiding the use of any other synthetic material. These microparticles were characterised with a testing campaign encompassing either the physical–chemical characterisation with SEM, DSC and DLS, or the technological and biological features with in vitro, ex vivo and in vivo studies, the latter being characterised by a human colon cancer xenograft model. These studies showed as the quercetin solubility and release rate improved when tested in condition mimicking oral administration, resulting in a general improvement of its bioavailability and the consequent anticancer activity. This study shows as the whey proteins may serves as natural adjuvant able to provide valuable technological features when used to manufactures micro carriers by spray drying.
In the present study, gastro-resistant microparticles (MPs) were produced using the spray-drying technique as controlled-release systems for some model liposoluble vitamins, including retinyl-palmitate, retinyl-acetate, β-carotene, cholecalciferol and α-tocopherol. The gastroprotective action of three different gastro-resistant excipients, the anionic methacrylic copolymer (Eudraguard®® Biotic, E1207), the cellulose acetate phthalate (CAP) and whey proteins (WPs), was compared. The latter was used to produce a novel delivery system manufactured with only food-derived components, such as milk, and showed several improvements over the two synthetic gastro-resistant agents. Scanning electron microscopy (SEM) images showed a quite homogeneous spherical shape of all microparticle batches, with an average diameter between 7 and 15 μm. FTIR analysis was used to evaluate the effective incorporation of vitamins within the microparticles and the absence of any degradation to the components of the formulation. The comparison graphs of differential scanning calorimetry (DSC) confirmed that the spray drying technique generates a solid in which the physical interactions between the excipients and the vitamins are very strong. Release studies showed a prominent pH-controlled release and partially a delayed-release profile. Ex vivo permeation studies of retinyl palmitate, retinyl acetate and α-tocopherol revealed greater transmucosal permeation capacity for microparticles produced with the WPs and milk.
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