Development of Solid Dispersion by Hot Melt Extrusion Using Mixtures of Polyoxylglycerides With Polymers as Carriers for Increasing Dissolution Rate of a Poorly Soluble Drug Model

Vasoya, Jaydip M.; Desai, Heta; Gumaste, Suhas G.; Tillotson, John; Kelemen, Donald; Dalrymple, Damon M.; Serajuddin, Abu T.M.

doi:10.1016/j.xphs.2018.09.019

Cited by 38 publications

(17 citation statements)

References 33 publications

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“…Whereas, a thermogram of MAG 10 shows one sharp endothermic peak of approximately 48 °C corresponding to the melting temperature (T m ) of monoacylglycerol, no melting peak was observed in the PVB/MAG 10 sample. Similar results obtained by DSC characterization were proved in the study of Vasoya et al [ 56 ], in which various polyglycerides have been investigated as potential carriers for poorly water-soluble drugs. Miscibility of PVB fibers and MAG 10 can be also presumed based on the SEM results ( Figure 3 ), where a change in fibers’ shape was observed with increasing monocaprin concentration.…”

Section: Resultssupporting

confidence: 88%

Novel Polyvinyl Butyral/Monoacylglycerol Nanofibrous Membrane with Antifouling Activity

et al. 2020

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Monoacylglycerols (MAGs) have proven of great interest to the foodstuffs industry due to the promising antibacterial activity they show for controlling microbial contamination. Prior to this paper, this antibacterial agent had not been incorporated in a nanofibrous membrane. This study details convenient fabrication of nanofibrous membranes based on polyvinyl butyral (PVB) containing various concentrations of monocaprin (MAG 10) by an electrospinning process. Increasing the concentration of MAG 10 caused differences to appear in the shape of the nanofibers, in addition to which the level of wettability was heightened. Besides exhibiting antibacterial properties, the functional membranes demonstrated especially good antifouling activity. The novel and efficient nanofibrous membranes described have the potential to find eventual application in medical or environmental fields.

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Section: Resultssupporting

confidence: 88%

Novel Polyvinyl Butyral/Monoacylglycerol Nanofibrous Membrane with Antifouling Activity

et al. 2020

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“…As mentioned earlier, carvedilol is a poorly watersoluble weakly basic drug demonstrating low aqueous solubility at intestinal pH conditions. 44 However, it is apparent from Figure 13 that the dissolution of drug from carvedilol-PVA binary extrudates and carvedilol-PVA-sorbitol ternary extrudates is pH-independent because high dissolution rates were observed at both pH 2 and 6.8.…”

Section: Moisture Sorption Analysismentioning

confidence: 97%

Development of 3D Printed Tablets by Fused Deposition Modeling Using Polyvinyl Alcohol as Polymeric Matrix for Rapid Drug Release

Wei

Solanki

Vasoya

et al. 2020

Journal of Pharmaceutical Sciences

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“…Improving the solubility of drugs is a significant challenge in the drug discovery field. Strategies have many approaches, such as micronization [2], cocrystallization [3], complexation [4], nanoparticle engineering, and solid dispersion [5][6][7][8]. Amorphous solid dispersions (ASDs) are dispersed amorphous drugs in a suitable polymeric carrier matrix, which typically form amorphous APIs leading to improved water solubility and dissolution rates due to the amorphous state exhibiting increased free energy, enthalpy, and entropy compared with the crystalline form.…”

Section: Introductionmentioning

confidence: 99%

Orodispersible Polymer Films with the Poorly Water-Soluble Drug, Olanzapine: Hot-Melt Pneumatic Extrusion for Single-Process 3D Printing

et al. 2020

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Amorphous solid dispersions (ASDs) improve the oral delivery of poorly water-soluble drugs. ASDs of olanzapine (OLZ), which have a high melting point and low solubility, are performed using a complicated process. Three-dimensional (3D) printing based on hot-melt pneumatic extrusion (HMPE) is a simplified method for producing ASDs. Unlike general 3D printing, printlet extrusion is possible without the preparation of drug-loaded filaments. By heating powder blends, direct fused deposition modeling (FDM) printing through a nozzle is possible, and this step produces ASDs of drugs. In this study, we developed orodispersible films (ODFs) loaded with OLZ as a poorly water-soluble drug. Various ratios of film-forming polymers and plasticizers were investigated to enhance the printability and optimize the printing temperature. Scanning electron microscopy (SEM) showed the surface morphology of the film for the optimization of the polymer carrier ratios. Differential scanning calorimetry (DSC) was used to evaluate thermal properties. Powder X-ray diffraction (PXRD) confirmed the physical form of the drug during printing. The 3D printed ODF formulations successfully loaded ASDs of OLZ using HMPE. Our ODFs showed fast disintegration patterns within 22 s, and rapidly dissolved and reached up to 88% dissolution within 5 min in the dissolution test. ODFs fabricated using HMPE in a single process of 3D printing increased the dissolution rates of the poorly water-soluble drug, which could be a suitable formulation for fast drug absorption. Moreover, this new technology showed prompt fabrication feasibility of various formulations and ASD formation of poorly water-soluble drugs as a single process. The immediate dissolution within a few minutes of ODFs with OLZ, an atypical antipsychotic, is preferred for drug compliance and administration convenience.

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Development of Solid Dispersion by Hot Melt Extrusion Using Mixtures of Polyoxylglycerides With Polymers as Carriers for Increasing Dissolution Rate of a Poorly Soluble Drug Model

Cited by 38 publications

References 33 publications

Novel Polyvinyl Butyral/Monoacylglycerol Nanofibrous Membrane with Antifouling Activity

Novel Polyvinyl Butyral/Monoacylglycerol Nanofibrous Membrane with Antifouling Activity

Development of 3D Printed Tablets by Fused Deposition Modeling Using Polyvinyl Alcohol as Polymeric Matrix for Rapid Drug Release

Orodispersible Polymer Films with the Poorly Water-Soluble Drug, Olanzapine: Hot-Melt Pneumatic Extrusion for Single-Process 3D Printing

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