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Methylamine acts as excellent chemical trigger to Harden emulsion droplets into spongy PLGA microspheres

机译:甲胺充当优异的化学触发器,使硬化乳液液滴进入海绵状PLGA微球

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The purpose of this research was to produce porous sponge-like PLGA microspheres through a simple emulsion technique using a non-halogenated organic solvent and methylamine. In order to achieve this objective, a dispersed phase consisting of PLGA and methyl propionate was emulsified in an aqueous polyvinyl alcohol solution to produce an oil-in-water emulsion. When methylamine was added to the aqueous phase, it partitioned to the oil phase and reacted with methyl propionate to produce methanol and N -methyl propionamide. These water-soluble decomposition products acted as anti-solvents against PLGA. As they leached to the aqueous phase, oil droplets effectively hardened to sponge-like microspheres. This technique, utilizing a chemical reaction between the dispersed solvent and methylamine, has shown excellence compared to the existing water-in-oil-in-water emulsion techniques that require the help of porogens. For example, even without using porogens and high-shear/high-energy mixing devices, our simple technology made it possible to produce very porous microspheres with a sponge-like skeleton. Also, rather than using halogenated methylene chloride, which has been commonly used to produce microspheres, this new technique used methyl propionate, a non-halogenated and safer alternative. Furthermore, it enabled us to adjust the amount of residual methyl propionate in the microspheres below 0.5%, meeting the standard of residual organic solvents in microspheres set by regulatory authorities. The innovative technology reported in this study would make a large contribution to producing porous microspheres with the use of various hydrophobic polymers.
机译:本研究的目的是通过使用非卤化有机溶剂和甲胺的简单乳液技术产生多孔海绵状PLGA微球。为了达到该目的,将由PLGA和丙酸甲酯组成的分散相在水性聚乙烯醇溶液中乳化,以产生水包油乳液。当将甲胺加入水相时,它将其分配给油相并与丙酸甲酯反应以产生甲醇和N-甲基丙胺。这些水溶性分解产物用作抗PLGA的抗溶剂。当它们浸出到水相时,油滴有效地硬化为像海绵状微球。这种技术利用分散溶剂和甲胺之间的化学反应,与需要散孔的现有的水包内乳液技术相比,卓越表现出来。例如,即使在不使用散装和高剪切/高能量混合装置的情况下,我们的简单技术也使得可以产生非常多孔的微球,用海绵状骨架。此外,该技术使用常用于生产微球的卤代二氯甲烷,而不是使用卤代二氯甲烷,而不是使用卤代二氯甲烷,该技术使用甲基丙酸甲酯,非卤化和更安全的替代品。此外,它使我们能够调节低于0.5%以下的微球中丙酸的残留甲基量,满足监管机构设定的微球中残留有机溶剂的标准。本研究报告的创新技术将对使用各种疏水聚合物产生多孔微球进行大量贡献。

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