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Dual-nozzle spray deposition process for improving the stability of proteins in polymer microneedles

机译:双喷嘴喷雾沉积工艺可提高聚合物微针中蛋白质的稳定性

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Polymer microneedles are an attractive way of transdermal delivery of various pharmaceutical compounds. Fabrication of drug-encapsulating polymer microneedles, however, often involves processing conditions unfavorable for maintaining the stability of drugs, including highly concentrated formulations, high temperature and long drying time. The stability of labile substances in biodegradable polymer matrices could also be significantly reduced by the use of organic solvents and emulsification. In this paper, we reported a new fabrication technique called the dual-nozzle spray deposition process, which utilizes a separate deposition of drug and polymer solutions, as a potential way to address the stability issue associated with current microneedle fabrication processes. A model protein, bovine serum albumin (BSA), was successfully incorporated into both water-soluble poly(vinyl alcohol) (PVA) and biodegradable poly(lactic-co-glycolic acid) (PLGA) microneedles by the dual-nozzle spray deposition process. The conformational change of BSA examined by circular dichroism and fluorescence spectroscopy suggests that the developed process helps maintain the structural stability of BSA during encapsulation in both PVA and PLGA matrices. We anticipate that the dual-nozzle spray deposition process would improve the stability of drugs by reducing adverse interaction with solvents and eliminating the emulsification process. Also, the developed process could be an attractive approach to fabricating polymer-based drug delivery devices.
机译:聚合物微针是各种药物化合物经皮递送的一种有吸引力的方式。然而,包封药物的聚合物微针的制造通常涉及不利于维持药物稳定性的加工条件,包括高浓度制剂,高温和长干燥时间。通过使用有机溶剂和乳化,不稳定物质在可生物降解的聚合物基质中的稳定性也可能大大降低。在本文中,我们报道了一种称为双喷嘴喷雾沉积工艺的新制造技术,该技术利用药物和聚合物溶液的单独沉积,作为解决与当前微针制造工艺相关的稳定性问题的潜在方法。通过以下方法,将模型蛋白牛血清白蛋白(BSA)成功地掺入了水溶性聚乙烯醇(PVA)和可生物降解的聚乳酸-乙醇-乙醇酸(PLGA)微针中双喷嘴喷雾沉积工艺。通过圆二色性和荧光光谱法检查的BSA的构象变化表明,所开发的方法有助于在PVA和PLGA基质封装过程中维持BSA的结构稳定性。我们预期双喷嘴喷雾沉积工艺将通过减少与溶剂的不利相互作用并消除乳化工艺来提高药物的稳定性。同样,开发的工艺可能是制造基于聚合物的药物输送装置的一种有吸引力的方法。

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