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基于乙酰化腰果胶的纳米粒子用于生物碱表异长春碱的包载。

Acetylated cashew gum-based nanoparticles for the incorporation of alkaloid epiisopiloturine.

机构信息

Núcleo de Pesquisa em Biodiversidade e Biotecnologia, BIOTEC, Campus Ministro Reis Velloso, Universidade Federal do Piauí, UFPI, Parnaíba, Piauí, Brazil.

Laboratório de Polímeros, LabPol, Campus do Pici, Universidade Federal do Ceará, UFC, Fortaleza, Ceará, Brazil.

出版信息

Int J Biol Macromol. 2019 May 1;128:965-972. doi: 10.1016/j.ijbiomac.2019.01.206. Epub 2019 Jan 31.

Abstract

The natural alkaloid epiisopiloturine has recently become the focus of study for various medicinal properties, particularly for its anti-inflammatory and antischistosomal effect. The incorporation of active molecules in natural polymeric matrices has garnered increasing interest during recent decades. A new derivative of cashew gum successfully obtained by gum acetylation has shown great potential as a carrier in controlled drug release systems. In this work, epiisopiloturine was encapsulated in acetylated cashew gum nanoparticles in order to increase solubility and allow slow release, whereas the morphology results were supported by computer simulations. The particles were produced under a variety of conditions, and thoroughly characterized using light scattering and microscopic techniques. The particles were spherical and highly stable in solution, and showed drug incorporation at high levels, up to 55% efficiency. Using a dialysis-based in vitro assay, these particles were shown to release the drug via a Fickian diffusion mechanism, leading to gradual drug release over approximately 6 h. These nanoparticles show potential for the use as drug delivery system, while studies on their potential anti-inflammatory action, as well as toxicity and efficacy assays would need to be performed in the future to confirm their suitability as drug delivery candidates.

摘要

天然生物碱表异岗田素最近因其抗炎和抗血吸虫作用而成为研究的焦点。在过去几十年中,将活性分子掺入天然聚合物基质中引起了越来越多的关注。通过胶乳乙酰化成功获得的一种新型腰果胶衍生物已显示出作为控制药物释放系统载体的巨大潜力。在这项工作中,表异岗田素被包封在乙酰化腰果胶纳米颗粒中,以提高溶解度并允许缓慢释放,而形态结果则得到了计算机模拟的支持。在各种条件下生产了这些颗粒,并使用光散射和显微镜技术对其进行了全面的表征。这些颗粒在溶液中呈球形且高度稳定,并且显示出药物高负载的包封效率,高达 55%。使用基于透析的体外测定法,这些颗粒通过 Fickian 扩散机制释放药物,导致药物在大约 6 小时内逐渐释放。这些纳米颗粒显示出作为药物传递系统的潜力,但是需要进行关于它们的抗炎作用、毒性和功效的研究,以确认它们作为药物传递候选物的适用性。

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