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用于可控药物递送的化学表面可调溶解度参数——以负载R6G模型药物的空心PAA包覆磁铁矿纳米颗粒为例及展望

Chemically Surface Tunable Solubility Parameter for Controllable Drug Delivery-An Example and Perspective from Hollow PAA-Coated Magnetite Nanoparticles with R6G Model Drug.

作者信息

He Quanguo, Liu Jun, Liang Jing, Liu Xiaopeng, Tuo Du, Li Wen

机构信息

School of Life Science and Chemistry, Hunan University of Technology, Zhuzhou 412007, China.

出版信息

Materials (Basel). 2018 Feb 6;11(2):247. doi: 10.3390/ma11020247.

DOI:10.3390/ma11020247
PMID:29415453
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5848944/
Abstract

Solubility parameter-dependent drug releasing property is essential in practical drug delivery systems (DDS), and how to combine magnetic nanoparticles(NPs) and suitable polymer coating towards DDS is always a crucial and valuable challenge in biomedical application. Herein, a controllable drug delivery model with a surface having a chemically tunable solubility parameter is presented using hollow magnetite/polyacrylic acid (Fe₃O₄/PAA) nanocomposites as nanocarrier towards DDS. This composite is prepared by simply coating the modified hollow Fe₃O₄ with PAA. The coating amount of PAA onto the surface of Fe₃O₄ (measured by TGA) is about 40% (/). Then, Rhodamine 6G (R6G) is selected as model drug in drug delivery experiment. The efficiency of drug loading and drug release of these Fe₃O₄/PAA nanocarriers are evaluated under various temperature, solvent and pH values. As a result, the best drug releasing rate was achieved as 93.0% in pH = 7.4 PBS solution after 14 h. The releasing efficiency is 86.5% in acidic condition, while a lower releasing rate (30.0%) is obtained in aqueous solution, as different forms (polyacrylic acid and polyacrylate) of PAA present different solubility parameters, causing different salt and acid effects in various solvents, swelling property of PAA, and binding force between PAA and R6G. Therefore, by changing the solubility parameter of coating polymers, the drug delivery properties could be effectively tuned. These findings prove that the DDS based on magnetic particle cores and polymer encapsulation could efficiently regulate the drug delivery properties by tuning surface solubility parameter in potential cancer targeting and therapy.

摘要

在实际的药物递送系统(DDS)中,溶解度参数依赖性药物释放特性至关重要,而如何将磁性纳米颗粒(NPs)与合适的聚合物涂层结合用于DDS,在生物医学应用中始终是一个关键且有价值的挑战。在此,提出了一种可控药物递送模型,该模型使用中空磁铁矿/聚丙烯酸(Fe₃O₄/PAA)纳米复合材料作为DDS的纳米载体,其表面具有化学可调的溶解度参数。这种复合材料是通过简单地用PAA包覆改性的中空Fe₃O₄制备而成。PAA在Fe₃O₄表面的包覆量(通过热重分析测量)约为40%(/)。然后,在药物递送实验中选择罗丹明6G(R6G)作为模型药物。在各种温度、溶剂和pH值下评估这些Fe₃O₄/PAA纳米载体的药物负载效率和药物释放效率。结果,在pH = 7.4的PBS溶液中14小时后,最佳药物释放率达到93.0%。在酸性条件下释放效率为86.5%,而在水溶液中释放率较低(30.0%),因为PAA的不同形式(聚丙烯酸和聚丙烯酸盐)具有不同的溶解度参数,在各种溶剂中会引起不同的盐和酸效应、PAA的溶胀特性以及PAA与R6G之间的结合力。因此,通过改变涂层聚合物的溶解度参数,可以有效地调节药物递送特性。这些发现证明,基于磁性颗粒核心和聚合物封装的DDS在潜在的癌症靶向和治疗中可以通过调节表面溶解度参数有效地调节药物递送特性。

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