姜黄素负载三嵌段共聚胶束的抗氧化反应及生物相容性

IF 2.8 4区 医学 Q2 TOXICOLOGY Toxicology Mechanisms and Methods Pub Date : 2017-01-02 DOI:10.1080/15376516.2016.1253811
V. Tzankova, Cvetelina Gorinova, M. Kondeva-Burdina, R. Simeonova, Stanislav Philipov, S. Konstantinov, P. Petrov, Dimitar Galabov, K. Yoncheva
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引用次数: 6

摘要

摘要为了评估阳离子胶束的安全性,基于聚(甲基丙烯酸二甲氨基乙酯)-聚(e-己内酯)-聚甲基丙烯酸二乙氨基乙酯三嵌段共聚物(PDMAEMA9–PCL70–PDMAEMA 9),考察了空(PM)和姜黄素负载胶束(PM-Crc)对体外非酶诱导的脂质过氧化(LPO)的影响,研究了体内重复腹腔给药后某些器官的溶血活性和形态学变化。为了诱导LPO,将大鼠肝微粒体与硫酸铁和抗坏血酸(Fe2+/AA)溶液一起孵育。空PM的影响(40和100 μg/ml)、PM Curc和游离姜黄素(均为3.48和8.7 μg姜黄素/ml)在20 最小孵育时间。在非酶诱导LPO模型中,与Fe2+/AA诱导的LPO组相比,所有浓度的研究物质都显著降低了丙二醛(MDA)的形成。根据结果可以得出结论,单独的姜黄素和负载在PM中的姜黄素具有显著的抗氧化活性。在生物相容性安全性研究中,聚合物载体的平均溶血指数小于2%,表明它是非溶血性的。用负载姜黄素的PM在体内处理的Wistar大鼠的器官组织的总体外观与对照组相似,因此在重复处理14天后没有显示出明显的毒性。
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Antioxidant response and biocompatibility of curcumin-loaded triblock copolymeric micelles
Abstract To evaluate the safety profile of cationic micelles, based on triblock copolymer poly(dimethylaminoethyl methacrylate)–poly(e-caprolactone)–poly(dimethylaminoethyl methacrylate) (PDMAEMA9– PCL70–PDMAEMA9), the effects of empty (PM) and curcumin loaded micelles (PM-Curc) on nonenzyme induced lipid peroxidation (LPO) in vitro, hemolytic activity and morphological changes in some organs after repeated intraperitoneal administration in vivo were studied. To induce LPO, rat liver microsomes were incubated with a solution of iron sulfate and ascorbinic acid (Fe2+/AA). The effect of empty PM (40 and 100 μg/ml), PM-Curc and free curcumin (both at 3.48 and 8.7 μg curcumin/ml) was assessed at 20 min incubation time. In the non-enzyme induced LPO model, the investigated substances at all concentrations significantly decreased the formation of malondialdehyde (MDA), compared to the Fe2+/AA induced LPO group. According to the results it can be concluded that curcumin alone and loaded in PM, exert significant antioxidant activity. In the biocompatibility safety studies, the mean hemolytic index for polymeric carrier was less than 2%, indicating it was non-hemolytic. The general appearance of the organ tissues from Wistar rats, treated in vivo with curcumin loaded PM was similar to that of controls, thus showing no apparent toxicity after repeated 14-days treatment.
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来源期刊
自引率
3.10%
发文量
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期刊介绍: Toxicology Mechanisms and Methods is a peer-reviewed journal whose aim is twofold. Firstly, the journal contains original research on subjects dealing with the mechanisms by which foreign chemicals cause toxic tissue injury. Chemical substances of interest include industrial compounds, environmental pollutants, hazardous wastes, drugs, pesticides, and chemical warfare agents. The scope of the journal spans from molecular and cellular mechanisms of action to the consideration of mechanistic evidence in establishing regulatory policy. Secondly, the journal addresses aspects of the development, validation, and application of new and existing laboratory methods, techniques, and equipment. A variety of research methods are discussed, including: In vivo studies with standard and alternative species In vitro studies and alternative methodologies Molecular, biochemical, and cellular techniques Pharmacokinetics and pharmacodynamics Mathematical modeling and computer programs Forensic analyses Risk assessment Data collection and analysis.
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