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甘露糖偶联姜黄素壳聚糖纳米粒:抗杜氏利什曼原虫的疗效和毒性评估。

Mannose-conjugated curcumin-chitosan nanoparticles: Efficacy and toxicity assessments against Leishmania donovani.

机构信息

Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, Uttar Pradesh, India; Department of Pharmaceutics, SVKM's Dr. Bhanuben Nanavati College of Pharmacy, Mithibai College Campus, Vile Parle, Mumbai, Maharashtra, India.

Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, Uttar Pradesh, India.

出版信息

Int J Biol Macromol. 2018 May;111:109-120. doi: 10.1016/j.ijbiomac.2017.12.143. Epub 2018 Jan 4.

Abstract

Aim was to fabricate and optimize CUR-loaded mannose-functionalized chitosan nanoparticles (Cur-MCN) which overcome the limitations of drugs to reach the intracellular locations and to establish its therapeutic potential in visceral leishmaniasis by targeting of CUR to macrophages. Cur-MCN were developed by mannose-conjugated chitosan and have been tested for their efficacy and toxicit. In vivo antileishmanial activity in hamsters has shown significantly greater suppression of parasite replication in the spleen with Cur-MCN than unconjugated chitosan nanoparticles. The in vitro cytotoxicity study against the J774A.1 cell line demonstrated its comparative non-toxicity towards the macrophage cells. The potential of Cur-MCN was also confirmed by minimal observed cytotoxicity in our in vivo studies.

摘要

目的是制备和优化 CUR 负载的甘露糖功能化壳聚糖纳米粒子(Cur-MCN),以克服药物到达细胞内位置的限制,并通过将 CUR 靶向巨噬细胞来建立其在内脏利什曼病中的治疗潜力。Cur-MCN 是通过甘露糖缀合壳聚糖开发的,并已对其功效和毒性进行了测试。在仓鼠体内抗利什曼原虫活性研究中,Cur-MCN 比未缀合壳聚糖纳米粒子更能显著抑制脾内寄生虫复制。对 J774A.1 细胞系的体外细胞毒性研究表明,它对巨噬细胞相对无毒。Cur-MCN 的潜力也通过我们体内研究中观察到的最小细胞毒性得到了证实。

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