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壳寡糖与泊洛沙姆 F-68 制备新型载水溶性姜黄素聚合物胶束及其初步生物活性评价

Preparation and Primary Bioactivity Evaluation of Novel Water-Soluble Curcumin-Loaded Polymeric Micelles Fabricated with Chitooligosaccharides and Pluronic F-68.

作者信息

Ingrungruengluet Pattarachat, Wang Dingfu, Li Xin, Yang Cheng, Waiprib Yaowapha, Li Chunxia

机构信息

Shandong Key Laboratory of Glycoscience and Glycotechnology, Key Laboratory of Marine Drugs of Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.

Department of Fishery Products, Faculty of Fisheries, Kasetsart University, Bangkok 10900, Thailand.

出版信息

Pharmaceutics. 2023 Oct 20;15(10):2497. doi: 10.3390/pharmaceutics15102497.

DOI:10.3390/pharmaceutics15102497
PMID:37896257
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10609826/
Abstract

Curcumin (CU) is a bioactive compound extracted from turmeric and has various advantages. However, the benefit of CU is limited by its low water solubility (11 ng/mL). This research aimed to fabricate a water-soluble CU nano-formulation with chitooligosaccharides (COS) and pluronic F-68 (PF) utilizing the polymeric micelle method. The optimized curcumin-loaded chitooligosaccharides/pluronic F-68 micelles (COSPFCU) exhibited high encapsulation efficiency and loading capacity (75.57 ± 2.35% and 10.32 ± 0.59%, respectively). The hydrodynamic diameter of lyophilized COSPFCU was 73.89 ± 11.69 nm with a polydispersity index below 0.3. The COSPFCU could be completely redispersed in water and showed high DPPH scavenging ability. Meanwhile, COSPFCU could significantly reduce the cytotoxicity of the RAW 264.7 cells compared to native CU. Furthermore, COSPFCU improved the inhibition of NO release activity at 72.83 ± 2.37% but 33.20 ± 3.41% for the CU, with a low cytotoxicity concentration in the RAW 264.7 cells.

摘要

姜黄素(CU)是从姜黄中提取的一种生物活性化合物,具有多种优点。然而,CU的益处因其低水溶性(11 ng/mL)而受到限制。本研究旨在利用聚合物胶束法制备一种含有壳寡糖(COS)和普朗尼克F-68(PF)的水溶性CU纳米制剂。优化后的载姜黄素壳寡糖/普朗尼克F-68胶束(COSPFCU)表现出高包封率和载药量(分别为75.57±2.35%和10.32±0.59%)。冻干的COSPFCU的流体动力学直径为73.89±11.69 nm,多分散指数低于0.3。COSPFCU可完全重新分散于水中,并表现出高DPPH清除能力。同时,与天然CU相比,COSPFCU可显著降低RAW 264.7细胞的细胞毒性。此外,COSPFCU提高了对NO释放活性的抑制作用,抑制率为72.83±2.37%,而CU为33.20±3.41%,在RAW 264.7细胞中的细胞毒性浓度较低。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2506/10609826/968795e2debc/pharmaceutics-15-02497-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2506/10609826/295c35e66ab2/pharmaceutics-15-02497-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2506/10609826/964fda837ada/pharmaceutics-15-02497-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2506/10609826/1f230bf8706d/pharmaceutics-15-02497-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2506/10609826/b186e4145d0a/pharmaceutics-15-02497-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2506/10609826/968795e2debc/pharmaceutics-15-02497-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2506/10609826/295c35e66ab2/pharmaceutics-15-02497-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2506/10609826/964fda837ada/pharmaceutics-15-02497-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2506/10609826/1f230bf8706d/pharmaceutics-15-02497-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2506/10609826/b186e4145d0a/pharmaceutics-15-02497-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2506/10609826/968795e2debc/pharmaceutics-15-02497-g005.jpg

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