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载有普洱茶提取物的透明质酸-抗利尿激素-聚苯乙烯纳米胶束的制备及性质

Preparation and properties of Pue-loaded HA-ADH-PS nanomicelles.

作者信息

Wang Huiru, Li Yuanyuan, Min Yunpeng, Zhang Hang, Hao Linkun, Zhang Ru, Jiang Yunying, Song Yimin

机构信息

Department of Pharmaceutical Engineering, Qingdao University of Science and Technology, Qingdao P.R. China.

College of Marines Life Science, Ocean University of China, Qingdao, P.R., China.

出版信息

Des Monomers Polym. 2021 Jan 17;24(1):1-12. doi: 10.1080/15685551.2020.1860481.

DOI:10.1080/15685551.2020.1860481
PMID:33536833
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7832032/
Abstract

Puerarin (Pue) is the most abundant isoflavonoid in kudzu root. It has been widely used as a therapeutic agent for the treatment of cardiovascular diseases. However, poor-bioavailability of puerarin is the main obstacle to its widespread clinical applications. In this paper, HA-ADH-PS nanomicelles were prepared by chemical modification, noncovalent modification and etc, and characterized by means of FT-IR, ultraviolet (UV) and thermogravimetric analysis (TG). The encapsulation efficiency and drug loading of Pue-loaded HA-ADH-PS nanomicelles were 45.1% and 19.89% by UV, respectively. It could be observed from the transmission electron microscopy (TEM) images that HA-ADH-PS micelles appeared obvious spherical structure in the water. The particle size of HA-ADH-PS nanomicelles and Pue-loaded HA-ADH-PS nanomicelles were about 136.8 nm and 119.5 nm with a PDI of 0.237 and 0.272, respectively. The fluorescence probe method was used to characterize the critical micelle concentration, the critical micelle concentration (CMC) value of the nanomicells was 0.002 g/L and the results met the requirements and ensured the stability of micelles after dilution. DPPH assay suggested that Pue-loaded HA-ADH-PS nanomicelles had an obvious radical scavenging effect in vitro. MTT test showed that Pue-loaded HA-ADH-PS nanomicelles was non-toxic and had good biocompatibility. Thus, Pue-loaded HA-ADH-PS nanomicelles could be used as a potential drug carrier for puerarin.

摘要

葛根素（Pue）是葛根中含量最为丰富的异黄酮类化合物。它已被广泛用作治疗心血管疾病的药物。然而，葛根素生物利用度差是其广泛临床应用的主要障碍。本文通过化学修饰、非共价修饰等方法制备了HA-ADH-PS纳米胶束，并通过傅里叶变换红外光谱（FT-IR）、紫外光谱（UV）和热重分析（TG）对其进行了表征。通过紫外光谱法测得负载葛根素的HA-ADH-PS纳米胶束的包封率和载药量分别为45.1%和19.89%。从透射电子显微镜（TEM）图像可以观察到，HA-ADH-PS胶束在水中呈现出明显的球形结构。HA-ADH-PS纳米胶束和负载葛根素的HA-ADH-PS纳米胶束的粒径分别约为136.8 nm和119.5 nm，多分散指数（PDI）分别为0.237和0.272。采用荧光探针法表征临界胶束浓度，纳米胶束的临界胶束浓度（CMC）值为0.002 g/L，结果符合要求，确保了胶束稀释后的稳定性。二苯基苦味酰基自由基（DPPH）测定表明，负载葛根素的HA-ADH-PS纳米胶束在体外具有明显的自由基清除作用。MTT试验表明，负载葛根素的HA-ADH-PS纳米胶束无毒且具有良好的生物相容性。因此，负载葛根素的HA-ADH-PS纳米胶束可作为葛根素潜在的药物载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7d2c/7832032/8590f8ff5e0b/TDMP_A_1860481_F0017_OC.jpg
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