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介孔硅纳米粒子的制备用于在局部应用中在痤疮部位释放甘草多糖。

Fabrication of mesoporous silica nanoparticles for releasable delivery of licorice polysaccharide at the acne site in topical application.

机构信息

College of Pharmaceutical Sciences, Soochow University, Suzhou 215021, PR China.

School of Medicine, Jiangsu University, Zhenjiang 212013, PR China.

出版信息

Carbohydr Polym. 2024 Sep 1;339:122250. doi: 10.1016/j.carbpol.2024.122250. Epub 2024 May 9.

DOI:10.1016/j.carbpol.2024.122250
PMID:38823917
Abstract

Glycyrrhizae Radix et rhizome/licorice is a precious herb in traditional Chinese medicine (TCM). TCM's polysaccharides are medicinally active. But herbal polysaccharides pose some limitations for topical applications. Therefore, this study aimed to utilize licorice polysaccharide via mesoporous silica nanoparticles (MSN) for anti-acne efficacy in topical delivery. The polysaccharide (GGP) was extracted with a 10 % NaOH solution. Chemical characterization suggested that GGP possesses an Mw of 267.9 kDa, comprised primarily of Glc (54.1 %) and Ara (19.12 %), and probably 1,4-linked Glc as a backbone. Then, MSN and amino-functionalized MSN were synthesized, GGP entrapped, and coated with polydopamine (PDA) to produce nanoparticle cargo. The resulted product exhibited 76 % entrapment efficiency and an in vitro release of 89 % at pH 5, which is usually an acne-prone skin's pH. Moreover, it significantly increased Sebocytes' cellular uptake. GGP effectively acted as an anti-acne agent and preserved its efficacy in synthesized nanoparticles. In vivo, the results showed that a 20 % gel of MSN-NH-GGP@PDA could mediate an inflammatory response via inhibiting pro-inflammatory cytokines and regulating anti-inflammatory cytokines. The MSN-NH-GGP@PDA inhibited TLR2-activated-MAPK and NF-κB pathway triggered by heat-killed P. acnes. In conclusion, fabricated MSN entrapped GGP for biomimetic anti-acne efficacy in topical application.

摘要

甘草根茎是中药(TCM)中的一种珍贵草药。TCM 的多糖具有药用活性。但是,草药多糖在局部应用方面存在一些局限性。因此,本研究旨在利用甘草多糖通过介孔硅纳米粒子(MSN)进行局部递送的抗痤疮功效。多糖(GGP)用 10%的 NaOH 溶液提取。化学特性表明 GGP 的Mw 为 267.9 kDa,主要由 Glc(54.1%)和 Ara(19.12%)组成,可能还有 1,4 连接的 Glc 作为主链。然后,合成了 MSN 和氨基功能化的 MSN,包封了 GGP,并涂有聚多巴胺(PDA)以产生纳米颗粒载体。所得产物的包封效率为 76%,在 pH 5 下的体外释放率为 89%,这通常是容易长粉刺的皮肤的 pH 值。此外,它显著增加了皮脂腺细胞的摄取。GGP 可有效作为抗痤疮剂,并在合成的纳米颗粒中保留其功效。在体内,结果表明,20%的 MSN-NH-GGP@PDA 凝胶可通过抑制促炎细胞因子和调节抗炎细胞因子来介导炎症反应。MSN-NH-GGP@PDA 抑制了热灭活 P. acnes 激活的 TLR2 激活的 MAPK 和 NF-κB 途径。总之,合成的 MSN 包封 GGP 用于仿生抗痤疮功效的局部应用。

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