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利用皮肤角朊脂质体增强渗透和传递促进甘草查尔酮 A 的经皮给药

Mechanisms of Penetration Enhancement and Transport Utilizing Skin Keratine Liposomes for the Topical Delivery of Licochalcone A.

机构信息

School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, China.

Department of Pharmacy and Nanfang Hospital, Southern Medical University, Guangzhou 510515, China.

出版信息

Molecules. 2022 Apr 13;27(8):2504. doi: 10.3390/molecules27082504.

DOI:10.3390/molecules27082504
PMID:35458701
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9029797/
Abstract

Keratin liposomes have emerged as a useful topical drug delivery system given theirenhanced ability to penetrate the skin, making them ideal as topical drug vehicles. However, the mechanisms of the drug penetration enhancement of keratin liposomes have not been clearly elucidated. Therefore, licochalcone A(LA)-loaded skin keratin liposomes (LALs) were prepared to investigate their mechanisms of penetration enhancement on the skin and inB16F10 cells. Skin deposition studies, differential scanning calorimetry (DSC), attenuated total reflection-Fourier Transform Infrared Spectroscopy (ATR-FTIR), and skin distribution and intracellular distribution studies were carried out to demonstrate the drug enhancement mechanisms of LALs. We found that the optimal application of LALs enhanced drug permeation via alterations in the components, structure, and thermodynamic properties of the stratum corneum (SC), that is, by enhancing the lipid fluidization, altering the skin keratin, and changing the thermodynamic properties of the SC. Moreover, hair follicles were the main penetration pathways for the LA delivery, which occurred in a time-dependent manner. In the B16F10 cells, the skin keratin liposomes effectively delivered LA into the cytoplasm without cytotoxicity. Thus, LAL nanoparticles are promising topical drug delivery systems for pharmaceutical and cosmetic applications.

摘要

角蛋白脂质体作为一种有用的局部药物传递系统，由于其增强的穿透皮肤的能力而受到关注，使其成为理想的局部药物载体。然而，角蛋白脂质体增强药物渗透的机制尚未得到明确阐明。因此，制备了载有甘草查尔酮 A（LA）的皮肤角蛋白脂质体（LAL），以研究其在皮肤和 B16F10 细胞中的渗透增强机制。进行了皮肤沉积研究、差示扫描量热法（DSC）、衰减全反射傅里叶变换红外光谱（ATR-FTIR）以及皮肤分布和细胞内分布研究，以证明 LAL 的药物增强机制。我们发现，LAL 的最佳应用通过改变角质层（SC）的成分、结构和热力学性质来增强药物渗透，即通过增强脂质流动性、改变皮肤角蛋白和改变 SC 的热力学性质。此外，毛囊是 LA 传递的主要渗透途径，其发生具有时间依赖性。在 B16F10 细胞中，皮肤角蛋白脂质体有效地将 LA 递送到细胞质中，没有细胞毒性。因此，LAL 纳米颗粒是用于药物和化妆品应用的有前途的局部药物传递系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/8fc77f180035/molecules-27-02504-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/1d9e9fb35fcf/molecules-27-02504-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/a0fdfd68a02d/molecules-27-02504-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/5732cdeff09e/molecules-27-02504-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/5e105749a4ed/molecules-27-02504-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/fc951f7719d0/molecules-27-02504-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/cb39c3cc4e4f/molecules-27-02504-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/8fc77f180035/molecules-27-02504-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/1d9e9fb35fcf/molecules-27-02504-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/a0fdfd68a02d/molecules-27-02504-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/5732cdeff09e/molecules-27-02504-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/5e105749a4ed/molecules-27-02504-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/fc951f7719d0/molecules-27-02504-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/cb39c3cc4e4f/molecules-27-02504-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/447d/9029797/8fc77f180035/molecules-27-02504-g007.jpg

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