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

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, licocha...

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Main Authors: Wenfeng Wu, Zhuxian Wang, Yufan Wu, Huiyi Wu, Tingting Chen, Yaqi Xue, Yuan Wang, Cuiping Jiang, Chunyan Shen, Li Liu, Hongxia Zhu, Qiang Liu
Format: Article
Language:English
Published: MDPI AG 2022-04-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/27/8/2504
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author Wenfeng Wu
Zhuxian Wang
Yufan Wu
Huiyi Wu
Tingting Chen
Yaqi Xue
Yuan Wang
Cuiping Jiang
Chunyan Shen
Li Liu
Hongxia Zhu
Qiang Liu
author_facet Wenfeng Wu
Zhuxian Wang
Yufan Wu
Huiyi Wu
Tingting Chen
Yaqi Xue
Yuan Wang
Cuiping Jiang
Chunyan Shen
Li Liu
Hongxia Zhu
Qiang Liu
author_sort Wenfeng Wu
collection DOAJ
description 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.
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spelling doaj.art-e38d705cd7ea4f4096c9f9dc45fb852e2023-12-03T13:46:36ZengMDPI AGMolecules1420-30492022-04-01278250410.3390/molecules27082504Mechanisms of Penetration Enhancement and Transport Utilizing Skin Keratine Liposomes for the Topical Delivery of Licochalcone AWenfeng Wu0Zhuxian Wang1Yufan Wu2Huiyi Wu3Tingting Chen4Yaqi Xue5Yuan Wang6Cuiping Jiang7Chunyan Shen8Li Liu9Hongxia Zhu10Qiang Liu11School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaDepartment of Pharmacy and Nanfang Hospital, Southern Medical University, Guangzhou 510515, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaIntegrated Hospital of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510315, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaKeratin 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.https://www.mdpi.com/1420-3049/27/8/2504topical drug delivery systemLicochalcone Amechanisms of penetration enhancementlipid nanoparticles
spellingShingle Wenfeng Wu
Zhuxian Wang
Yufan Wu
Huiyi Wu
Tingting Chen
Yaqi Xue
Yuan Wang
Cuiping Jiang
Chunyan Shen
Li Liu
Hongxia Zhu
Qiang Liu
Mechanisms of Penetration Enhancement and Transport Utilizing Skin Keratine Liposomes for the Topical Delivery of Licochalcone A
Molecules
topical drug delivery system
Licochalcone A
mechanisms of penetration enhancement
lipid nanoparticles
title Mechanisms of Penetration Enhancement and Transport Utilizing Skin Keratine Liposomes for the Topical Delivery of Licochalcone A
title_full Mechanisms of Penetration Enhancement and Transport Utilizing Skin Keratine Liposomes for the Topical Delivery of Licochalcone A
title_fullStr Mechanisms of Penetration Enhancement and Transport Utilizing Skin Keratine Liposomes for the Topical Delivery of Licochalcone A
title_full_unstemmed Mechanisms of Penetration Enhancement and Transport Utilizing Skin Keratine Liposomes for the Topical Delivery of Licochalcone A
title_short Mechanisms of Penetration Enhancement and Transport Utilizing Skin Keratine Liposomes for the Topical Delivery of Licochalcone A
title_sort mechanisms of penetration enhancement and transport utilizing skin keratine liposomes for the topical delivery of licochalcone a
topic topical drug delivery system
Licochalcone A
mechanisms of penetration enhancement
lipid nanoparticles
url https://www.mdpi.com/1420-3049/27/8/2504
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