TY - JOUR
T1 - Glycyrrhizin micellar nanocarriers for topical delivery of baicalin to the hair follicles
T2 - A targeted approach tailored for alopecia treatment
AU - Zeng, Quanfu
AU - Wang, Zhuxian
AU - Zhu, Zhaoming
AU - Hu, Yi
AU - Wang, Yuan
AU - Xue, Yaqi
AU - Wu, Yufan
AU - Guo, Yinglin
AU - Liang, Peiyi
AU - Chen, Hongkai
AU - Zheng, Zeying
AU - Shen, Chunyan
AU - Jiang, Cuiping
AU - Zhu, Hongxia
AU - Shen, Qun
AU - Yi, Yankui
AU - Li, Hui
AU - Yang, Zhijun
AU - Liu, Li
AU - Liu, Qiang
N1 - Publisher Copyright:
© 2022 Elsevier B.V. All rights reserved.
PY - 2022/9/25
Y1 - 2022/9/25
N2 - Alopecia affected approximately 16.6% of all people in China, however, treatment options remain limited due to the side effects. Plant bioactive compound baicalin (BC) possesses hair growth-promotion activity, but poor water solubility and unsuitable log P value restrict its topical application, and natural Glycyrrhizin (GL) can exactly overcome these drawbacks. Here, BC was encapsulated in GL to form GL-BC micelles for alopecia treatment. Simultaneously, tween 80 (TW) as carriers was incorporated in the GL-BC to form GL-TW-BC micelles. The topical penetration, penetration pathways, cellular uptake and the underlying mechanisms behind the hair loss reconstruction of the GL micelles were investigated. We found the optimal GL-BC and GL-TW-BC formulations significantly improved the penetration and accumulation of BC in the porcine skin predominantly through the hair follicles pathways without causing skin irritation, which resulted in a targeted treatment. The proliferation of human dermal papilla cells (hDPCs) and effective cellular uptake was also enhanced. Moreover, the activation of the Wnt/β-catenin pathway, up-expression of vascular endothelial growth factor (VEGF), α-melanocyte-stimulating hormone (α-MSH) and interleukin-10 (IL-10) were the mechanisms of micelles for the hair recovery. Interestingly, GL and BC exhibited a synergistic treatment of alopecia. Collectively, GL-BC and GL-TW-BC can be used as promising approaches for the treatment of alopecia.
AB - Alopecia affected approximately 16.6% of all people in China, however, treatment options remain limited due to the side effects. Plant bioactive compound baicalin (BC) possesses hair growth-promotion activity, but poor water solubility and unsuitable log P value restrict its topical application, and natural Glycyrrhizin (GL) can exactly overcome these drawbacks. Here, BC was encapsulated in GL to form GL-BC micelles for alopecia treatment. Simultaneously, tween 80 (TW) as carriers was incorporated in the GL-BC to form GL-TW-BC micelles. The topical penetration, penetration pathways, cellular uptake and the underlying mechanisms behind the hair loss reconstruction of the GL micelles were investigated. We found the optimal GL-BC and GL-TW-BC formulations significantly improved the penetration and accumulation of BC in the porcine skin predominantly through the hair follicles pathways without causing skin irritation, which resulted in a targeted treatment. The proliferation of human dermal papilla cells (hDPCs) and effective cellular uptake was also enhanced. Moreover, the activation of the Wnt/β-catenin pathway, up-expression of vascular endothelial growth factor (VEGF), α-melanocyte-stimulating hormone (α-MSH) and interleukin-10 (IL-10) were the mechanisms of micelles for the hair recovery. Interestingly, GL and BC exhibited a synergistic treatment of alopecia. Collectively, GL-BC and GL-TW-BC can be used as promising approaches for the treatment of alopecia.
KW - Alopecia
KW - Baicalin
KW - Glycyrrhizin micelles
KW - Hair follicles
KW - Wnt/β-catenin pathway
UR - http://www.scopus.com/inward/record.url?scp=85136679597&partnerID=8YFLogxK
U2 - 10.1016/j.ijpharm.2022.122109
DO - 10.1016/j.ijpharm.2022.122109
M3 - Journal article
C2 - 35973589
AN - SCOPUS:85136679597
SN - 0378-5173
VL - 625
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
M1 - 122109
ER -