Key Laboratory for Applied Technology of Sophisticated Analytical Instruments of Shandong Province, Shandong Analysis and Test Center, Qilu University of Technology (Shandong Academy of Sciences), Jinan, 250014, China.
Key Laboratory for Natural Active Pharmaceutical Constituents Research in Universities of Shandong Province, School of Pharmaceutical Sciences, Qilu University of Technology (Shandong Academy of Sciences), Jinan, 250014, China.
Anal Bioanal Chem. 2024 Dec;416(29):6869-6877. doi: 10.1007/s00216-024-05584-3. Epub 2024 Oct 14.
Berberine (BR), an alkaloid isolated from the Chinese traditional medicine Coptidis rhizoma, exhibits therapeutic effects on several diseases including bacterial infections, diabetes, and hyperlipidemia, but the oral availability is poor. In this work, we prepared the chitosan microneedle array-loaded BR (BR-CS MNAs) to transdermally deliver BR, and the spatial distribution of BR in heterogeneous skin tissues was analyzed and imaged by matrix-assisted laser desorption ionization mass spectrometry imaging (MALDI-MSI). Some endogenous phospholipids with specific spatial distribution were used to differentiate the epidermis and dermis regions of the skin. The results showed that BR was effectively delivered and could permeate to both epidermis and dermis regions of the skin. This demonstrated the feasibility of MALDI-MSI to evaluate the transdermal delivery efficiency of microneedle arrays and suggested BR could be transdermally delivered by CS MNAs.
小檗碱（BR）是从中国传统中药黄连中分离得到的一种生物碱，对细菌感染、糖尿病和高血脂等多种疾病均具有治疗作用，但口服生物利用度较差。本工作制备了载有 BR 的壳聚糖微针阵列（BR-CS MNAs）以经皮递送 BR，并通过基质辅助激光解吸电离质谱成像（MALDI-MSI）分析和成像来研究 BR 在异质皮肤组织中的空间分布。使用具有特定空间分布的一些内源性磷脂来区分皮肤的表皮和真皮区域。结果表明，BR 能够有效地递送到皮肤的表皮和真皮区域并渗透进入其中。这证明了 MALDI-MSI 可用于评估微针阵列的经皮递送效率，并且提示 BR 可以通过 CS MNAs 经皮递送到体内。
