Alkhaldi Muzn, Sehra Tehseen, Sengupta Soma, Keck Cornelia M
Department of Pharmaceutics and Biopharmaceutics, Philipps-Universität Marburg, Robert-Koch-Str. 4, 35037 Marburg, Germany.
Institute of Pharmacy, Faculty of Pharmaceutical and Allied Health Sciences, Lahore College for Women University, Lahore 54000, Pakistan.
Molecules. 2024 Dec 16;29(24):5926. doi: 10.3390/molecules29245926.
The limited water solubility of active compounds remains a significant challenge for efficient dermal drug delivery, particularly for BCS class IV drugs such as curcumin. This study aimed to enhance curcumin's dermal penetration using two strategies: extracellular vesicles (EVs) and plantCrystals derived from soybeans. EVs were isolated using classical methods. However, plantCrystals containing extracellular vesicles (PCEVs) were formed during the preparation of plantCrystals through bead milling. Curcumin was either added after PCEVs were formed, resulting in curcumin-added PCEVs, or added to the soybean dispersion before bead milling, forming curcumin-loaded PCEVs. The formulations were characterized for their physicochemical properties and assessed for dermal penetration efficacy using quantitative dermatokinetic and semi-quantitative ex vivo porcine ear models. The results indicated that curcumin-loaded PCEVs achieved higher penetration efficacy compared to curcumin-added PCEVs and curcumin-loaded EVs, with approximately 1.5-fold and 2.7-fold increases in penetration efficacy, respectively. Additionally, curcumin-loaded PCEVs showed superior penetration depth, while curcumin from the curcumin-loaded EVs remained in the stratum corneum. These findings suggest that the plantCrystals strategy via bead milling offers a more effective approach than the classical EVs strategy for improving the topical delivery of class IV drugs like curcumin.
活性化合物有限的水溶性仍然是高效皮肤给药的重大挑战，尤其是对于姜黄素等BCS IV类药物。本研究旨在通过两种策略提高姜黄素的皮肤渗透性：细胞外囊泡（EVs）和源自大豆的植物晶体。EVs采用经典方法分离。然而，在通过珠磨法制备植物晶体的过程中形成了含有细胞外囊泡的植物晶体（PCEVs）。姜黄素要么在PCEVs形成后添加，得到添加姜黄素的PCEVs，要么在珠磨前添加到大豆分散液中，形成负载姜黄素的PCEVs。对这些制剂的理化性质进行了表征，并使用定量皮肤动力学和半定量离体猪耳模型评估了皮肤渗透效果。结果表明，与添加姜黄素的PCEVs和负载姜黄素的EVs相比，负载姜黄素的PCEVs具有更高的渗透效果，渗透效果分别提高了约1.5倍和2.7倍。此外，负载姜黄素的PCEVs显示出更好的渗透深度，而负载姜黄素的EVs中的姜黄素则保留在角质层中。这些发现表明，通过珠磨法的植物晶体策略比经典的EVs策略提供了一种更有效的方法来改善姜黄素等IV类药物的局部给药。
