负载香芹酚的植物甾醇体促进伤口愈合的研究：分子对接、制剂学、基于设计实验的优化、以及体内外评价。
Carvacrol-Loaded Phytosomes for Enhanced Wound Healing: Molecular Docking, Formulation, DoE-Aided Optimization, and in vitro/in vivo Evaluation.
机构信息
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Horus University, New Damietta, 34518, Egypt.
出版信息
Int J Nanomedicine. 2023 Oct 12;18:5749-5780. doi: 10.2147/IJN.S421617. eCollection 2023.
BACKGROUND
Despite recent advances in wound healing products, phytochemicals have been considered promising and attractive alternatives. Carvacrol (CAR), a natural phenolic compound, has been reported to be effective in wound healing.
PURPOSE
This work endeavored to develop novel CAR-loaded phytosomes for the enhancement of the wound healing process.
METHODS
Molecular docking was performed to compare the affinities of the different types of phospholipids to CAR. Phytosomes were prepared by three methods (thin-film hydration, cosolvency, and salting out) using Lipoid S100 and Phospholipon 90H with three levels of saturation percent (0%, 50%, and 100%), and three levels of phospholipid molar percent (66.67%, 75%, and 80%). The optimization was performed using Design Expert where particle size, polydispersity index, and zeta potential were chosen as dependent variables. The optimized formula (F1) was further investigated regarding entrapment efficiency, TEM, H-NMR, FT-IR, DSC, X-RD, in vitro release, ex vivo permeation, and stability. Furthermore, it was incorporated into a hydrogel formulation, and an in vivo study was conducted to investigate the wound-healing properties of F1.
RESULTS
F1 was chosen as the optimized formula prepared via the thin-film hydration method with a saturation percent and a phospholipid molar percent of zero and 66.67, respectively. TEM revealed the spherical shape of phytosomal vesicles with uniform size, while the results of H-NMR, FT-IR, DSC, and X-RD confirmed the formation of the phytosomal complex. F1 demonstrated a higher in vitro release and a slower permeation than free CAR. The wound area of F1-treated animals showed a marked reduction associated with a high degree of collagen fiber deposition and enhanced cellular proliferation.
CONCLUSION
F1 can be considered as a promising remedy for the enhancement of wound healing and hence it would be hoped to undergo further investigation.
背景
尽管近年来在伤口愈合产品方面取得了进展，但植物化学物质仍被认为是有前途和有吸引力的替代品。香芹酚 (CAR) 是一种天然酚类化合物，已被证明在伤口愈合方面有效。
目的
本工作旨在开发新型 CAR 负载的植物甾醇体以增强伤口愈合过程。
方法
进行分子对接以比较不同类型的磷脂与 CAR 的亲和力。使用 Lipoid S100 和 Phospholipon 90H 通过三种方法（薄膜水化、共溶剂和盐析）制备植物甾醇体，并使用三种饱和度百分比（0%、50%和 100%）和三种磷脂摩尔百分比（66.67%、75%和 80%）。使用 Design Expert 进行优化，其中选择粒径、多分散指数和 Zeta 电位作为因变量。进一步研究了优化配方 (F1) 的包封效率、TEM、H-NMR、FT-IR、DSC、X-RD、体外释放、离体渗透和稳定性。此外，它被纳入水凝胶配方中，并进行了体内研究以研究 F1 的伤口愈合特性。
结果
选择 F1 作为通过薄膜水化法制备的优化配方，饱和度百分比和磷脂摩尔百分比分别为零和 66.67。TEM 显示了植物甾醇体囊泡的球形形状，具有均匀的大小，而 H-NMR、FT-IR、DSC 和 X-RD 的结果证实了植物甾醇体复合物的形成。F1 显示出比游离 CAR 更高的体外释放和更慢的渗透。F1 处理动物的伤口面积明显减少，伴随着胶原纤维沉积程度高和细胞增殖增强。
结论
F1 可以被认为是增强伤口愈合的有前途的治疗方法，因此希望进一步研究。
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