研究动态
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用于皮肤黑色素瘤治疗的金雀异黄素转移体嵌入局部递送系统:体外和离体评估。

Genistein transfersome-embedded topical delivery system for skin melanoma treatment: in vitro and ex vivo evaluations.

发表日期:2024 Dec
作者: Amira Motawea, Sara N Maria, Doaa N Maria, Monica M Jablonski, Mohamed Moustafa Ibrahim
来源: DRUG DELIVERY

摘要:

皮肤黑色素瘤被认为是最危险的皮肤癌,因为它具有高转移风险、高死亡率和对不同治疗方案的高抵抗力。金雀异黄酮是一种天然异黄酮类化合物,具有已知的化疗活性。不幸的是,由于其水溶性差和过度代谢,其生物利​​用度较低。在当前的研究中,金雀异黄酮被纳入转移体水凝胶中以提高其生物利用度。所制备的转移体制剂的特征在于:颗粒大小;多分散指数; zeta 电位;封装效率;透射电镜;红外光谱;差示扫描量热法; X射线衍射;体外药物释放;粘度;酸碱度; 3D 皮肤黑色素瘤球体的离体抗肿瘤活性以及不同储存温度下的 1 年稳定性研究。优化的配方具有高封装效率和优异的粒径,有利于其渗透皮肤。传递体呈球形,具有持续的药物释放特性。金雀异黄素转移体的抗肿瘤活性评估表明,金雀异黄素是一种有效的化疗剂,当掺入转移体时,其穿过黑色素瘤球体的渗透能力增强。稳定性研究结果证明我们的配方具有较高的物理和化学稳定性。所有这些结果都证明我们的金雀异黄素转移体水凝胶是皮肤黑色素瘤的一种有前途的治疗选择。
Skin melanoma is considered the most dangerous form of skin cancer due to its association with high risk of metastasis, high mortality rate and high resistance to different treatment options. Genistein is a natural isoflavonoid with known chemotherapeutic activity. Unfortunately, it has low bioavailability due to its poor aqueous solubility and excessive metabolism. In the current study, genistein was incorporated into transferosomal hydrogel to improve its bioavailability. The prepared transferosomal formulations were characterized regarding: particle size; polydispersity index; zeta potential; encapsulation efficiency; TEM; FTIR; DSC; XRD; in vitro drug release; viscosity; pH; ex vivo anti-tumor activity on 3D skin melanoma spheroids and 1-year stability study at different storage temperatures. The optimized formulation has high encapsulation efficiency with an excellent particle size that will facilitate its penetration through the skin. The transfersomes have a spherical shape with sustained drug release profile. The anti-tumor activity evaluation of genistein transfersome revealed that genistein is a potent chemotherapeutic agent with enhanced penetration ability through the melanoma spheroids when incorporated into transfersomes. Stability study results demonstrate the high physical and chemical stability of our formulations. All these outcomes provide evidence that our genistein transferosomal hydrogel is a promising treatment option for skin melanoma.