Background: Orthosiphon stamineus Benth (O.S) is a traditional south-east Asian herb. The extract of O.S is used in the formulation of ethanolic nanolipid vesicle system to have considerable potential for tumour therapeutics. Method: The research objective is to develop and characterise the anticancer and antiangiogenic effect of O.S extract in the form of nano-ethanolic spherosomes (ESP) using phospholipids in melanoma. Spherosomes formulation of O.S was developed using the thin-film re-hydration method and converted to gel using Acrypol 1%. The formulations were subjected to optimisation and physical-chemical characterisations like particle size, surface charge, DSC, FTIR, and TEM. Cytotoxicity of O.S and ESP was studied using an endothelial cell line (EA. hy926). Furthermore, anti-melanoma effect of O.S spherosome gel was studied in albino mice after topical administration. Results: ESP-6 with the ratio of extract (O.S): cholesterol: phospholipid (1: 6: 0.5) showed the highest entrapment efficiency (80.56 ± 0.84%) using ultraviolet spectroscopy. In-vivo permeation/penetration studies revealed deeper absorption of ESP-6 compared to a hydroethanolic gel of O.S. In-vitro and in vivo anti-melanoma studies demonstrated the significant tumour-suppressing effect of ESP-6 on murine melanoma. Percentage inhibition of tumour growth by O.S and ESP-6 at 3000 mg/kg showed to be 63.98 ± 7.86% and 87.76 ± 7.90%, respectively. Conclusion: Spherosome vesicles were developed with a smooth surface. The results demonstrated that O.S extract showed no toxicity when tested on the endothelial cell line. O.S loaded in spherosomes has the potential to lower the growth of melanoma in mice. The spherosomes loaded with O.S do not promote tumour growth or act as antiangiogenetic in melanoma.

中文翻译：

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使用 Orthosiphon stamineus Benth 抑制小鼠肿瘤模型中的黑色素瘤生长。载入乙醇磷脂囊泡（球体）的提取物

背景：Orthosiphon stamineus Benth (OS) 是一种传统的东南亚草本植物。OS 的提取物用于制备乙醇纳米脂质囊泡系统，具有相当大的肿瘤治疗潜力。方法：研究目标是利用磷脂在黑色素瘤中开发和表征纳米乙醇球体 (ESP) 形式的 OS 提取物的抗癌和抗血管生成作用。OS 的球体制剂是使用薄膜再水化方法开发的，并使用 Acrypol 1% 转化为凝胶。对配方进行了优化和物理化学表征，如粒径、表面电荷、DSC、FTIR 和 TEM。使用内皮细胞系 (EA.hy926) 研究了 OS 和 ESP 的细胞毒性。此外，O. 的抗黑色素瘤作用。在局部给药后，在白化小鼠中研究了 S 球体凝胶。结果：ESP-6 与提取物 (OS)：胆固醇：磷脂 (1: 6: 0.5) 的比例使用紫外光谱显示出最高的包封率 (80.56 ± 0.84%)。体内渗透/渗透研究表明，与 OS 的水乙醇凝胶相比，ESP-6 的吸收更深 体外和体内抗黑色素瘤研究证明了 ESP-6 对小鼠黑色素瘤的显着肿瘤抑制作用。OS 和 ESP-6 在 3000 mg/kg 时抑制肿瘤生长的百分比分别为 63.98 ± 7.86% 和 87.76 ± 7.90%。结论：形成了具有光滑表面的球体囊泡。结果表明，在内皮细胞系上测试时，OS 提取物没有显示出毒性。欧。载入球体的 S 有可能降低小鼠黑色素瘤的生长。装载 OS 的球体不会促进肿瘤生长或在黑色素瘤中起到抗血管生成作用。