Department of Pharmacology, Faculty of Medicine, Khon Kaen University, Khon Kaen 40002, Thailand.
Graduate School in the Program of Research and Development in Pharmaceuticals, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.
Molecules. 2024 Jun 6;29(11):2695. doi: 10.3390/molecules29112695.
Oleoresin of Roxb. ex G. Don (DA) has been traditionally used for local medicinal applications. Several in vitro studies have indicated its pharmacological potential. However, the low water solubility hinders its use and development for pharmaceutical purposes. The study aimed to (1) formulate oil-in-water (/) Pickering emulsions of DA oleoresin and (2) demonstrate its activities in cancer cells. The Pickering emulsions were formulated using biocompatible carboxylated cellulose nanocrystal (cCNC) as an emulsifier. The optimized emulsion comprised 3% (F1) and 4% (/) (F2) of oleoresin in 1% cCNC and 0.1 M NaCl, which possessed homogeneity and physical stability compared with other formulations with uniform droplet size and low viscosity. The constituent analysis indicated the presence of the biomarker dipterocarpol in both F1 and F2. The pharmacological effects of the two emulsions were demonstrated in vitro against two cancer cell lines, HepG2 and HCT116. Both F1 and F2 suppressed cancer cell viability. The treated cells underwent apoptosis, as demonstrated by distinct nuclear morphological changes in DAPI-stained cells and Annexin V/PI-stained cells detected by flow cytometry. Our study highlights the prospect of Pickering emulsions for oleoresin, emphasizing enhanced stability and potential pharmacological advantages.
罗比侧柏醇树脂（DA）的油树脂在传统上被用于局部药用应用。几项体外研究表明其具有药理学潜力。然而，低水溶性阻碍了其在药物方面的使用和开发。本研究旨在：（1）制备 DA 油树脂的水包油（/）Pickering 乳液；（2）证明其在癌细胞中的活性。Pickering 乳液是使用生物相容性的羧化纤维素纳米晶体（cCNC）作为乳化剂制备的。优化的乳液包含 3%（F1）和 4%（/）（F2）油树脂，在 1%cCNC 和 0.1 M NaCl 中，与其他具有均匀液滴大小和低粘度的制剂相比，具有均一性和物理稳定性。成分分析表明 F1 和 F2 中均存在生物标志物双柏醇。两种乳液在体外对两种癌细胞系 HepG2 和 HCT116 的药理作用进行了证明。F1 和 F2 均抑制癌细胞活力。用 DAPI 染色细胞和流式细胞术检测 Annexin V/PI 染色细胞观察到的明显核形态变化，证明处理后的细胞发生了凋亡。我们的研究强调了 Pickering 乳液在油树脂中的前景，突出了增强的稳定性和潜在的药理优势。
