Weerapol Yotsanan, Manmuan Suwisit, Chuenbarn Tiraniti, Limmatvapirat Sontaya, Tubtimsri Sukannika
Faculty of Pharmaceutical Sciences, Burapha University, Chonburi 20131, Thailand.
Department of Industrial Pharmacy, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Pharmaceutics. 2023 Nov 16;15(11):2631. doi: 10.3390/pharmaceutics15112631.
Among natural sources, guava leaf oil (GLO) has emerged as a potential anticancer agent. However, its limited water solubility poses a significant challenge for its use. Oil-in-water nanoemulsions are used to address the limitation of water solubility of GLO prior to its incorporation into orodipersible films. Nanoemulsions containing GLO:virgin coconut oil (VCO) at a ratio of 50:50 to 70:30 presented a small droplet size of approximately 50 nm and a relatively low zeta potential. GLO:VCO at a ratio of 70:30 was selected for incorporation into sodium alginate film at various concentrations ranging from 1% to 30% /. Tensile strength and elongation at break relied on the concentration of nanoemulsions as well as the internal structure of films. Fourier transform infrared spectroscopy revealed that GLO was compatible with sodium alginate. Film containing 2% / of nanoemulsions (2G_ODF) exhibited effective in vitro antioral cancer activity, with an IC of 62.49 ± 6.22 mg/mL; furthermore, its anticancer activity showed no significant difference after storage at 25 °C for 1 year. Moreover, 2G_ODF at IC arrested colony formation and cell invasion. There is also evidence that cell death occurred via apoptosis, as indicated by nuclear fragmentation and positive Annexin-V staining. These findings highlight the potential of orodispersible films containing GLO nanoemulsions as a prospective oral anticancer agent.
在天然来源中,番石榴叶油(GLO)已成为一种潜在的抗癌剂。然而,其有限的水溶性对其使用构成了重大挑战。在将GLO掺入口腔崩解膜之前,水包油纳米乳液被用于解决其水溶性的限制问题。含有比例为50:50至70:30的GLO:初榨椰子油(VCO)的纳米乳液呈现出约50nm的小液滴尺寸和相对较低的zeta电位。选择比例为70:30的GLO:VCO以1%至30%/的各种浓度掺入海藻酸钠膜中。拉伸强度和断裂伸长率取决于纳米乳液的浓度以及膜的内部结构。傅里叶变换红外光谱表明GLO与海藻酸钠相容。含有2%/纳米乳液的膜(2G_ODF)表现出有效的体外抗口腔癌活性,IC为62.49±6.22mg/mL;此外,在25℃储存1年后其抗癌活性无显著差异。此外,IC浓度下的2G_ODF抑制了集落形成和细胞侵袭。也有证据表明细胞死亡是通过凋亡发生的,如核碎片化和膜联蛋白-V染色阳性所示。这些发现突出了含有GLO纳米乳液的口腔崩解膜作为一种潜在的口服抗癌剂的潜力。