Abstract：
Liposomes as drug-delivery systems have been researched and applied in multiple scientific reports and introduced as patented products with interesting therapeutic properties. Despite various advantages, this drug carrier faces major difficulties in its innate stability, cancer cell specificity, and control over the release of hydrophobic drugs, particularly quercetin, a naturally derived drug that carries many desirable characteristics for anticancer treatment. To improve the effectiveness of liposomes to deliver quercetin by tackling and mitigating the mentioned hurdles, we developed a strategy to establish the ability to passively target cancerous cells, as well as to increase the bioavailability of loaded drugs by incorporating poly(ethylene glycol), gelatin, and folic acid moieties to modify the liposomal system\'s surface. This research developed a chemically synthesized gelatin, poly(ethylene glycol), and folic acid as a single polymer to coat drug-loaded liposome systems. Liposomes were coated with gelatin-poly(ethylene glycol)-folic acid by electrostatic interaction, characterized by their size, morphology, ζ potential, drug loading efficiency, infrared structures, differential scanning calorimetry spectra, and drug-releasing profiles, and then evaluated for their cytotoxicity to MCF-7 breast cancer cells, as well as cellular uptake, analyzed by confocal imaging to further elaborate on the in vitro behavior of the coated liposome. The results indicated an unusual change in size with increased coating materials, followed by increased colloidal stability, ζ potential, and improved cytotoxicity to cancer cells, as shown by the cellular viability test with MCF-7. Cellular uptake also confirmed these results, providing data for the effects of biopolymer coating, while confirming that folic acid can increase the uptake of liposome by cancer cells. In consideration of such results, the modified gelatin-poly(ethylene glycol)-folic acid-coated liposome can be a potential system in delivering the assigned anticancer compound. This modified biopolymer showed excellent properties as a coating material and should be considered for further practical applications in the future.
摘要：
脂质体作为药物递送系统已经在多个科学报告中被研究和应用,并且作为具有令人感兴趣的治疗特性的专利产品被引入。尽管有各种优势，这种药物载体在其先天稳定性方面面临重大困难，癌细胞特异性，控制疏水性药物的释放，尤其是槲皮素,一种天然来源的药物，具有许多抗癌治疗所需的特性。通过解决和减轻上述障碍来提高脂质体递送槲皮素的有效性，我们开发了一种策略来建立被动靶向癌细胞的能力，以及通过掺入聚（乙二醇）来增加装载药物的生物利用度，明胶,和叶酸部分来修饰脂质体系统的表面。这项研究开发了一种化学合成的明胶，聚(乙二醇)，和叶酸作为单一聚合物来包被载药脂质体系统。脂质体用明胶-聚（乙二醇）-叶酸通过静电相互作用包被，以它们的大小为特征，形态学,ζ电位,药物装载效率，红外结构，差示扫描量热法光谱，和药物释放曲线，然后评估它们对MCF-7乳腺癌细胞的细胞毒性，以及细胞摄取，共聚焦成像分析,进一步阐述包被脂质体的体外行为。结果表明，随着涂层材料的增加，尺寸发生了不寻常的变化，随后增加了胶体稳定性，ζ电位,并改善对癌细胞的细胞毒性，如用MCF-7的细胞活力试验所示。细胞摄取也证实了这些结果，提供生物聚合物涂层效果的数据，同时证实叶酸可以增加癌细胞对脂质体的摄取。考虑到这些结果，修饰的明胶-聚(乙二醇)-叶酸包被的脂质体可以是递送指定的抗癌化合物的潜在系统。这种改性的生物聚合物作为涂层材料显示出优异的性能，应考虑将来的进一步实际应用。
