a Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine , Nanjing , China.
b Jiangsu Province Academy of Traditional Chinese Medicine , Nanjing , China.
Drug Deliv. 2018 Nov;25(1):1802-1810. doi: 10.1080/10717544.2018.1516006.
The aim of this study is to explore the influence of Ganoderma lucidum-derived polysaccharides (GLP) to coix oil-based microemulsion on pharmaceutical performance and anti-lung cancer treatment. GLP-integrated coix oil-based microemulsion (MEs(PS-GLP)) exhibited a clear spherical shape, small particle size, and good hydrodynamics similar to the coix oil-based microemulsion, but showed a lower zeta potential and a better stability. Fluorescence resonance energy transfer analysis presented that GLP was integrated with microemulsion as a single system. Notably, the average molecular distance between polysaccharide and microemulsion was approximately 1.7 nm. The half-maximal inhibitory concentration of MEs(PS-GLP) against A549 cells was about 119 μg/mL. In vivo imaging studies showed that introduction of GLP promoted the tumor-specific accumulation of microemulsion in comparison with controls. In vivo, antitumor results showed that MEs(PS-GLP) markedly inhibited the tumor growth of A549-bearing xenograft nude mice and obviously improve the serum immune index. Collectively, this study demonstrates the potential mechanism of spatial relation between polysaccharides and microemulsion and validates the significances of GLP on tumoral accumulation and antitumor efficacy.
本研究旨在探讨灵芝多糖(GLP)对薏苡仁油基微乳的影响及其对肺癌治疗的药物性能。GLP 整合薏苡仁油基微乳(MEs(PS-GLP))表现出清晰的球形、小粒径和良好的流体动力学特性,与薏苡仁油基微乳相似,但具有较低的 Zeta 电位和更好的稳定性。荧光共振能量转移分析表明,GLP 作为一个单一系统与微乳整合在一起。值得注意的是,多糖和微乳之间的平均分子距离约为 1.7nm。MEs(PS-GLP)对 A549 细胞的半最大抑制浓度约为 119μg/ml。体内成像研究表明,与对照组相比,GLP 的引入促进了微乳在肿瘤部位的特异性积累。体内实验结果表明,MEs(PS-GLP)显著抑制了 A549 荷瘤裸鼠的肿瘤生长,并明显改善了血清免疫指标。综上所述,本研究揭示了多糖与微乳之间空间关系的潜在机制,并验证了 GLP 在肿瘤积累和抗肿瘤疗效方面的重要意义。