羧甲基壳聚糖和十八胺包被的脂质体含WPTS的设计、优化和评价。
Carboxymethyl chitosan and Octadecylamine-coated liposome-containing WPTS: design, optimization and evaluation.
发表日期:2023 Aug 09
作者:
Nan Wang, Chi Zhang, Jiahui Wu, Dachuan Zhang, Junling Li, Galvbu A, Leimengyuan Tang, Yan Li, Houxier Li, Shuting Tan, Xueyong Wang
来源:
JOURNAL OF LIPOSOME RESEARCH
摘要:
脂质体(LPs)是一种用于稳定具有有限使用的药物传递系统,因其会聚和融合的倾向而受到限制。解决这些问题的一种提议的方法是聚合物包覆。本研究调查了十八胺酸(ODA)包被脂质体和羧甲基壳聚糖(CMCS/ODA-LPs)用于提高油茶五环萜皂苷(WPTS)的转运能力的潜力。CMCS/ODA-LPs通过静电吸附和薄膜水合法制备。响应面方法(RSM)被应用于提高过程和最佳药物封装效率(Encapsulation Efficiency, EE)。合成的WPTS-CMCS/ODA-LPs在圆形形状中均匀分散,并在4℃存放14天期间,其粒径和形态没有显著变化。囊泡尺寸、zeta电位、多分散性指数(Polydispersity Index, PDI)和封装效率(%)分别为179.1±7.31 nm,-29.6±1.35mV,0.188±0.052和75.62±0.43。溶血试验表明WPTS-CMCS/ODA-LPs具有足够的生物相容性。与WPTS-LPs相比,WPTS-CMCS/ODA-LPs对癌细胞显示了更显著的细胞毒性作用。早期和WPTS-CMCS/ODA-LPs诱导的细胞凋亡导致的细胞死亡几乎是对照组的七倍。与生理pH 7.3相比,pH敏感的CMCS耦合脂质体在酸性pH 6.5条件下增加了药物释放。这些发现表明pH敏感的CMCS/ODA-LPs作为WPTS的治疗传递方法的有效性。
Liposomes (LPs) are a delivery system for stabilizing pharmaceuticals with limited use due to their propensity to congregate and fuse. A proposed method of addressing these is problems polymer coating. In this study, the potential of octadecylamine (ODA)-coated liposomes and carboxymethyl chitosan (CMCS/ODA-LPs) for enhancing wacao pentacyclic triterpene saponin (WPTS) transport capacity was investigated. CMCS/ODA-LPs were produced by electrostatic adsorption and thin-film hydration. Response surface methodology (RSM) was employed to enhance the process and encapsulation efficiency (EE) for optimum drug encapsulation efficiency. The synthesized WPTS-CMCS/ODA-LPs were uniformly dispersed in a circular shape, and during 14 days of storage at 4 °C, the particle size and morphology did not significantly change. Vesicle size, zeta potential, polydispersity index (PDI), and entrapment efficiency (%) were 179.1 ± 7.31nm, -29.6 ± 1.35mV, 0.188 ± 0.052, and 75.62 ± 0.43, respectively. The hemolysis test revealed that WPTS-CMCS/ODA-LPs were sufficiently biocompatible. Compared to WPTS-LPs, WPTS-CMCS/ODA-LPs consistently showed a much more significant cytotoxic effect on cancer cells. Early and WPTS-CMCS/ODA-LPs-induced apoptosis resulted in almost seven times more cell death than the control. Compared to physiological pH 7.3, the pH-sensitive CMCS coupled liposomes increased drug release at acidic pH 6.5. These findings suggest the efficacy of pH-sensitive CMCS/ODA-LPs as a medication delivery method for WPTS.