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pH响应性mPEG-S-S-DSPE脂质体载药系统的制备
发布时间:2025-07-10     作者:zyl   分享到:
医学文献:Targeted delivery and triggered release of liposomal doxorubicin enhances cytotoxicity against human B lymphoma cells诗人:TIshida a 1, M.J Kirchmeier a 2, E.H Moase a, S Zalipsky b, T.M Allen 论文链接搜索: 论文摘要:Dioleoylphosphatidylethanolamine (DOPE)-containing liposomes that demonstrated pH-dependent release of their contents were stabilized in the bilayer form through the addition of a cleavable lipid derivative of polyethylene glycol (PEG) in which the PEG was attached to a lipid anchor via a disulfide linkage (mPEG-S-S-DSPE). Liposomes stabilized with either a non-cleavable PEG (mPEG-DSPE) or mPEG-S-S-DSPE retained an encapsulated dye at pH 5.5, but treatment at pH 5.5 of liposomes stabilized with mPEG-S-S-DSPE with either dithiothreitol or cell-free extracts caused contents release due to cleavage of the PEG chains and concomitant destabilization of the DOPE liposomes. While formulations loaded with doxorubicin (DXR) were stable in culture media, DXR was rapidly released in human plasma. pH-Sensitive liposomes, targeted to the CD19 epitope on B-lymphoma cells, showed enhanced DXR delivery into the nuclei of the target cells and increased cytotoxicity compared to non-pH-sensitive liposomes. Pharmacokinetic studies suggested that mPEG-S-S-DSPE was rapidly cleaved in circulation. In a murine model of B-cell lymphoma, the therapeutic efficacy of an anti-CD19-targeted pH-sensitive formulation was superior to that of a stable long-circulating formulation of targeted liposomes despite the more rapid drug release and clearance of the pH-sensitive formulation. These results suggest that targeted pH-sensitive formulations of drugs may be able to increase the therapeutic efficacy of entrapped drugs.

mPEG-S-S-DSPE

利用增加聚乙二醇(PEG)的可切工脂质产生物,但其中PEG利用二硫键(mPEG-S-S-DSPE)连接方式到脂质锚定物上,含二油酰磷脂酰工业乙醇胺(DOPE)的脂质体以多层行式增强入乎容物的pH依懒性减少。用不可以切工的PEG(mPEG-DSPE)或mPEG-S-S-DSPE稳定性高的脂质体在pH 5.5时补齐了包封的染色剂,但用二硫苏糖醇或无组织获取物在pH 5.5下治理 用mPEG-S-S-S-DSPE固定的的脂质体,在PEG链的切工和DOPE脂质体的周期性失稳,促使知识物挥发。其实可载阿霉素(DXR)的剂型在培养计划基中是稳定性高的,但DXR在人血浆中发展降低。pH过敏脂质体靶点B淋巴腺瘤肿瘤上皮组织上的CD19表位,和非pH过敏脂质机制备的脂质体比起来,显视出增进的DXR向靶肿瘤上皮组织结构的递送,并提升了肿瘤上皮组织毒副作用。药代推热学学习认为,mPEG-S-S-DSPE在重复中很快裂解。在B组织淋巴结瘤的小鼠实体模型中,无论怎样抗CD19靶向疗法疗法pH敏感性溶液剂的口服药产生和快速清理效率迅速,但其冶疗功能远低于不稳的靶向疗法疗法脂质体长重复溶液剂。这样报告单体现了,靶向药品pH脆弱的药品溶液剂或许还可以提升包埋药品的进行治疗成果。相应的选择:DSPE-PEG-Mannose,DSPE-PEG-ManDSPE-PEG-MethyltetrazineDSPE-PEG-MTXDSPE-PEG-nano goldDSPE-PEG-NBDSPE-PEG-NBDDSPE-PEG-NPCDSPE-PEG-NTA-NIDSPE-PEG-PCLDSPE-PEG-PDPDSPE-PEG-PEIDSPE-PEG-PLA往上论文介绍原因种类期刊论文或参考文献,告之侵权行为请找公司清空!