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Cypate介导的靶向热敏纳米脂质体用于肿瘤成像和光热触发的药物释放

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Cypate介导的靶向热敏纳米脂质体用于肿瘤成像和光热触发的药物释放
Cypate-Mediated Thermosensitive Nanoliposome for Tumor Imaging and Photothermal Triggered Drug Release
投稿时间：2016-11-19
DOI：10.15918/j.tbit1001-0645.2017.增刊1.019
中文关键词:Cypate光热敏感脂质体EPR效应触发释放光热转换
English Keywords:Cypatephotothermal sensitive liposomeERP effect triggered releasephotothermal conversion
基金项目:国家"九七三"计划项目（2015CB755504），国家自然科学基金资助项目（81220108012）
作者单位E-mail
吕丽伟中国药科大学 生物医学工程教研室, 江苏 南京 210009
韩智豪中国药科大学 生物医学工程教研室, 江苏 南京 210009
顾月清中国药科大学 生物医学工程教研室, 江苏 南京 210009guyueqingsubmission@hotmail.com
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中文摘要:
本文合成了一种新型多功能的纳米靶向脂质体药物递送系统，即所述的光热敏感脂质体（PTSL），它的水溶性层掺杂了阿霉素作为治疗剂，同时它的疏水层包裹了Cypate作为诊断剂外层磷脂修饰了靶向穿膜肽H4-1.测试了PTSL的物理性质，稳定性以及脂质体的装载性能，合成的纳米复合材料具有针对性，稳定性和精准性，具有载药量（DL）9±1.5%和包封率（EE）82.7±2.1%.其Tm值落在43.1℃，其温度可以被认为能够显示有效的热疗法，但不燃烧的正常组织的合适温度.提高脂质体的Tm温度达到热敏脂质体的热敏温度，脂质体崩解同时包裹的化疗药物释放.与此同时，在细胞器水平上，PTSLs主要位于细胞质.当暴露在近红外光下，所述的Cypate可以产生单线态氧，从而引起膜的破裂.该脂质体可以实现靶向输送，增强光化学内化释放，化疗和热疗的功能.实验表明该PTSL是一种有前途的药物递送系统，用于肿瘤的诊断和靶向治疗.
English Summary:
Synthesized a novel multifunctional targeting nano liposome drug delivery system,the photothermal sensitive liposome(PTSL),with doxorubicin wrapped in the hydropholic layer as the therapeutical agents and cypate dopped in the hydrophobic layer as the diagnostic agents,and the outer phospholipid modified the targeted transmembrance peptide H4-1.The physical properties,stabilities and loading properties of the liposomes were tested,the nano composites we synthesized were targeted,stable and delicate,with a drug loading(DL)of 9±1.5% and encapsulation efficiency(EE)of 82.7±2.1%.The Tm value falls on 43.1℃,the temperature of which can be regarded as the proper temperature which can show the thermal therapy effective as well as not burn the normal tissue.It can raise the temperature of liposome to the Tm of thermal sensitive liposome,the liposome cracks and the wrapped chemotherapy drugs release.At the same time,in the level of organelles,the PTSLs mainly located in the cytoplasm.When exposured to the NIR light,the cypate can incuce the producing of singlet oxygen,causing the crack of the organelle membrane.And the liposome can achieve the functions of target-delivery,enhanced photochemical internalized release,chemotherapy and thremal therapy,indicating that the PTSL is a kind of promising drug delivery system for tumor diagnosis and targeting therapy.
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相关话题/江苏 中国药科大学 生物医学工程 药物 纳米

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