Lipidated Peptidomimetic Ligand-Functionalized HER2 Targeted Liposome as Nano-Carrier Designed for Doxorubicin Delivery in Cancer Therapy.
Lipidated Peptidomimetic Ligand-Functionalized HER2 Targeted Liposome as Nano-Carrier Designed for Doxorubicin Delivery in Cancer Therapy.
复制标题
脂质化拟肽配体功能化 HER2 靶向脂质体作为纳米载体，设计用于癌症治疗中的阿霉素递送。
DOI：
10.3390/ph14030221
复制
发表时间：
2021-03-06
期刊：
影响因子：
--
通讯作者：
Jois S
中科院分区：
文献类型：
--
作者：
Naik H;Sonju JJ;Singh S;Chatzistamou I;Shrestha L;Gauthier T;Jois S
利用纳米载体介导的化疗给药可以提高化疗药物的治疗指标。配体靶向药物递送可用于实现化疗药物对癌细胞的选择性和特异性递送。在这项研究中，我们制备了一种拟肽偶联物（SA-5）标记的多柔比星（Dox）脂质体（LP）制剂（SA-5-Dox-LP），以评估SA-5在人表皮生长因子受体-2 （HER2）过表达的非小细胞肺癌（NSCLC）和乳腺癌细胞系中的靶向递送潜力。脂质体采用薄脂膜水合制备，并对其粒径、包封效率、细胞活力和靶向细胞摄取进行了表征。在非小细胞肺癌小鼠模型中进行了脂质体制剂的体内评价。细胞活力研究表明，靶向SA-5-Dox-LP比非靶向Dox脂质体（Dox- lp）具有更好的抗增殖活性。与非靶向脂质体相比，靶向her2的脂质体在癌细胞上表现出选择性的细胞摄取。体外释药研究表明，Dox在24 h内缓释缓慢，Dox- lp制剂与SA-5-Dox-LP制剂的Dox释放量无差异。非小细胞肺癌小鼠模型的体内研究表明，与对照和Dox相比，SA-5-Dox-LP能显著减少肺肿瘤。总之，本研究表明，SA-5-Dox-LP脂质体具有提高HER2过表达癌症的治疗效率和靶向递送Dox的潜力。
The therapeutic index of chemotherapeutic agents can be improved by the use of nano-carrier-mediated chemotherapeutic delivery. Ligand-targeted drug delivery can be used to achieve selective and specific delivery of chemotherapeutic agents to cancer cells. In this study, we prepared a peptidomimetic conjugate (SA-5)-tagged doxorubicin (Dox) incorporated liposome (LP) formulation (SA-5-Dox-LP) to evaluate the targeted delivery potential of SA-5 in human epidermal growth factor receptor-2 (HER2) overexpressed non-small-cell lung cancer (NSCLC) and breast cancer cell lines. The liposome was prepared using thin lipid film hydration and was characterized for particle size, encapsulation efficiency, cell viability, and targeted cellular uptake. In vivo evaluation of the liposomal formulation was performed in a mice model of NSCLC. The cell viability studies revealed that targeted SA-5-Dox-LP showed better antiproliferative activity than non-targeted Dox liposomes (Dox-LP). HER2-targeted liposome delivery showed selective cellular uptake compared to non-targeted liposomes on cancer cells. In vitro drug release studies indicated that Dox was released slowly from the formulations over 24 h, and there was no difference in Dox release between Dox-LP formulation and SA-5-Dox-LP formulation. In vivo studies in an NSCLC model of mice indicated that SA-5-Dox-LP could reduce the lung tumors significantly compared to vehicle control and Dox. In conclusion, this study demonstrated that the SA-5-Dox-LP liposome has the potential to increase therapeutic efficiency and targeted delivery of Dox in HER2 overexpressing cancer.
登录
查看更多内容
DOI：
10.2147/dddt.s149814
发表时间：
2017
期刊：
Drug design, development and therapy
影响因子：
--
作者：
Ding Y;Cui W;Sun D;Wang GL;Hei Y;Meng S;Chen JH;Xie Y;Wang ZQ
通讯作者：
Wang ZQ
影响因子：
3
作者：
Kanthala S;Banappagari S;Gokhale A;Liu YY;Xin G;Zhao Y;Jois S
通讯作者：
Jois S
影响因子：
14
作者：
Chiang, Yi-Ting;Lo, Chun-Liang
通讯作者：
Lo, Chun-Liang
影响因子：
4.4
作者：
Banappagari S;Ronald S;Satyanarayanajois SD
通讯作者：
Satyanarayanajois SD
影响因子：
3.7
作者：
Kim EK;Kim KA;Lee CY;Shim HS
通讯作者：
Shim HS