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基于高负载多西他赛的聚恶唑啉胶束的抗癌活性。

Anti-Cancer Activity Based on the High Docetaxel Loaded Poly(2-Oxazoline)s Micelles.

机构信息

School of Pharmacy, Second Military Medical University, Shanghai, 200433, People's Republic of China.

Department of Pharmacy, Changzheng Hospital, Shanghai, 200003, People's Republic of China.

出版信息

Int J Nanomedicine. 2021 Apr 9;16:2735-2749. doi: 10.2147/IJN.S298093. eCollection 2021.

Abstract

PURPOSE

Nanocarriers, with a high drug loading content and good safety, to achieve desirable therapeutic effect are always the goals for industry and research.

METHODS AND RESULTS

In the present study, we developed a docetaxel loaded poly-2-oxazoline polymer micellar system which employed poly-2-butyl-2 oxazoline and poly-2-methyl-2 oxazoline as the hydrophobic chain and hydrophilic chain, respectively. This micellar system achieves a high load up to 25% against the docetaxel, and further demonstrates an IC50 as low as 40% of the commercialized docetaxel injection in vitro and a double maximum tolerated dose in MCF-7 cells in vivo.

CONCLUSION

The high drug loading content, superior safety, and considerable anti-cancer activity make this newly developed docetaxel loaded poly(2-oxazoline) micelle go further in future clinical research.

摘要

目的

载药纳米载体具有高载药量和良好的安全性,可实现理想的治疗效果,一直是工业和研究的目标。

方法和结果

在本研究中,我们开发了一种负载多西紫杉醇的聚-2-恶唑啉聚合物胶束系统,该系统分别采用聚-2-丁基-2 恶唑啉和聚-2-甲基-2 恶唑啉作为疏水链和亲水链。该胶束系统的载药量高达 25%,并且在体外对商业化多西紫杉醇注射液的 IC50 低至 40%,在 MCF-7 细胞中的最大耐受剂量也提高了一倍。

结论

高载药量、优越的安全性和相当的抗癌活性使得这种新开发的负载多西紫杉醇的聚(2-恶唑啉)胶束在未来的临床研究中更有前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/17c8/8043799/2251cfaed545/IJN-16-2735-g0001.jpg

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