期刊
EUROPEAN POLYMER JOURNAL
卷 145, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.eurpolymj.2020.110232
关键词
Glioblastoma; Poly(2-ethyl-2-oxazoline); Micelle; Temozolomide; Prodrug
资金
- National Natural Science Foundation of China [51802127]
- PAPD of Jiangsu Province, Postgraduate Research & Practice Innovation Program of Jiangsu Province [KYCX20_2252, KYCX19-2236]
- Social Development Project of Jiangsu Department of Science and Technology [BE2016646]
- Jiangsu Provincial Commission of Health and Family Planning [Q201608]
The synthesis of PEtOz-TMZ conjugate has shown enhanced efficacy and stability of TMZ in vivo, indicating a promising route of administration for TMZ in clinical practice.
The current treatment of glioblastoma (GBM) remains challenging. Temozolomide (TMZ), a first-line chemotherapy drug used to treat glioblastoma, is rapidly cleared under normal physiological conditions and has poor stability, which severely limits its efficacy. In current work, poly(2-ethyl-2-oxazoline) (PEtOz) conjugated TMZ (PEtOz-TMZ) was synthesized and directly dissolved in PBS to form prodrug micelles. This PEtOz-TMZ conjugation did not affect the DNA alkylation of TMZ and enhanced the stability of TMZ, prolonged the circulation time in vivo and increased the TMZ accumulation in glioblastoma. In vivo, the PEtOz-TMZ micelle significantly enhanced the efficiency of TMZ to inhibit the growth of glioblastoma. These results indicate that binding to the polymer can effectively improve the efficacy and stability of TMZ, and is a promising route of administration of TMZ in clinic.
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