کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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598913 | 1454262 | 2016 | 7 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Complete regression of xenograft tumors using biodegradable mPEG-PLA-SN38 block copolymer micelles Complete regression of xenograft tumors using biodegradable mPEG-PLA-SN38 block copolymer micelles](/preview/png/598913.png)
• A series of amphiphilic mPEG-PLA-SN38-conjugates were synthesized and formed to micelles by self-assembly.
• The lengths of mPEG and PLA chains had a major impact on the physicochemical characteristics and antitumor activity of mPEG-PLA-SN38 micelles.
• mPEG2K-PLA8.9K-SN38 micelles are the most effective with complete regression of xenograft tumors.
7-Ethyl-10-hydroxy-comptothecin (SN38) is an active metabolite of irinotecan (CPT-11) and the clinical application of SN38 is limited by its hydrophobicity and instability. To address these issues, a series of novel amphiphilic mPEG-PLA-SN38-conjugates were synthesized by linking SN38 to mPEG-PLA-SA, and they could form micelles by self-assembly. The effects of mPEG-PLA composition were studied in vitro and in vivo. The mean diameters of mPEG2K-PLA-SN38 micelles and mPEG4K-PLA-SN38 micelles were 10–20 nm and 120 nm, respectively, and mPEG2K-PLA-SN38 micelles showed greater antitumor efficacy than mPEG4K-PLA-SN38 micelles both in vitro and in vivo. These data suggest that the lengths of mPEG and PLA chains had a major impact on the physicochemical characteristics and antitumor activity of SN38-conjugate micelles.
A series of new amphiphilic mPEG-PLA-SN38-conjugates were synthesized and formed micelles by self-assembly. Micelles of mPEG2K-PLA-SN38 have small size (∼20 nm) and narrow size distribution. The lengths of mPEG and PLA chains had a major impact on the physicochemical characteristics and antitumor activity of SN38-conjugate micelles. The mPEG2K-PLA8·9k-SN38 micelles showed greater antitumor efficacy in HCT116 human colon cancer xenograft model.Figure optionsDownload as PowerPoint slide
Journal: Colloids and Surfaces B: Biointerfaces - Volume 142, 1 June 2016, Pages 417–423