Bhattacharya Koushik, Banerjee Sovan Lal, Kundu Moumita, Mandal Mahitosh, Singha Nikhil K
Rubber Technology Centre, Indian Institute of Technology, Kharagpur 721302, West Bengal, India.
School of Medical Science and Technology, Indian Institute of Technology, Kharagpur 721302, West Bengal, India.
Mater Sci Eng C Mater Biol Appl. 2020 Nov;116:111210. doi: 10.1016/j.msec.2020.111210. Epub 2020 Jun 25.
In this study, a polyhedral oligomeric silsesquioxane-polycaprolactone (POSS-PCL)-cored octa-arm star-shaped glyco block copolymer (BCP), poly(ε-caprolactone)-b-poly(glucopyranose) (Star-POSS-PCL-b-PGlc) was successfully synthesized via the combination of ring opening polymerization (ROP) and MADIX (macromolecular design by interchange of xanthate) polymerization technique. Herein, initially octa(3-hydroxy-3-methylbutyl dimethylsiloxy) POSS (Star-POSS) was utilized to initiate the ROP of the ε-caprolactone to get octa-arm star-shaped Star-POSS-PCL. A successive bromination followed by xanthation of the synthesized Star-POSS-PCL polymer allowed us to further polymerize 3-O-acryloyl-1,2:5,6-di-O-isopropylidene-α-D-glucofuranose (AIpGlc) via MADIX polymerization. Formation of the star-shaped block copolymer (BCP) was characterized using H NMR, FT-IR and DSC analyses. The morphology and the aqueous solution behavior of the Star-POSS-PCL-b-PGlc were analyzed using FESEM, HRTEM and DLS analyses, respectively. The lectin-binding efficiency of the star-shaped BCP having different glycopolymer block length was studied using turbidimetry assay and fluorescence quenching titration (FQT) using photoluminescence spectroscopy (PL). Here, FITC labeled concanavalin A (FITC-Con A) was used as a model lectin. The cytotoxicity study of the star-shaped BCPs over the human fibroblast cells revealed the non-toxic nature of the BCPs which open up its great potential towards drug delivery vector.
在本研究中，通过开环聚合（ROP）和MADIX（黄原酸酯交换法进行大分子设计）聚合技术相结合，成功合成了一种以多面体低聚倍半硅氧烷 - 聚己内酯（POSS - PCL）为核的八臂星形糖嵌段共聚物（BCP），即聚（ε - 己内酯） - b - 聚（吡喃葡萄糖）（Star - POSS - PCL - b - PGlc）。在此，首先利用八（3 - 羟基 - 3 - 甲基丁基二甲基硅氧基）POSS（Star - POSS）引发ε - 己内酯的ROP反应，得到八臂星形的Star - POSS - PCL。对合成的Star - POSS - PCL聚合物进行连续溴化，随后进行黄原酸化，使我们能够通过MADIX聚合进一步聚合3 - O - 丙烯酰基 - 1,2:5,6 - 二 - O - 异亚丙基 - α - D - 葡萄糖呋喃糖（AIpGlc）。使用核磁共振氢谱（H NMR）、傅里叶变换红外光谱（FT - IR）和差示扫描量热法（DSC）分析对星形嵌段共聚物（BCP）的形成进行了表征。分别使用场发射扫描电子显微镜（FESEM）、高分辨率透射电子显微镜（HRTEM）和动态光散射（DLS）分析对Star - POSS - PCL - b - PGlc的形态和水溶液行为进行了分析。使用比浊法和光致发光光谱（PL）的荧光猝灭滴定（FQT）研究了具有不同糖聚合物嵌段长度的星形BCP的凝集素结合效率。在此，异硫氰酸荧光素标记的伴刀豆球蛋白A（FITC - Con A）用作模型凝集素。对星形BCP对人成纤维细胞的细胞毒性研究表明，BCP具有无毒性质，这为其作为药物递送载体开辟了巨大潜力。
