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pH --- Nanogel using pH sensitive block copolymer polyaspartic acid-graft-imidazole-polyethylene glycol and preparing method thereof

机译:pH敏感型嵌段共聚物聚天冬氨酸接枝咪唑聚乙二醇的pH ---纳米凝胶及其制备方法

摘要

The present invention relates to a nanogel using a pH-sensitive block copolymer and poly(aspartic acid-graft-imidazole)-polyethylene glycol, and a preparation method for the same. More specifically, the pH-sensitive nanogel is prepared through a chemical crosslinking reaction between poly(aspartic acid-graft-imidazole)-polyethylene glycol and polyethylene glycol on which chemically modified bis-N-hydroxysuccinimide (bis-NHS) is grafted. In particular, the nanogel has appropriate physicochemical characteristics (appropriate pK_a value, a wide buffer zone, a nano size, a positive Zeta potential, and morphology) and pH-dependent characteristics and thus, by an electrostatic interaction due to the imidazole group turning positively charged, can control drug release and increase drug efficacy to a target cell in an acidic tumor microenvironment (between pH 7.2 and pH 6.5) through reversible swelling and endosome destruction. Accordingly, the nanogel using poly(aspartic acid-graft-imidazole)-polyethylene glycol having the above effects can be utilized as a composition for drug delivery for tumor treatment.
机译:本发明涉及使用pH敏感型嵌段共聚物和聚(天冬氨酸-接枝-咪唑)-聚乙二醇的纳米凝胶及其制备方法。更具体地,pH敏感的纳米凝胶是通过聚(天冬氨酸-接枝-咪唑)-聚乙二醇和聚乙二醇(其上接枝了化学改性的双-N-羟基琥珀酰亚胺(bis-NHS))之间的化学交联反应制备的。特别地,纳米凝胶具有适当的物理化学特性(适当的pK_a值,宽的缓冲带,纳米尺寸,正Zeta电势和形态)和pH依赖性特性,并且因此由于咪唑基团正向旋转而通过静电相互作用而具有。在酸性肿瘤微环境(pH 7.2和pH 6.5之间)中,通过带电,可以控制药物释放,并通过可逆溶胀和内体破坏来提高对靶细胞的药效。因此,具有上述效果的使用聚(天冬氨酸-接枝-咪唑)-聚乙二醇的纳米凝胶可用作用于治疗肿瘤的药物递送的组合物。

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