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A Smart Nano‐Prodrug Platform with Reactive Drug Loading, Superb Stability, and Fast Responsive Drug Release for Targeted Cancer Therapy

机译：一种具有反应性药物负荷，极好稳定性和靶向癌症治疗的快速响应药物释放的智能纳米前药平台

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Abstract > Nano‐prodrugs usually involve a multistep synthesis which largely compromises their benefits. Here, a smart nano‐prodrug platform with reactive drug loading, superb stability, and triggered drug release is reported for targeted melanoma therapy. cRGD‐decorated polymersomal mertansine prodrug (cRGD‐PS‐DM1) is readily fabricated from cRGD‐functionalized poly(ethylene glycol)‐ b ‐poly(trimethylene carbonate‐ co ‐dithiolane trimethylene carbonate) with simultaneous loading of mertansine (DM1) via thiol–disulfide exchange reaction and disulfide cross‐linking of polymersomal membrane. cRGD‐PS‐DM1 exhibits a size of ≈100 nm, little drug leakage, and fast DM1 release in the presence of 2 × 10 ?3 –10 × 10 ?3 <sc>m</sc> glutathione. Tetrazolium‐based colorimetric assay (MTT) and confocal microscopy studies confirm effective homing of cRGD‐PS‐DM1 to α <sub>v</sub> β <sub>3</sub> overexpressing B16F10 melanoma cells. Notably, the in vivo studies show that cRGD‐PS‐DM1 has a greatly improved toleration as compared with free DM1 and effectively inhibits tumor growth and extends the survival time of B16F10 melanoma‐bearing mice. cRGD‐PS‐DM1 nano‐prodrug with reactive drug loading and multifunction provides an advanced nanomedicine for cancer therapy. <blockFixed type="graphic"> <mediaResourceGroup> <mediaResource alt="image" href="urn:x-wiley:16165187:media:mabi201600518:mabi201600518-abs-0001"/> </mediaResourceGroup> </blockFixed> </abstract> </span> <span class="z_kbtn z_kbtnclass hoverxs" style="display: none;">展开▼</span> </div> <div class="translation abstracttxt"> <span class="zhankaihshouqi fivelineshidden" id="abstract"> <span>机译：</span><Abstract Type =“main”XML：Lang =“en”> <标题类型=“main”>抽象</ title> >纳米前药通常涉及多步综合，这主要损害它们的益处。这里，据报道了一种具有反应性药物负载，极好稳定性和触发药物释放的智能纳米前药平台，用于靶向黑素瘤治疗。 CRGD装饰聚合物MERTANE产品（CRGD-PS-DM1）易于由CRGD-官能化聚（乙二醇） - <I> B-Poly（三甲基碳酸亚乙酯 - <I> CO-I> - 二硫烷三甲基碳酸酯，通过硫醇二硫化物交换反应同时加载Mertansine（DM1）和聚合物膜的二硫化物交联。 CRGD-PS-DM1在2×10 α3</ sup> -10×10 3 </ sup>的情况下表现出≈100nm的尺寸，少量药物泄漏，少量药物泄漏和快速DM1释放<sc> m </ sc>谷胱甘肽。基于四唑基的比色测定（MTT）和共聚焦显微镜研究证实了CRGD-PS-DM1至α<亚> V </ sub>β<sub> 3 </ sub>过表达B16F10黑素瘤细胞的有效归巢。值得注意的是，体内研究表明，与游离DM1相比，CRGD-PS-DM1具有大大提高的耐受性，并有效抑制肿瘤生长并延长B16F10黑色素瘤小鼠的存活时间。 CRGD-PS-DM1纳米前药具有反应性药物载荷和多功能，为癌症治疗提供先进的纳米胺。 <blockfixed类型=“图形”> <mediaresourcegroup> <mediaresource alt =“图像”href =“urn：x-wiley：16165187：mabi201600518：mabi201600518：mabi201600518-abs-abs-0001”/> </ mediaresourcegroup> </ blockfixed> < / p> </ abstract> </span> <span class="z_kbtn z_kbtnclass hoverxs" style="display: none;">展开▼</span> </div> </div> <div class="record"> <h2 class="all_title" id="enpatent33" >著录项</h2> <ul> <li> <span class="lefttit">来源</span> <div style="width: 86%;vertical-align: text-top;display: inline-block;"> <a href='/journal-foreign-24307/'>《Macromolecular bioscience》</a> <b style="margin: 0 2px;">|</b><span>2017年第10期</span><b style="margin: 0 2px;">|</b><span>共8页</span> </div> </li> <li> <div class="author"> <span class="lefttit">作者</span> <p id="fAuthorthree" class="threelineshidden zhankaihshouqi"> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Meng Hao&option=202" target="_blank" rel="nofollow">Meng Hao;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Zou Yan&option=202" target="_blank" rel="nofollow">Zou Yan;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Zhong Ping&option=202" target="_blank" rel="nofollow">Zhong Ping;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Meng Fenghua&option=202" target="_blank" rel="nofollow">Meng Fenghua;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Zhang Jian&option=202" target="_blank" rel="nofollow">Zhang Jian;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Cheng Ru&option=202" target="_blank" rel="nofollow">Cheng Ru;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Zhong Zhiyuan&option=202" target="_blank" rel="nofollow">Zhong Zhiyuan;</a> </p> <span class="z_kbtnclass z_kbtnclassall hoverxs" id="zkzz" style="display: none;">展开▼</span> </div> </li> <li> <div style="display: flex;"> <span class="lefttit">作者单位</span> <div style="position: relative;margin-left: 3px;max-width: 639px;"> <div class="threelineshidden zhankaihshouqi" id="fOrgthree"> <p>Biomedical Polymers Laboratory and Jiangsu Key Laboratory of Advanced Functional Polymer Design and ApplicationSoochow UniversitySuzhou 215123 P. R. China;</p> <p>Biomedical Polymers Laboratory and Jiangsu Key Laboratory of Advanced Functional Polymer Design and ApplicationSoochow UniversitySuzhou 215123 P. R. China;</p> <p>Biomedical Polymers Laboratory and Jiangsu Key Laboratory of Advanced Functional Polymer Design and ApplicationSoochow UniversitySuzhou 215123 P. R. China;</p> <p>Biomedical Polymers Laboratory and Jiangsu Key Laboratory of Advanced Functional Polymer Design and ApplicationSoochow UniversitySuzhou 215123 P. R. China;</p> <p>Biomedical Polymers Laboratory and Jiangsu Key Laboratory of Advanced Functional Polymer Design and ApplicationSoochow UniversitySuzhou 215123 P. R. China;</p> <p>Biomedical Polymers Laboratory and Jiangsu Key Laboratory of Advanced Functional Polymer Design and ApplicationSoochow UniversitySuzhou 215123 P. R. China;</p> <p>Biomedical Polymers Laboratory and Jiangsu Key Laboratory of Advanced Functional Polymer Design and ApplicationSoochow UniversitySuzhou 215123 P. R. China;</p> </div> <span class="z_kbtnclass z_kbtnclassall hoverxs" id="zhdw" style="display: none;">展开▼</span> </div> </div> </li> <li > <span class="lefttit">收录信息</span> <span style="width: 86%;vertical-align: text-top;display: inline-block;"></span> </li> <li> <span class="lefttit">原文格式</span> <span>PDF</span> </li> <li> <span class="lefttit">正文语种</span> <span>eng</span> </li> <li> <span class="lefttit">中图分类</span> <span><a href="https://www.zhangqiaokeyan.com/clc/1185.html" title="高分子化学（高聚物）">高分子化学（高聚物）;</a></span> </li> <li class="antistop"> <span class="lefttit">关键词</span> <p style="width: 86%;vertical-align: text-top;"> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=active targeting&option=203" rel="nofollow">active targeting;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=melanoma&option=203" rel="nofollow">melanoma;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=polymer–drug conjugate&option=203" rel="nofollow">polymer–drug conjugate;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=polymersomes&option=203" rel="nofollow">polymersomes;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=reduction‐sensitive&option=203" rel="nofollow">reduction‐sensitive;</a> </p> <div class="translation"> 机译：活性靶向;黑色素瘤;聚合物 - 药物缀合物;聚合物;还原敏感; 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href="/academic-journal-cn_journal-gansu-united-university-natural-science-edition_thesis/0201249271372.html">智能给药系统研究进展——物理刺激响应性药物释放系统</a> <b>[J]</b> <span> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=张玉翠&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor"> . 张玉翠</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=王斌&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor">,王斌</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=李维民&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor">,李维民</a> <span> <a href="/journal-cn-4600/" target="_blank" rel="nofollow" class="tuijian_authcolor"> . 甘肃联合大学学报（自然科学版） </a> </span> <span> . 2006</span><span>,第006期</span> </span> </div> </li> <li> <div> <b>4. </b><a class="enjiyixqcontent" href="/academic-journal-cn_journal-tongren-university_thesis/0201233161161.html">具有磁靶向性的pH响应智能药物载体的制备</a> <b>[J]</b> <span> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=黄啸&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor"> . 黄啸</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=许佐娟&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor">,许佐娟</a> <span> <a href="/journal-cn-3762/" target="_blank" rel="nofollow" class="tuijian_authcolor"> . 铜仁学院学报 </a> </span> <span> . 2017</span><span>,第012期</span> </span> </div> </li> <li> <div> <b>5. </b><a class="enjiyixqcontent" href="/academic-degree-domestic_mphd_thesis/020312037310.html">PUA/PSS层层自组装药物载体的制备及智能响应性药物释放</a> <b>[A] </b> <span> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=杜超&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor"> . 杜超</a> <span> . 2013</span> </span> </div> </li> </ul> <ul style="display: none;"> <li> <div> <b>1. </b><a class="enjiyixqcontent" href="/patent-detail/06120101326896.html">一种叶酸修饰纳米MOF-Al具有靶向功能的响应性药物载体的制备方法</a> <b>[P]</b> . <span> 中国专利： CN110559274A </span> <span> . 2019-12-13</span> </div> </li> <li> <div> <b>2. </b><a class="enjiyixqcontent" href="/patent-detail/06120108206332.html">用于癌症化学治疗剂的亲脂性药物和酸不稳定性亲脂性前体药物的靶向递送的纳米颗粒组合物及它们的制备</a> <b>[P]</b> . <span> 中国专利： CN105722506A </span> <span> . 2016-06-29</span> </div> </li> <li> <div> <b>3. </b><a class="enjiyixqcontent" href="/patent-detail/06130430406827.html">Method and composition for treating a subject having a cancer, kit, pharmaceutical composition, method for impregnating or loading an implantable drug release device, implantable drug release device, method for assessing an individual's response to a cancer. treatment using a tlr3 agonist or selecting an individual having a cancer responsive to treatment using a tlr3 agonist, complex, method for determining whether a test compound is useful for cancer treatment, and use of a tlr3 agonist</a> <b>[P]</b> . <span> 外国专利： <!-- --> BRPI0518307A2 </span> <span> . 2008-11-11</span> </div> <p class="zwjiyix translation" style="max-width: initial;height: auto;word-break: break-all;white-space: initial;text-overflow: initial;overflow: initial;"> <span>机译：用于治疗患有癌症的受试者的方法和组合物，试剂盒，药物组合物，用于浸渍或加载可植入药物释放装置的方法，可植入药物释放装置，用于评估个体对癌症反应的方法。使用tlr3激动剂的治疗或选择对tlr3激动剂的治疗有反应的癌症的个体，复合物，确定测试化合物是否可用于癌症治疗的方法以及tlr3激动剂的用途 </span> </p> </li> <li> <div> <b>4. </b><a class="enjiyixqcontent" href="/patent-detail/06130500332950.html">Porous nanocomposite of CuS and Silica for photothermal therapy and drug release by cancer cell targeting type double stimuli and method for preparing the same</a> <b>[P]</b> . <span> 外国专利： <!-- --> KR20210088221A </span> <span> . 2021-07-14</span> </div> <p class="zwjiyix translation" style="max-width: initial;height: auto;word-break: break-all;white-space: initial;text-overflow: initial;overflow: initial;"> <span>机译：CUS和二氧化硅的多孔纳米复合物用于光热疗和通过癌细胞靶向型双刺激的药物释放及其制备方法 </span> </p> </li> <li> <div> <b>5. </b><a class="enjiyixqcontent" href="/patent-detail/06130408578388.html">Au/Ag Au/Ag hollow nanoshells for treating lung cancer using target drug release and photothermal therapy at near-IR range</a> <b>[P]</b> . <span> 外国专利： <!-- 韩国专利： --> KR101757273B1 </span> <span> . 2017-07-12</span> </div> <p class="zwjiyix translation" style="max-width: initial;height: auto;word-break: break-all;white-space: initial;text-overflow: initial;overflow: initial;"> <span>机译：Au / Ag Au / Ag中空纳米壳，用于靶药物释放和近红外范围内的光热疗法，用于治疗肺癌 </span> </p> </li> </ul> </div> </div> </div> <div class="theme cardcommon" style="overflow: auto;display:none"> <h3 class="all_title" id="enpatent55">相关主题</h3> <ul id="subject"> </ul> </div> </div> </div> </div> <div class="right rightcon"> <div class="details_img cardcommon clearfix" style="margin-bottom: 10px;display:none;" > </div> </div> </div> <div id="thesis_get_original1" class="downloadBth" style="bottom: 19px;z-index: 999;" 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