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Camptothecin nanocolloids based on NNN-trimethyl chitosan: Efficient suppression of growth of multiple myeloma in a murine model

机译:基于NNN-三甲基壳聚糖的喜树碱纳米胶体:在小鼠模型中有效抑制多发性骨髓瘤的生长

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摘要

Camptothecin (CPT) exhibits very strong antitumor effects by inhibiting the activity of DNA topoisomerase I, but its application is greatly limited due to its low solubility and the instability of the active lactone form. To overcome these shortcomings, in the present study, we prepared novel camptothecin nanocolloids based on N,N,N-trimethyl chitosan (CPT-TMC) to efficiently and safely administer CPT systemically. Herein, we investigated the antitumor activity of CPT-TMC against a murine Balb/c myeloma model. Our results showed that CPT-TMC more effectively inhibited tumor growth and prolonged survival time than CPT in vivo, but no statistical difference was observed in vitro between CPT-TMC and CPT. These findings suggest that N,N,N-trimethyl chitosan could increase the stability and the antitumor effect of CPT and CPT-TMC is a potential approach for the effective treatment of multiple myeloma.
机译:喜树碱(CPT)通过抑制DNA拓扑异构酶I的活性表现出非常强的抗肿瘤作用,但由于其低溶解度和活性内酯形式的不稳定性,其应用受到极大限制。为克服这些缺点,在本研究中,我们基于N,N,N-三甲基壳聚糖(CPT-TMC)制备了新型喜树碱纳米胶体,以有效,安全地全身性管理CPT。本文中,我们研究了CPT-TMC对鼠Balb / c骨髓瘤模型的抗肿瘤活性。我们的结果表明,CPT-TMC在体内比CPT更有效地抑制肿瘤生长并延长了生存时间,但CPT-TMC和CPT在体外没有观察到统计学差异。这些发现表明,N,N,N-三甲基壳聚糖可以提高稳定性,CPT和CPT-TMC的抗肿瘤作用是有效治疗多发性骨髓瘤的潜在方法。

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