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A Novel MPEG-PDLLA-PLL Copolymer for Docetaxel Delivery in Breast Cancer Therapy
Theranostics ( IF 12.4 ) Pub Date : 2017-07-06 , DOI: 10.7150/thno.19680 Liwei Tan 1 , Jinrong Peng 1 , Qian Zhao 1 , Lan Zhang 1 , Xichuan Tang 1 , Lijuan Chen 1 , Minyi Lei 1 , Zhiyong Qian 1
Theranostics ( IF 12.4 ) Pub Date : 2017-07-06 , DOI: 10.7150/thno.19680 Liwei Tan 1 , Jinrong Peng 1 , Qian Zhao 1 , Lan Zhang 1 , Xichuan Tang 1 , Lijuan Chen 1 , Minyi Lei 1 , Zhiyong Qian 1
Affiliation
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Satisfactory drug loading capacity and stability are the two main factors that determine the anti-cancer performance. In general, the stability of the micelles is reduced when the drug loading (DL) is increased. Therefore, it was a challenge to have high drug loading capacity and good stability. In this study, we introduced a hydrophilic poly (L-Lysine) (PLL) segment with different molecular-weights into the monomethoxy poly (ethylene glycol)-poly (D, L-lactide) (MPEG-PDLLA) block copolymer to obtain a series of novel triblock MPEG-PDLLA-PLL copolymers. We found that the micelles formed by a specific MPEG2k-PDLLA4k-PLL1k copolymer could encapsulate docetaxel (DTX) with a satisfactory loading capacity of up to 20% (w/w) via the thin film hydration method, while the stability of drug loaded micellar formulation was still as good as that of micelles formed by MPEG2k-PDLLA1.7k with drug loading of 5% (w/w). The results from computer simulation study showed that compared with MPEG2k-PDLLA1.7k, the molecular chain of MPEG2k-PDLLA4k-PLL1k could form a more compact funnel-shaped structure when interacted with DTX. This structure favored keeping DTX encapsulated in the copolymer molecules, which improved the DL and stability of the nano-formulations. The in vitro and in vivo evaluation showed that the DTX loaded MPEG2k-PDLLA4k-PLL1k (DTX/MPEG2k-PDLLA4k-PLL1k) micelles exhibited more efficiency in tumor cell growth inhibition. In conclusion, the MPEG2k-PDLLA4k-PLL1k micelles were much more suitable than MPEG2k-PDLLA1.7k for DTX delivery, and then the novel nano-formulations showed better anti-tumor efficacy in breast cancer therapy.
中文翻译：
一种用于乳腺癌治疗中多西紫杉醇输送的新型 MPEG-PDLLA-PLL 共聚物
良好的载药量和稳定性是决定抗癌性能的两个主要因素。一般来说，当载药量 (DL) 增加时，胶束的稳定性会降低。因此，具有高载药量和良好的稳定性是一个挑战。在本研究中，我们将不同分子量的亲水性聚（L-赖氨酸）（PLL）片段引入到单甲氧基聚（乙二醇）-聚（D，L-丙交酯）（MPEG-PDLLA）嵌段共聚物中，获得了系列新型三嵌段 MPEG-PDLLA-PLL 共聚物。我们发现，由特定的 MPEG 2k -PDLLA 4k -PLL 1k共聚物形成的胶束可以通过薄膜水合方法封装多西紫杉醇 (DTX)，其负载量高达 20% (w/w)，同时稳定性也很好。载药胶束制剂仍然与载药量为 5% (w/w) 的 MPEG 2k -PDLLA 1.7k形成的胶束一样好。计算机模拟研究结果表明，与MPEG 2k -PDLLA 1.7k相比，MPEG 2k -PDLLA 4k -PLL 1k的分子链与DTX相互作用时能形成更致密的漏斗状结构。这种结构有利于将 DTX 封装在共聚物分子中，从而提高了纳米制剂的 DL 和稳定性。体外和体内评价表明，负载DTX的MPEG 2k -PDLLA 4k -PLL 1k (DTX/MPEG 2k -PDLLA 4k -PLL 1k )胶束在肿瘤细胞生长抑制方面表现出更高的效率。 总之，MPEG 2k -PDLLA 4k -PLL 1k胶束比 MPEG 2k -PDLLA 1.7k更适合 DTX 递送，并且新型纳米制剂在乳腺癌治疗中显示出更好的抗肿瘤功效。
更新日期：2017-10-01
中文翻译：
一种用于乳腺癌治疗中多西紫杉醇输送的新型 MPEG-PDLLA-PLL 共聚物
良好的载药量和稳定性是决定抗癌性能的两个主要因素。一般来说，当载药量 (DL) 增加时，胶束的稳定性会降低。因此，具有高载药量和良好的稳定性是一个挑战。在本研究中，我们将不同分子量的亲水性聚（L-赖氨酸）（PLL）片段引入到单甲氧基聚（乙二醇）-聚（D，L-丙交酯）（MPEG-PDLLA）嵌段共聚物中，获得了系列新型三嵌段 MPEG-PDLLA-PLL 共聚物。我们发现，由特定的 MPEG 2k -PDLLA 4k -PLL 1k共聚物形成的胶束可以通过薄膜水合方法封装多西紫杉醇 (DTX)，其负载量高达 20% (w/w)，同时稳定性也很好。载药胶束制剂仍然与载药量为 5% (w/w) 的 MPEG 2k -PDLLA 1.7k形成的胶束一样好。计算机模拟研究结果表明，与MPEG 2k -PDLLA 1.7k相比，MPEG 2k -PDLLA 4k -PLL 1k的分子链与DTX相互作用时能形成更致密的漏斗状结构。这种结构有利于将 DTX 封装在共聚物分子中，从而提高了纳米制剂的 DL 和稳定性。体外和体内评价表明，负载DTX的MPEG 2k -PDLLA 4k -PLL 1k (DTX/MPEG 2k -PDLLA 4k -PLL 1k )胶束在肿瘤细胞生长抑制方面表现出更高的效率。 总之，MPEG 2k -PDLLA 4k -PLL 1k胶束比 MPEG 2k -PDLLA 1.7k更适合 DTX 递送，并且新型纳米制剂在乳腺癌治疗中显示出更好的抗肿瘤功效。
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