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Theranostics 2017; 7(10):2652-2672. doi:10.7150/thno.19680 This issue Cite

Research Paper

A Novel MPEG-PDLLA-PLL Copolymer for Docetaxel Delivery in Breast Cancer Therapy

Liwei Tan, Jinrong Peng, Qian Zhao, Lan Zhang, Xichuan Tang, Lijuan Chen, Minyi Lei, Zhiyong Qian✉

State Key Laboratory of Biotherapy and Cancer Center, Collaborative Innovation Center of Biotherapy, West China Hospital, Sichuan University, Sichuan, China

✉ Corresponding author: Tel/Fax: +86-28-85501986, E-mail: anderson-qiancom

Citation:
Tan L, Peng J, Zhao Q, Zhang L, Tang X, Chen L, Lei M, Qian Z. A Novel MPEG-PDLLA-PLL Copolymer for Docetaxel Delivery in Breast Cancer Therapy. Theranostics 2017; 7(10):2652-2672. doi:10.7150/thno.19680. https://www.thno.org/v07p2652.htm
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Abstract

Graphic abstract

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.

Keywords: Docetaxel micelles, polymeric micelles, interaction, anti-tumor, drug loading capacity.

Citation styles

APA
Tan, L., Peng, J., Zhao, Q., Zhang, L., Tang, X., Chen, L., Lei, M., Qian, Z. (2017). A Novel MPEG-PDLLA-PLL Copolymer for Docetaxel Delivery in Breast Cancer Therapy. Theranostics, 7(10), 2652-2672. https://doi.org/10.7150/thno.19680.

ACS
Tan, L.; Peng, J.; Zhao, Q.; Zhang, L.; Tang, X.; Chen, L.; Lei, M.; Qian, Z. A Novel MPEG-PDLLA-PLL Copolymer for Docetaxel Delivery in Breast Cancer Therapy. Theranostics 2017, 7 (10), 2652-2672. DOI: 10.7150/thno.19680.

NLM
Tan L, Peng J, Zhao Q, Zhang L, Tang X, Chen L, Lei M, Qian Z. A Novel MPEG-PDLLA-PLL Copolymer for Docetaxel Delivery in Breast Cancer Therapy. Theranostics 2017; 7(10):2652-2672. doi:10.7150/thno.19680. https://www.thno.org/v07p2652.htm

CSE
Tan L, Peng J, Zhao Q, Zhang L, Tang X, Chen L, Lei M, Qian Z. 2017. A Novel MPEG-PDLLA-PLL Copolymer for Docetaxel Delivery in Breast Cancer Therapy. Theranostics. 7(10):2652-2672.

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