BACKGROUND 3-(2-Nitrophenyl) propionic acid-paclitaxel (NPPA-PTX) is a paclitaxel (PTX) bioreductive prodrug synthesized by our lab. We hypothesize that NPPA-PTX can self-assemble to form nanoparticles (NPs). MATERIALS AND METHODS In the present research, the theoretical partition coefficient (XlogP) and Hansen solubility parameters of NPPA-PTX were calculated. NPPA-PTX nanoparticles prepared by NPPA-PTX and DSPE-PEG (NPPA-PTX:DSPE-PEG =1:0.1, w/w) (NPPA-PTX@PEG NPs) were prepared and characterized. The cellular uptake, in vitro antitumor activity, in vivo targeting effect, tumor distribution, in vivo antitumor activity, and safety of NPPA-PTX@PEG NPs were investigated. RESULTS Our results indicate that NPPA-PTX can self-assemble to form NPPA-PTX@PEG NPs. Both the cellular uptake and safety of NPPA-PTX@PEG NPs were higher than those of Taxol. NPPA-PTX@PEG NPs could target tumor tissues by a passive targeting effect. In tumor tissues, NPPA-PTX@PEG NPs could completely transform into active PTX. The in vivo antitumor activity of NPPA-PTX@PEG NPs was confirmed in MDA-MB-231 tumor-bearing nude mice. CONCLUSION The bioreductive prodrug NPPA-PTX could self-assemble to form NPs. The safety and antitumor activity of NPPA-PTX@PEG were confirmed in our in vitro and in vivo experiments. The NPPA-PTX@PEG NPs developed in this study could offer a new way of preparing bioreductive prodrug, self-assembled NPs suitable for antitumor therapy.

中文翻译：

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生物还原性前药 3-(2-硝基苯基) 丙酸-紫杉醇纳米粒子 (NPPA-PTX NPs) 对 MDA-MB-231 细胞的抗肿瘤活性：体外和体内。

背景技术3-(2-硝基苯基)丙酸-紫杉醇(NPPA-PTX)是本实验室合成的紫杉醇(PTX)生物还原性前药。我们假设 NPPA-PTX 可以自组装形成纳米粒子 (NPs)。材料与方法在本研究中，计算了NPPA-PTX的理论分配系数（XlogP）和汉森溶解度参数。制备并表征了由NPPA-PTX和DSPE-PEG制备的NPPA-PTX纳米颗粒（NPPA-PTX:DSPE-PEG =1:0.1，w/w）（NPPA-PTX@PEG NPs）。研究了 NPPA-PTX@PEG NPs 的细胞摄取、体外抗肿瘤活性、体内靶向作用、肿瘤分布、体内抗肿瘤活性和安全性。结果我们的结果表明NPPA-PTX可以自组装形成NPPA-PTX@PEG NPs。NPPA-PTX@PEG NPs 的细胞摄取和安全性均高于紫杉醇。NPPA-PTX@PEG NPs可以通过被动靶向作用靶向肿瘤组织。在肿瘤组织中，NPPA-PTX@PEG NPs可以完全转化为活性PTX。NPPA-PTX@PEG NPs 的体内抗肿瘤活性在 MDA-MB-231 荷瘤裸鼠中得到证实。结论生物还原性前药NPPA-PTX可以自组装形成NPs。NPPA-PTX@PEG 的安全性和抗肿瘤活性在我们的体外和体内实验中得到证实。本研究开发的NPPA-PTX@PEG NPs可以提供一种制备适合抗肿瘤治疗的生物还原性前药、自组装NPs的新方法。结论生物还原性前药NPPA-PTX可以自组装形成NPs。NPPA-PTX@PEG 的安全性和抗肿瘤活性在我们的体外和体内实验中得到证实。本研究开发的NPPA-PTX@PEG NPs可以提供一种制备适合抗肿瘤治疗的生物还原性前药、自组装NPs的新方法。结论生物还原性前药NPPA-PTX可以自组装形成NPs。NPPA-PTX@PEG 的安全性和抗肿瘤活性在我们的体外和体内实验中得到证实。本研究开发的NPPA-PTX@PEG NPs可以提供一种制备适合抗肿瘤治疗的生物还原性前药、自组装NPs的新方法。