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INTRODUCTION

Poor cell uptake and incomplete intracellular drug release are the two major challenges for polymeric prodrug-based drug delivery systems (PPDDSs) in cancer treatment.

METHODS

Herein, a PPDDS with pH-induced surface charge-reversal and reactive oxygen species (ROS) amplification for ROS-triggered self-accelerating drug release was developed, which was formed by encapsulating a ROS generation agent (vitamin K3 (VK3)) in pH/ROS dual-sensitive polymetric prodrug (PEG--P(LL--TK-PTX)-(LL--DMA)) based micelle nanoparticles (denoted as PVD-NPs).

RESULTS

The surface charge of the PVD-NPs can change from negative to positive for enhanced cell uptake in response to tumor extracellular acidity pH. After internalization by cancer cells, PVD-NPs demonstrate dual drug release in response to intracellular ROS-rich conditions. In addition, the released VK3 can produce ROS under the catalysis by NAD(P)H:quinone oxidoreductase-1, which facilitates tumor-specific ROS amplification and drug release selectively in cancer cells to enhance chemotherapy.

CONCLUSION

Both in vitro and in vivo experiments demonstrated that the PVD-NPs showed significant antitumor activity in human prostate cancer.

INTRODUCTION

Poor cell uptake and incomplete intracellular drug release are the two major challenges for polymeric prodrug-based drug delivery systems (PPDDSs) in cancer treatment.

METHODS

RESULTS

CONCLUSION

Both in vitro and in vivo experiments demonstrated that the PVD-NPs showed significant antitumor activity in human prostate cancer.

简介

细胞摄取率低和不完全的细胞内药物释放是聚合物前药药物递送系统（PPDDS）在癌症治疗中面临的两个主要挑战。

方法

本文开发了一种具有 pH 诱导的表面电荷反转和活性氧（ROS）放大功能的 PPDDS，用于 ROS 触发的自加速药物释放，该系统由 ROS 生成剂（维生素 K3（VK3））包封在 pH/ROS 双重敏感聚合物前药（PEG--P（LL--TK-PTX）-（LL--DMA））基胶束纳米粒（表示为 PVD-NPs）中形成。

结果

PVD-NPs 的表面电荷可以从负变为正，以响应肿瘤细胞外酸度 pH 增强细胞摄取。被癌细胞内化后，PVD-NPs 在响应细胞内富含 ROS 的条件下表现出双重药物释放。此外，释放的 VK3 在 NAD(P)H：醌氧化还原酶-1 的催化下可以产生 ROS，这有助于肿瘤特异性 ROS 放大和选择性地在癌细胞中释放药物，以增强化疗效果。