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苯硼酸 (PBA)
Journal of Materials Chemistry B · 2017 ·Vol. 5 ·期 15 ·2823-2831 · IF 4.543

Design and construction of self-hidden and pH-reversed targeting drug delivery nanovehicles via noncovalent interactions to overcome drug resistance

Dan Zhao,Xiaoqing Yi,Jiaqi Xu,Gongdao Yuan,Renxi Zhuo,Feng Li

Using the host–guest interaction between β-cyclodextrin (β-CD) and adamantane (Ad), and borate formation between phenylboronic acid (PBA) and cis-diols, a smart pH-responsible targeting drug delivery nanovehicle, PBA–PEG–CD/Ad-lys(Diol)–PCL, was prepared via one-step self-assembly. Under physiological conditions, the targeted PBA function could be restrained by binding PBA with diol components located at the interface of self-assemblies, and hydrophilic PEG segments could be shielded simultaneously. When the environmental pH decreased, the PBA groups could be unbound and exposed on the surface of self-assemblies, leading to recovery of its targeted function, as shown using fluorescence spectroscopy, in vitro cell toxicity, and uptake. Under acidic conditions, PBA–PEG–CD/Ad-lys(Diol)–PCL/Dox showed significantly increased uptake and toxicity toward HepG2 cells in comparison with the control group. The smart vehicles were further utilized to test their efficiency in overcoming drug resistance in chemotherapy. Compared with free Dox, PBA–PEG–CD/Ad-lys(Diol)–PCL delivered six times more Dox into MCF-7/ADR cells and showed greater toxicity toward the ADR cells. As a result, this may be a facile strategy toward constructing efficient targeting vehicles through the rational utilization of noncovalent interactions.

研究领域: 药剂学 · 纳米技术 · 药物递送系统 · 癌症研究
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ACS Applied Materials & Interfaces · 2025 · IF 8.2

Glucose-Responsive Self-Rolling Antioxidant Hydrogel Actuators for a Cell Culture Platform

Zhiyu Zheng,Ruxin Xiao,Xiaochen Ma,Ziqian Yu,Jiaxin Zeng,Liqiong Liao

Three-dimensional (3D) cell culture technology can mimic the physiological characteristics of tissues and organs, making it highly suitable for cell therapy, organ chips, and tissue engineering applications. However, achieving a uniform cell distribution within the 3D matrix while mitigating the effects of reactive oxygen species (ROS) accumulation generated during the 3D cell culture remains a critical challenge. Hydrogel actuators, with their excellent bioactivity and controllable self-rolling behavior, provide an optimal microenvironment for the 3D cell culture. To support normal cellular function, hydrogel actuators must be triggered by external stimuli that are biocompatible with the cell culture process. Glucose, a key intermediate in energy metabolism and biological processes, is ubiquitous in cell culture media and physiological systems. In this work, a glucose-responsive hydrogel actuator (AP@Que/gelatin) with controllable self-rolling behaviors and ROS scavenging capability was constructed for 3D cell culture, which consists of an active layer composed of phenylboronic acid (PBA)–quercetin (Que) complexes and a passive layer of a biocompatible gelatin hydrogel. The hydrogel actuator exhibited excellent glucose response performance, characterized by notable reswelling behavior, favorable ductility, and cytocompatibility. Its self-rolling behavior in high-glucose culture media was synchronized with cell adhesion timelines, enabling its application as a 2D-to-3D dynamic substrate for cell culture and expansion. Meanwhile, Que was released from the hydrogel actuator through the competitive reaction of PBA with glucose and Que. The formation of the 3D tubular architecture during cell culture facilitated cell growth, while the sustained release of Que effectively eliminated ROS generated during cell passaging. These findings highlight the potential of AP@Que/gelatin hydrogel actuators as an advanced platform for a 3D cell culture.

CAS / MDL: 26570-48-9
研究领域: 生物材料 · 组织工程 · 细胞培养技术 · 药物递送系统 · 生物执行器
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CHEMICAL ENGINEERING JOURNAL · 2024 · IF 13.3

Time-space regulating prodrug hydrogels for prevention of peritendinous adhesion

Zhipeng Ni,Haiying Zhou,Haojie Yu,Li Wang,Chenguang Ouyang,Jian Yang,Yanzhao Dong,Ahmad Alhaskawi,Tian Tu,Hui Lu

The bidirectional regulations of antiadhesion and regeneration are crucial for Achilles tendon injuries. However, the precise prevention and treatments of peritendinous adhesions both in time and space are still great challenges. Here, a series of time–space regulating prodrug (tannic acid (TA), epigallocatechin (EGC) and epigallocatechin gallate (EGCG)) hydrogels are designed for the prevention of peritendinous adhesion in Achilles tendon contusion and rupture injuries. In the term of space, the self-healing and deformable hydrogels prepared by crosslinking phenylboric acid (PBA) functionalized polyphosphazene (PZBA) with guar gum (GG) through ROS-responsive phenylborate ester (PBAE) can specifically aggregate to the high ROS sites via the ROS-responsive degradation and recombination of PBAE. Thus, providing support and acting as barriers to inhibit fibroblast proliferation. In the term of time, the prodrug strategy using ROS-responsive PBAE as bridging linker can achieve long-term anti-inflammatory effect over 2 weeks. Furthermore, the degradation time of hydrogels matched the course of peritendinous adhesion, thus achieved bidirectional regulations (decrease the gene expression of TGF-β1, COL-1 and COL-3 to antiadhesion in the early stage but increase them to promote regeneration in the late stage). This study presents a promising approach employing smart prodrug hydrogels with time–space regulating properties for prevention of peritendinous adhesion.

研究领域: 生物医学工程 · 药剂学 · 材料科学 · 组织工程
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