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Polymers · 2022 ·Vol. 14 ·期 21 ·4515 · IF 4.967

Tumor-Targeting Polymer–Drug Conjugate for Liver Cancer Treatment In Vitro

Jiankun Xu,Shanmeng Lin,Hao Hu,Qi Xing,Jin Geng

Bufalin (buf) has poor solubility in aqueous solution, poor tumor targeting, and many non-specific toxic and side effects. The advantages of high-molecular-weight polymer conjugates are that they can improve the water solubility of buf, prolong plasma half-life, and reduce non-specific toxicity. A novel water-soluble polymer–drug conjugate with buf and fluorescein pendants was prepared by the combination of reversible addition-fragmentation transfer (RAFT) polymerization and click chemistry. Its anticancer performance and cellular uptake behavior against liver cancer were investigated in vitro. The polymer–buf conjugates exhibit controlled release and tumor-targeting capabilities, showing promise for clinical applications.Keywords:polymer–drug conjugate;liver cancer;esterase responsive;bufalin

研究领域: 药学 · 肿瘤学
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FERROELECTRICS · 2021 · IF 0.62

Synthesis of MoS2 nanosheets drug delivery system and its drug release behaviors

Feng Wang,Fang-Yuan Lv,Kui-Long Liu,Zhi-Hao Li,Shu Niu,Yun-Yi Zhang,Hai-Lin Cong,You-Qing Shen,Bing Yu

A MoS2 nanosheets drug delivery system with photothermal conversion ability was synthesized. The drug loading content of the synthesized was as high as 24.5%. The drug HCPT was modified by lipoic acid (LA) and connected onto MoS2 nanosheets through S-Mo bond, which is more stable than physical adsorption. Due to the ester bond between HCPT and MoS2 nanosheets, the drug delivery system could responsively release HCPT when exposed to esterase.

研究领域: 材料科学与工程 · 生物医学工程 · 药剂学
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Journal of Materials Chemistry B · 2023 ·Vol. 11 ·期 38 ·9246-9259 · IF 7

Exploring release mechanisms by disrupting π–π stacking regions in stable micelles

Fusheng Zhang,Gongcui Pei,Baihao Huang,Jianchang Xu,Lijuan Zhang

π–π stacking strategies can enhance the stability performance of delivery platforms but are often restricted by incomplete drug release performance, even with the help of crosslinking strategies. Therefore, there has been considerable interest in enhancing the drug release performance by disrupting the π–π stacking region (structural rearrangements). Herein, we synthesized poly(3-(isobutyloxy)-2-oxopropyl benzoate)-b-poly(2-hydroxybutyl methacrylate)-co-poly((ethylene glycol)methylether methacrylate) [PBOOPMA-b-P(HBMA-co-PEGMA), PHB] and revealed the drug release mechanism of PHB-based micelles. The structural rearrangements derived from the crosslinking strategy were revealed to improve the early release performance by 43–55% using micellar dissolutions. Moreover, the esterase-responsive strategy was elucidated to induce reassembly with 77–79% size variation, intensifying the structural rearrangements, which was also synergistic with the crosslinking strategy. Based on the advantages of improving drug release performance, the esterase-responsive strategy was considered a promising candidate for enhancing late release performance. Meanwhile, it is believed that such responsive modulation (crosslinking, esterase-responsive) in the π–π stacking region will become highly promising for subsequent research. Finally, the biosafety of 95.81% at 400 mg L−1 and drug cytotoxicity of IC50 ≈ 2.5 mg L−1 of PHB-EDE@CPT were also validated, confirming the broad application prospects of PHB-based crosslinked micelles.

研究领域: 药剂学 · 生物材料科学
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Journal of the American Chemical Society · 2012 · IF 9.907

Cholinesterase-Responsive Supramolecular Vesicle

Dong-Sheng Guo,Kui Wang,Yi-Xuan Wang,Yu Liu

Enzyme-responsive, amphiphilic self-assembly represents one of the increasingly significant topics in biomaterials research and finds feasible applications to the controlled release of therapeutic agents at specific sites where the target enzyme is located. The supramolecular approach, using “superamphiphiles”, provides a smart way to fabricate drug delivery systems responsive to enzymatic catalysis. In this work based on the concept of supramolecular chemistry, we report an enzyme-responsive vesicle using p-sulfonatocalix[4]arene as the macrocyclic host and natural enzyme-cleavable myristoylcholine as the guest molecule. The complexation of p-sulfonatocalix[4]arene with myristoylcholine directs the formation of a supramolecular binary vesicle, which is dissipated by cholinesterase with high specificity and efficiency. Cholinesterase is a key protein overexpressed in Alzheimer’s disease, and therefore, the present system may have potential for the delivery of Alzheimer’s disease drugs.

研究领域: 生物材料 · 医学 · 超分子化学
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Nanomedicine-Nanotechnology Biology and Medicine · 2022 · IF 6.458

Esterase-responsive and size-optimized prodrug nanoparticles for effective intracranial drug delivery and glioblastoma treatment

Zhang Ye,Lun Gao,Jiayang Cai,Yixuan Wang,Yong Li,Shiao Tong,Tengfeng Yan,Qian Sun,Yangzhi Qi,Yang Xu,Hongxiang Jiang,Si Zhang,Linyao Zhao,Shenqi Zhang,Qianxue Chen

Glioblastoma multiforme (GBM) is the intracranial malignancy with the highest rates of morbidity and mortality. Chemotherapy is often ineffective against GBM due to the presence of the blood–brain barrier (BBB); however, the application of nanotechnology is expected to overcome this limitation. Poly(lactic-co-glycolic acid) (PLGA) is a degradable and nontoxic functional polymer with good biocompatibility that is widely used in the pharmaceutical industry. Previous studies have shown that the ability of PLGA nanoparticles (NPs) to penetrate the BBB is largely determined by their size; however, determination of the optimal PLGA NP size requires further research. Here, we report a tandutinib-based prodrug (proTan), which responds to the GBM microenvironment , that was combined with NPs to overcome the BBB. AMD3100-PLGA NPs loaded with proTan inhibited tumor growth and effectively prolonged the survival of tumor-bearing mice.

CAS / MDL: 62669-70-9 51805-45-9
研究领域: 药学 · 纳米技术 · 肿瘤学 · 神经科学
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