journal article·2023-11-10Open access

Self-Assembled Lenalidomide/AIE Prodrug Nanobomb for Tumor Imaging and Cancer Therapy

Zhijian Mai, Nengjie Cao, Erzhuo Cheng, Zhiwen Zeng, Yancong Feng, Yao Wang, Paddy J. French, Yi-Kuen Lee, Haihong Yang, Bin Yang, Hao Li, Guofu Zhou

ACS Applied Nano Materials· Volume 6· Issue 21

Abstract

To develop multifunctional small-molecule prodrugs is highly desirable for cancer treatment but remains challenging in intrinsic traceability. As an acid-cleavable linkage, a Schiff bases benefiting from its distinctive fluorescence quenching ability was selected to prepare a small-molecule prodrug with cancer-targeted and self-indicating. In this study, we designed and developed a multifunctional self-assembled nanobomb of amphiphilic TPE-Lenalidomide prodrug, which comprises a hydrophobic aggregation-induced emission (AIE) probe 4-(1,2,2-triphenylvinyl)benzaldehyde (TPE-CHO) and a hydrophilic anticancer drug Lenalidomide via a Schiff base linkage. We investigated the synergistic effect of d-PET and C═N isomerization which would keep the fluorescence of TPE-Lenalidomide in the “always off” state by density functional theory (DFT) calculation. Once reaching the pathological site, such a vesicular nanobomb of TPE-Lenalidomide will be acidolyzed to release the AIE probe and Lenalidomide molecules simultaneously, consequently realizing high-efficiency effects of tumor imaging and cancer therapy (cell viability: normal cell L929, ∼79.49%; cancer cell 4T1, ∼27.08%; p = 0.000118). This work may pave an avenue to prepare small-molecule prodrugs for tumor-targeted diagnosis and cancer therapy.
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Research context

OpenAlex topics: Advanced biosensing and bioanalysis techniques · Supramolecular Self-Assembly in Materials · Luminescence and Fluorescent Materials

SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.

Affiliations

Guangdong Provincial Key Laboratory of Optical Information Materials and Technology, Institute of Electronic Paper Displays, South China Academy of Advanced Optoelectronics, South China Normal University, Guangzhou 510006, P. R. China

National Center for International Research on Green Optoelectronics, South China Normal University, Guangzhou 510006, P. R. China

The Sixth Affiliated Hospital of Guangzhou Medical University, Qingyuan People’s Hospital; School of Biomedical Engineering, Guangzhou Medical University, Guangzhou 511436, P. R. China

BE Laboratory, EWI, Delft University of Technology, Delft 2628CD, The Netherland

Department of Mechanical & Aerospace Engineering, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong Special Administrative Region 999077, P. R. China

Department of Electronic & Computer Engineering, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong Special Administrative Region 999077, P. R. China

Department of Thoracic Oncology, State Key Laboratory of Respiratory Diseases, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou, 510006, P. R. China

Funding

Science and Technology Planning Project of Guangdong Province · Basic and Applied Basic Research Foundation of Guangdong Province · Department of Education of Guangdong Province · Guangzhou Municipal Science and Technology Project · Special Fund Project for Science and Technology Innovation Strategy of Guangdong Province · National Natural Science Foundation of China · Higher Education Discipline Innovation Project · South China Normal University · Guangdong Provincial Key Laboratory of Optical Information Materials and Technology · MOE International Laboratory for Optical Information Technologies

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