Charge Regulation of Self-Assembled Tubules by Protonation for Efficiently Selective and Controlled Drug Delivery
Liping Huang,
Hang Zhang,
Shanshan Wu,
Xin Xu,
Lingling Zhang,
Hongbing Ji,
Liang He,
Yuna Qian,
Zhiyong Wang,
Yongming Chen,
Jianliang Shen,
Zong-Wan Mao,
Zhegang Huang
Affiliations
Liping Huang
Fine Chemical Industry Research Insitute, Key Laboratory for Polymeric Composite & Functional Materials of Ministry of Education and MOE Key Laboratory of Bioinorganic and Synthetic Chemistry Lab, School of Chemistry, Sun Yat-sen University, Guangzhou 510275, PR China
Hang Zhang
Fine Chemical Industry Research Insitute, Key Laboratory for Polymeric Composite & Functional Materials of Ministry of Education and MOE Key Laboratory of Bioinorganic and Synthetic Chemistry Lab, School of Chemistry, Sun Yat-sen University, Guangzhou 510275, PR China
Shanshan Wu
Fine Chemical Industry Research Insitute, Key Laboratory for Polymeric Composite & Functional Materials of Ministry of Education and MOE Key Laboratory of Bioinorganic and Synthetic Chemistry Lab, School of Chemistry, Sun Yat-sen University, Guangzhou 510275, PR China
Xin Xu
Fine Chemical Industry Research Insitute, Key Laboratory for Polymeric Composite & Functional Materials of Ministry of Education and MOE Key Laboratory of Bioinorganic and Synthetic Chemistry Lab, School of Chemistry, Sun Yat-sen University, Guangzhou 510275, PR China
Lingling Zhang
Fine Chemical Industry Research Insitute, Key Laboratory for Polymeric Composite & Functional Materials of Ministry of Education and MOE Key Laboratory of Bioinorganic and Synthetic Chemistry Lab, School of Chemistry, Sun Yat-sen University, Guangzhou 510275, PR China
Hongbing Ji
Fine Chemical Industry Research Insitute, Key Laboratory for Polymeric Composite & Functional Materials of Ministry of Education and MOE Key Laboratory of Bioinorganic and Synthetic Chemistry Lab, School of Chemistry, Sun Yat-sen University, Guangzhou 510275, PR China
Liang He
Fine Chemical Industry Research Insitute, Key Laboratory for Polymeric Composite & Functional Materials of Ministry of Education and MOE Key Laboratory of Bioinorganic and Synthetic Chemistry Lab, School of Chemistry, Sun Yat-sen University, Guangzhou 510275, PR China
Yuna Qian
State Key Laboratory of Ophthalmology, Optometry and Vision Science, School of Ophthalmology and Optometry, School of Biomedical Engineering, Wenzhou Medical University, Wenzhou 325027, PR China; Wenzhou Institute, University of Chinese Academy of Sciences, Wenzhou 325001, PR China
Zhiyong Wang
Key Laboratory for Polymeric Composite & Functional Materials of Ministry of Education, School of Materials Science and Engineering, Sun Yat-sen University, Guangzhou 510275, PR China
Yongming Chen
Key Laboratory for Polymeric Composite & Functional Materials of Ministry of Education, School of Materials Science and Engineering, Sun Yat-sen University, Guangzhou 510275, PR China
Jianliang Shen
State Key Laboratory of Ophthalmology, Optometry and Vision Science, School of Ophthalmology and Optometry, School of Biomedical Engineering, Wenzhou Medical University, Wenzhou 325027, PR China; Wenzhou Institute, University of Chinese Academy of Sciences, Wenzhou 325001, PR China; Corresponding author
Zong-Wan Mao
Fine Chemical Industry Research Insitute, Key Laboratory for Polymeric Composite & Functional Materials of Ministry of Education and MOE Key Laboratory of Bioinorganic and Synthetic Chemistry Lab, School of Chemistry, Sun Yat-sen University, Guangzhou 510275, PR China; Corresponding author
Zhegang Huang
Fine Chemical Industry Research Insitute, Key Laboratory for Polymeric Composite & Functional Materials of Ministry of Education and MOE Key Laboratory of Bioinorganic and Synthetic Chemistry Lab, School of Chemistry, Sun Yat-sen University, Guangzhou 510275, PR China; Corresponding author
Summary: Despite the success for targeted delivery in the body, the efficient release without side effects caused by residual drug remains a challenge. For reducing residual drug, the pH-responsive carriers were prepared by self-assembly from aromatic macrocycles, which were non-toxic and biocompatible. The inner surroundings of aromatic macrocycles could be protonated positively by acid inducing the separation of neighboring macrocycles. Thus, Dox-loaded carriers successfully inhibited the proliferation of carcinoma cells (HepG2 and 4T1) rather than normal cells (HL7702). The effects were further proved in vivo without systemic cytotoxicity. Notably, the responsive environment for drug release depended on the concentration of carriers. Particularly, drug release was promoted by carrier separation. Carrier 2 exhibited preferable anticancer efficacy than carrier 1 due to the efficient release of Dox by full separation of the carrier. Collectively, we have developed a novel strategy serving as a selective and controlled drug release platform for cancer therapeutics. : Drug Delivery System; Supramolecular Materials; Biomaterials Subject Areas: Drug Delivery System, Supramolecular Materials, Biomaterials