International Journal of Nanomedicine (Apr 2020)
Targeted Prodrug-Based Self-Assembled Nanoparticles for Cancer Therapy
Abstract
Weiwei Wang,1 Junting Fan,2 Guang Zhu,1 Jing Wang,1 Yumei Qian,1 Hongxia Li,1 Jianming Ju,3 Lingling Shan1 1Institute of Pharmaceutical Biotechnology, School of Biology and Food Engineering, Key Laboratory of Spin Electron and Nanomaterials of Anhui Higher Education Institutes, Suzhou University, Suzhou 234000, People’s Republic of China; 2Department of Pharmaceutical Analysis, School of Pharmacy, Nanjing Medical University, Nanjing 211166, People’s Republic of China; 3Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, People’s Republic of ChinaCorrespondence: Lingling Shan; Junting Fan Email [email protected]; [email protected]: Targeted prodrug has various applications as drug formulation for tumor therapy. Therefore, amphoteric small-molecule prodrug combined with nanoscale characteristics for the self-assembly of the nano-drug delivery system (DDS) is a highly interesting research topic.Methods and Results: In this study, we developed a prodrug self-assembled nanoplatform, 2-glucosamine-fluorescein-5(6)-isothiocyanate-glutamic acid-paclitaxel (2DA-FITC-PTX NPs) by integration of targeted small molecule and nano-DDS with regular structure and perfect targeting ability. 2-glucosamine (DA) and paclitaxel were conjugated as the targeted ligand and anti-tumor chemotherapy drug by amino acid group. 2-DA molecular structure can enhance the targeting ability of prodrug-based 2DA-FITC-PTX NPs and prolong retention time, thereby reducing the toxicity of normal cell/tissue. The fluorescent dye FITC or near-infrared fluorescent dye ICG in prodrug-based DDS was attractive for in vivo optical imaging to study the behavior of 2DA-FITC-PTX NPs. In vitro and in vivo results proved that 2DA-FITC-PTX NPs exhibited excellent targeting ability, anticancer activity, and weak side effects.Conclusion: This work demonstrates a new combination of nanomaterials for chemotherapy and may promote prodrug-based DDS clinical applications in the future.Keywords: targeted prodrug, nanoplatform, NIR imaging, chemotherapy