4.8 Article

Bioinspired Microenvironment Responsive Nanoprodrug as an Efficient Hydrophobic Drug Self-Delivery System for Cancer Therapy

Journal

ACS APPLIED MATERIALS & INTERFACES
Volume 13, Issue 29, Pages 33926-33936

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acsami.1c09612

Keywords

Bioinspired nanoprodrug; self-delivery; anti-cancer; cost-effective; artemisinin

Funding

  1. National Key Research and Development Program of China Stem Cell and Translational Research [2016YFA0101202]
  2. National Natural Science Foundation of China [21571168, 21271163, 31471268]
  3. Anhui Key Research and Development Program [201904a07020092]
  4. CAS Hefei Science Center [2016HSC-IU011]

Ask authors/readers for more resources

A bioinspired coordination-driven self-assembly strategy was developed to manufacture artemisinin-based nanoprodrug, which showed high drug loading efficiency and low preparation complexity. The nanoprodrug demonstrated favorable characteristics for cancer targeting in vivo.
Artemisinin compounds have shown satisfactory safety records in anti-malarial clinical practice over decades and have revealed value as inexpensive anti-tumor adjuvant chemotherapeutic drugs. However, the rational design and precise preparation of nanomedicines based on the artemisinin drugs are still limited due to their non-aromatic and fragile chemical structure. Herein, a bioinspired coordination-driven self-assembly strategy was developed to manufacture the artemisinin-based nanoprodrug with a significantly increased drug loading efficacy (similar to 70 wt %) and decreased preparation complexity compared to conventional nanodrugs. The nano-prodrug has suitable size distribution and robust colloidal stability for cancer targeting in vivo. The nanoprodrug was able to quickly disassemble in the tumor microenvironment with weak acidity and a high glutathione concentration, which guarantees a better tumor inhibitory effect than direct administration and fewer side effects on normal tissues in vivo. This work highlights a new strategy to harness a robust, simplified, organic solvent-free, and highly repeatable route for nanoprodrug manufacturing, which may offer opportunities to develop cost-effective, safe, and clinically available nanomedicines.

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