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Updated: Oct 1, 2025

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies
Published on: February 17, 2023
Emerging pro-drug and nano-drug strategies for gemcitabine-based cancer therapy
Haijie Han1,2,3, Su Li1,2, Yueyang Zhong1,2
1Eye Center, the Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou 310009, China.
Abstract:
Gemcitabine has been extensively applied in treating various solid tumors. Nonetheless, the clinical performance of gemcitabine is severely restricted by its unsatisfactory pharmacokinetic parameters and easy deactivation mainly because of its rapid deamination, deficiencies in deoxycytidine kinase (DCK), and alterations in nucleoside transporter. On this account, repeated injections with a high concentration of gemcitabine are adopted, leading to severe systemic toxicity to healthy cells. Accordingly, it is highly crucial to fabricate efficient gemcitabine delivery systems to obtain improved therapeutic efficacy of gemcitabine. A large number of gemcitabine pro-drugs were synthesized by chemical modification of gemcitabine to improve its biostability and bioavailability. Besides, gemcitabine-loaded nano-drugs were prepared to improve the delivery efficiency. In this review article, we introduced different strategies for improving the therapeutic performance of gemcitabine by the fabrication of pro-drugs and nano-drugs. We hope this review will provide new insight into the rational design of gemcitabine-based delivery strategies for enhanced cancer therapy.
Insights
Gemcitabine drug delivery faces challenges due to poor pharmacokinetics and toxicity. This review explores novel pro-drug and nano-drug strategies to enhance gemcitabine
Area of Science:
- Oncology
- Pharmacology
- Nanotechnology
Background:
- Gemcitabine is a key chemotherapy agent for solid tumors.
- Its clinical efficacy is limited by rapid deactivation, poor pharmacokinetics, and systemic toxicity.
- Challenges include deamination, deoxycytidine kinase (DCK) deficiencies, and altered nucleoside transporters.
Purpose of the Study:
- To review strategies for improving gemcitabine's therapeutic performance.
- To explore the design of novel gemcitabine delivery systems.
- To provide insights for enhanced cancer therapy using gemcitabine.
Main Methods:
- Review of existing literature on gemcitabine pro-drugs and nano-drugs.
- Analysis of chemical modification strategies for gemcitabine.
- Evaluation of gemcitabine-loaded nano-drug formulations.
Main Results:
- Pro-drug synthesis improves gemcitabine's biostability and bioavailability.
- Nano-drug formulations enhance gemcitabine delivery efficiency.
- These strategies aim to overcome gemcitabine's limitations.
Conclusions:
- Fabricating efficient gemcitabine delivery systems is crucial for improved cancer therapy.
- Pro-drugs and nano-drugs represent promising strategies to enhance gemcitabine's therapeutic efficacy.
- Further research into rational design of gemcitabine delivery systems is warranted.
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