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Updated: May 18, 2026

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Targeting and delivery of platinum-based anticancer drugs
1State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, State Key Laboratory of Analytical Chemistry for Life Science, Nanjing 210093, P. R. China.
Abstract:
Platinum-based anticancer drugs occupy a crucial role in the treatment of various malignant tumours. However, the efficacy and applicability of platinum drugs are heavily restricted by severe systemic toxicities and drug resistance. Different drug targeting and delivery (DTD) strategies have been developed to prevent the shortcomings of platinum-based chemotherapy. These approaches can be roughly categorized into two groups; namely, active and passive tactics. Active DTD is realized through specific molecular interactions between the drugs and cell or tissue elements, while passive DTD is achieved by exploiting the enhanced permeability and retention effect in tumour tissues. The principal methods for active DTD include conjugation of platinum drugs with selective targeting moieties or encapsulation of platinum drugs in host molecules. Bioactive substances such as hormones, carbohydrates, bisphosphonates, peptides and proteins are commonly used in active DTD. Passive DTD generally involves the fabrication of functionalized polymers or nanoparticles and the subsequent conjugation of platinum drugs with such entities. Polymeric micelles, liposomes, nanotubes and nanoparticles are frequently used in passive DTD. In some cases, both active and passive mechanisms are involved in one DTD system. This review concentrates on various targeting and delivery techniques for improving the efficacy and reducing the side effects of platinum-based anticancer drugs. The content covers most of the related literatures published since 2006. These innovative tactics represent current state-of-the-art developments in platinum-based anticancer drugs.
Insights
Platinum-based chemotherapy faces challenges with toxicity and resistance. Novel drug targeting and delivery (DTD) strategies, including active and passive approaches, aim to enhance efficacy and reduce side effects of these vital anticancer drugs.
Area of Science:
- Oncology
- Pharmacology
- Biotechnology
Background:
- Platinum-based anticancer drugs are essential for treating various cancers.
- Their clinical use is limited by severe systemic toxicities and acquired drug resistance.
- Drug targeting and delivery (DTD) strategies are crucial for overcoming these limitations.
Purpose of the Study:
- To review and summarize recent advancements in DTD strategies for platinum-based anticancer drugs.
- To highlight techniques that improve therapeutic efficacy and minimize adverse effects.
- To cover literature published since 2006, focusing on state-of-the-art developments.
Main Methods:
- Categorization of DTD strategies into active and passive approaches.
- Active DTD involves specific molecular interactions (e.g., conjugation with targeting moieties, encapsulation in host molecules using bioactive substances).
- Passive DTD utilizes the enhanced permeability and retention (EPR) effect (e.g., via nanoparticles, liposomes, polymeric micelles).
Main Results:
- Active DTD employs targeting moieties like hormones, carbohydrates, peptides, and proteins.
- Passive DTD utilizes nanocarriers such as nanoparticles, liposomes, and nanotubes.
- Combined active and passive mechanisms are also employed in integrated DTD systems.
Conclusions:
- Innovative DTD strategies significantly enhance the efficacy of platinum-based anticancer drugs.
- These advanced delivery systems effectively reduce systemic toxicities and combat drug resistance.
- Current research focuses on sophisticated targeting and delivery techniques for improved cancer chemotherapy.
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