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A water-soluble nucleolin aptamer-paclitaxel conjugate for tumor-specific targeting in ovarian cancer
Fangfei Li1, Jun Lu1, Jin Liu2
1Institute of Precision Medicine and Innovative Drug Discovery (PMID), School of Chinese Medicine, Hong Kong Baptist University, Hong Kong SAR, 999077, China.
Abstract:
Paclitaxel (PTX) is among the most commonly used first-line drugs for cancer chemotherapy. However, its poor water solubility and indiscriminate distribution in normal tissues remain clinical challenges. Here we design and synthesize a highly water-soluble nucleolin aptamer-paclitaxel conjugate (NucA-PTX) that selectively delivers PTX to the tumor site. By connecting a tumor-targeting nucleolin aptamer (NucA) to the active hydroxyl group at 2' position of PTX via a cathepsin B sensitive dipeptide bond, NucA-PTX remains stable and inactive in the circulation. NucA facilitates the uptake of the conjugated PTX specifically in tumor cells. Once inside cells, the dipeptide bond linker of NucA-PTX is cleaved by cathepsin B and then the conjugated PTX is released for action. The NucA modification assists the selective accumulation of the conjugated PTX in ovarian tumor tissue rather than normal tissues, and subsequently resulting in notably improved antitumor activity and reduced toxicity.
Insights
This study developed a novel aptamer-paclitaxel conjugate (NucA-PTX) for targeted cancer therapy. This conjugate improves paclitaxel delivery to tumors, enhancing efficacy and reducing side effects.
Area of Science:
- Biochemistry
- Nanotechnology
- Oncology
Background:
- Paclitaxel (PTX) is a vital chemotherapy drug but faces challenges with poor water solubility and non-specific distribution.
- Targeted drug delivery systems are needed to improve PTX efficacy and minimize toxicity in cancer treatment.
Purpose of the Study:
- To design and synthesize a water-soluble nucleolin aptamer-paclitaxel conjugate (NucA-PTX) for selective tumor targeting.
- To evaluate the efficacy and safety of NucA-PTX in delivering paclitaxel to cancer cells.
Main Methods:
- Synthesis of a NucA-PTX conjugate using a cathepsin B-sensitive dipeptide linker.
- Assessment of NucA-PTX stability, cellular uptake, and drug release mechanisms.
- Evaluation of NucA-PTX antitumor activity and toxicity in ovarian tumor models.
Main Results:
- The NucA-PTX conjugate demonstrated high water solubility and stability in circulation.
- NucA-PTX exhibited selective uptake and drug release in tumor cells via cathepsin B cleavage.
- NucA-PTX significantly improved antitumor activity and reduced toxicity in ovarian tumor tissues compared to free PTX.
Conclusions:
- The nucleolin aptamer-paclitaxel conjugate (NucA-PTX) offers a promising strategy for targeted cancer chemotherapy.
- NucA-PTX enhances drug delivery to tumors, leading to improved therapeutic outcomes and reduced systemic toxicity.
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