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Functionalizing Sgc8-Paclitaxel Conjugates with F-Base Modifications: Targeted Drug Delivery with Optimized Cardiac
Yue Ma1, Xianying Liao1, Guiping Lu1
1Department of Cardiology, Ren ji Hospital, State Key Laboratory of Oncogenes and Related Genes, School of Medicine, Shanghai Jiao Tong University, Shanghai, 200127, China.
Abstract:
Recent advancements in cancer treatment have improved patient prognoses, but chemotherapy induced cardiotoxicity remains a prevalent concern. This study explores the potential of F-base-modified aptamers for targeted drug delivery, focusing on their impact on cardiotoxicity. From the phosphoramidite, F-base-functionalized Sgc8-F23 was prepared in an automated and programmable way, which was further reacted with paclitaxel (PTX) to give the F-base- modified aptamer Sgc8-paclitaxel conjugates (Sgc8-F23-PTX) efficiently. The conjugate exhibited prolonged circulation time and enhanced efficacy as a precision anticancer drug delivery system. Echocardiographic assessments revealed no exacerbation of cardiac dysfunction after myocardial infarction (MI) and no pathological changes or increased apoptosis in non-infarcted cardiac regions. Autophagy pathway analysis showed no discernible differences in Sgc8-F23-PTX-treated cardiomyocytes compared with controls, in contrast to the increased autophagy with nanoparticle albumin-bound-paclitaxel (Nab-PTX). Similarly, apoptosis analysis showed no significant differences. Moreover, Sgc8-F23-PTX exhibited no inhibitory effect on hERG, hNav1.5, or hCav1.2 channels. These findings suggest the safety and efficacy of F-base-modified Sgc8 aptamers for targeted drug delivery with potential clinical applications. Further research is warranted for clinical translation and exploration of other drug carriers.
Insights
F-base-modified aptamers offer a safer way to deliver chemotherapy drugs, reducing cardiotoxicity. This precision drug delivery system shows promise for cancer treatment with minimal cardiac side effects.
Area of Science:
- Biochemistry
- Nanotechnology
- Cardiology
Background:
- Chemotherapy-induced cardiotoxicity is a significant challenge in cancer treatment.
- Targeted drug delivery systems aim to improve efficacy and reduce side effects.
Purpose of the Study:
- To evaluate the cardiotoxicity and efficacy of F-base-modified aptamer-paclitaxel conjugates (Sgc8-F23-PTX) as a targeted drug delivery system.
- To compare Sgc8-F23-PTX with nanoparticle albumin-bound paclitaxel (Nab-PTX) regarding cardiac safety.
Main Methods:
- Synthesis of F-base-functionalized Sgc8 aptamer and conjugation with paclitaxel (PTX).
- Assessment of cardiac function using echocardiography in a myocardial infarction model.
- Analysis of cardiomyocyte apoptosis and autophagy.
- Evaluation of ion channel effects (hERG, hNav1.5, hCav1.2).
Main Results:
- Sgc8-F23-PTX demonstrated prolonged circulation time and enhanced anticancer efficacy.
- No cardiotoxicity, pathological changes, or increased apoptosis were observed in non-infarcted cardiac regions.
- Sgc8-F23-PTX did not induce significant autophagy or apoptosis in cardiomyocytes, unlike Nab-PTX.
- No inhibitory effects on key cardiac ion channels were detected.
Conclusions:
- F-base-modified Sgc8 aptamers represent a safe and effective platform for targeted anticancer drug delivery.
- This approach shows potential for reducing chemotherapy-induced cardiotoxicity in clinical applications.
- Further research is needed for clinical translation and exploring other drug carriers.
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