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A versatile tumor-targeted drug-delivery system based on IR808-modified nanoparticles, its co-loading with PTX and
Yaoyao Guo1,2, Manzhen Li1, Xinxin Liu1
1Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China. xtaowang@163.com.
Abstract:
Nearly all antitumor drugs can benefit greatly from effective tumor-targeted delivery for improved therapeutic efficacy and reduced toxic side effects. However, the vast majority of tumor-targeting ligands can only target specific tumor cells that highly express the corresponding receptors and thus are only applicable to limited tumor types. Heptamethine cyanines with medium cyclohexene and medium Cl atoms, such as IR780 and IR808, have shown an unusual ability to indiscriminately accumulate into virtually all tumor types. In this study, IR808 was conjugated with DSPE-mPEG2000-NH2, and the resultant DSPE-PEG2000-IR808 (DP-IR808) in combination with TPGS successfully encapsulated paclitaxel (PTX) and immunomodulator R848 into nanoparticles with a small particle size of 150.20 nm, negative charge of -16.50 mV, rod-like morphology, and PTX loading content of 31.6%. The obtained DP-IR808@PTX-R848 NPs rapidly accumulated in 4T1 tumors with a tumor/liver fluorescence ratio of 1.71, and it demonstrated a significant photothermal effect and could be directly used for NIR imaging. The DP-IR808@PTX-R848 NPs achieved a high tumor inhibition rate of 94%, a mean survival time of >90 d, and a tumor-free survival percentage of 57%. To the best of our knowledge, this was the first time that nanoparticles were modified with heptamethylcyanine molecules. The nanoparticles system based on DSPE-PEG-IR808, which integrates tumor-targeted drug delivery, in vivo infrared imaging and photothermal therapy, is expected to become a versatile drug-delivery platform for tumor therapy.
Insights
This study developed novel nanoparticles using IR808 for broad tumor targeting. These nanoparticles effectively delivered chemotherapy and immunotherapy drugs, showing high tumor inhibition and prolonged survival in preclinical models.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Effective tumor-targeted drug delivery improves cancer therapy efficacy and reduces side effects.
- Current tumor-targeting ligands are limited to specific receptor-expressing tumors.
- Heptamethine cyanines like IR808 show broad tumor accumulation across various cancer types.
Purpose of the Study:
- To develop and evaluate novel nanoparticles for broad tumor targeting, combining drug delivery, imaging, and photothermal therapy.
- To conjugate IR808 with DSPE-PEG2000-NH2 to create DSPE-PEG2000-IR808 (DP-IR808) for nanoparticle formulation.
- To encapsulate paclitaxel (PTX) and R848 into DP-IR808 nanoparticles for combination therapy.
Main Methods:
- Conjugation of IR808 with DSPE-mPEG2000-NH2 to form DP-IR808.
- Encapsulation of paclitaxel (PTX) and R848 into DP-IR808 nanoparticles using TPGS.
- Characterization of nanoparticle size, charge, morphology, and drug loading.
- Evaluation of in vivo tumor accumulation, photothermal effect, NIR imaging, and therapeutic efficacy in 4T1 tumor models.
Main Results:
- DP-IR808@PTX-R848 nanoparticles exhibited optimal characteristics: 150.20 nm size, -16.50 mV charge, rod-like morphology, and 31.6% PTX loading.
- Rapid tumor accumulation was observed with a high tumor/liver fluorescence ratio (1.71).
- Significant photothermal effect and NIR imaging capability were demonstrated.
- Achieved a 94% tumor inhibition rate, mean survival time >90 days, and 57% tumor-free survival.
Conclusions:
- This study presents the first nanoparticle system modified with heptamethine cyanine (IR808).
- The DSPE-PEG-IR808 based nanoparticles effectively integrate tumor-targeted drug delivery, in vivo infrared imaging, and photothermal therapy.
- This versatile platform holds promise for advanced tumor therapy strategies.
