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Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
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CRGDK-Functionalized PAMAM-Based Drug-Delivery System with High Permeability
Dongfang Liu1, Chao Wang1, Jian Yang1
1Jiangsu Key Laboratory of Molecular and Functional Imaging, Department of Radiology, Medical School, Zhongda Hospital, Southeast University, No. 87, Dingjiaqiao, Nanjing 210009, China.
ACS Omega
|May 5, 2020
Summary
This study developed small, peptide-functionalized nanoparticles for improved tumor drug delivery. These enhanced nanomedicines show better tumor penetration and higher anticancer efficacy compared to traditional treatments.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Drug Delivery
Background:
- Low tumor permeability of nanomedicines hinders effective cancer therapy.
- Strategies like size reduction and peptide functionalization can enhance nanomedicine tumor penetration.
Purpose of the Study:
- To design and evaluate poly(amidoamine) (PAMAM) nanoparticles functionalized with the CRGDK peptide for improved tumor drug delivery.
- To assess the efficacy of these peptide-functionalized nanoparticles loaded with paclitaxel (PTX) against tumors.
Main Methods:
- Synthesized approximately 5 nm PAMAM nanoparticles.
- Functionalized nanoparticles with the CRGDK penetrating peptide.
- Covalently linked paclitaxel (PTX) to the carrier via a biocleavable ester bond.
- Compared cellular uptake, tumor accumulation, penetration, and antitumor efficiency with non-targeted nanoparticles and Taxol.
Main Results:
- CRGDK-functionalized nanoparticles demonstrated significantly higher cellular uptake.
- Enhanced tumor accumulation and penetration were observed in the targeted nanomedicine.
- The functionalized nanomedicine exhibited superior antitumor efficiency compared to non-targeted counterparts and Taxol.
Conclusions:
- Peptide-functionalized PAMAM-based nanomedicines show a feasible strategy to improve nanomedicine tumor accumulation and penetration.
- This approach holds promise for enhancing the therapeutic efficacy of nanomedicines in cancer treatment.
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