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Updated: Mar 19, 2026

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Core-shell nanocarriers with high paclitaxel loading for passive and active targeting.

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Modified nanocapsules with iRGD peptide show improved tumor targeting and penetration for enhanced chemotherapy delivery. This nanocarrier system offers a promising approach for effective cancer therapy.

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Area of Science:

  • Biomedical Engineering
  • Nanotechnology
  • Drug Delivery

Background:

  • Conventional nanoparticles suffer from rapid clearance and poor tumor selectivity.
  • iRGD peptide targets αVβ3 integrins and enhances cell membrane penetration.
  • Poorly water-soluble chemotherapy agents require effective delivery systems.

Purpose of the Study:

  • To develop iRGD-modified nanocapsules (iRGD-NCs) for enhanced paclitaxel (PTX) delivery.
  • To improve tumor targeting, penetration, and antitumor activity of PTX.
  • To evaluate the pharmacokinetic and safety profile of the developed nanocarriers.

Main Methods:

  • Preparation of core-shell nanocapsules (NCs) and iRGD-NCs with high drug payload for PTX.
  • In vitro and in vivo evaluation of tumor targeting and penetration.
  • Assessment of cytotoxicity, cellular uptake mechanisms (lipid raft-mediated, energy-dependent endocytosis), and pharmacokinetic parameters (AUC, MRT).

Main Results:

  • iRGD-NCs demonstrated improved tumor targeting and penetration compared to unmodified NCs.
  • PTX-loaded NCs (PTX-NCs) showed significantly enhanced antitumor activity.
  • PTX-NCs exhibited a 4-fold increase in AUC, an 8-fold prolonged MRT, and a >68-fold reduced elimination rate constant compared to commercial PTX.
  • NCs were cytocompatible, histocompatible, and non-toxic to healthy tissues.

Conclusions:

  • iRGD-modified nanocarriers offer efficient tumor targeting and penetration for enhanced chemotherapy.
  • The developed nanocarriers possess high drug-loading capacity and improve the pharmacokinetic profile of paclitaxel.
  • This nanocarrier system shows significant potential for improving cancer therapy outcomes.