Related Experiment Video
Updated: Sep 14, 2025
Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
Published on: February 8, 2017
Development of a KRP-based pH-responsive drug delivery system for solid tumors
Yu Wu1, Jiahong Pei2, Hanzhuo Wang3
1Department of Oral and Maxillofacial Surgery, Guangzhou Institute of Pediatrics, Guangzhou Women and Children's Medical Center, Guangzhou Medical University, Guangdong Province Clinical Research Center for Child Health, Guangzhou, China.
A novel pH-responsive drug delivery system, KRP-Hyd-DOX, was developed using cell-penetrating peptides (CPPs) and doxorubicin (DOX). This system enhances drug efficacy and reduces side effects by improving cellular uptake and targeted release.
Area of Science:
- Biotechnology
- Drug Delivery Systems
- Nanomedicine
Background:
- Cell-penetrating peptides (CPPs) are effective carriers for intracellular drug delivery.
- CPPs enhance drug bioavailability and reduce side effects.
- A novel polypeptide, KRP, was developed as a CPP carrier.
Purpose of the Study:
- To create a pH-responsive drug delivery system by linking KRP with doxorubicin (DOX).
- To evaluate the drug release, cell penetration, and cytotoxicity of the novel system.
- To compare the novel system with a non-pH-sensitive counterpart and free DOX.
Main Methods:
- KRP was synthesized using Fmoc solid-phase peptide synthesis.
- DOX was conjugated to KRP via stable amide (KRP-DOX) and pH-sensitive hydrazone (KRP-Hyd-DOX) bonds.
- Drug release kinetics, cell penetration, and cytotoxicity were assessed under varying pH conditions and concentrations.
Main Results:
- KRP-Hyd-DOX demonstrated significantly higher DOX release (65%) at pH 5.0 compared to pH 7.4 (30%).
- KRP-DOX showed minimal pH-dependent release.
- KRP-Hyd-DOX exhibited lower IC50 values (5.22 µM) than KRP-DOX (7.41 µM) against MG63 cells, indicating enhanced cytotoxicity.
Conclusions:
- The developed KRP-Hyd-DOX system is a pH-responsive drug delivery platform.
- This system effectively utilizes the synergistic effects of CPPs and DOX.
- KRP-Hyd-DOX enhances therapeutic efficacy while minimizing systemic side effects.
