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Double Sequential Encrypted Targeting Sequence: A New Concept for Bone Cancer Treatment.

Gonzalo Villaverde1, Valentina Nairi1, Alejandro Baeza1

  • 1Depto. Química Inorgánica y Bioinorgánica, Facultad de Farmacia, Universidad Complutense de Madrid. Plaza Ramon y CajaLs/n. Instituto de Investigación Sanitaria Hospital 12 de Octubre i+12 ¡ Centro de Investigación Biomédica en Red de Bioingeniería, Biomateriales y Nanomedicina (CIBER-BBN), Madrid, Spain.

Chemistry (Weinheim an Der Bergstrasse, Germany)
|February 23, 2017
PubMed
Summary

A novel double sequential encrypted targeting system enhances drug delivery selectivity to bone cancer cells. This stimuli-responsive system uses a primary targeting of diseased tissue and a secondary enzyme-activated targeting for improved therapeutic agent delivery.

Keywords:
cancerdrug deliverydual targetingencrypted peptidestimuli-responsive targeting

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Area of Science:

  • Biomedical Engineering
  • Drug Delivery Systems
  • Oncology

Background:

  • Selective drug delivery to tumor cells is crucial for effective cancer treatment.
  • Current targeting moieties often lack sufficient selectivity, leading to off-target effects.
  • The binding-site barrier effect can impede therapeutic agent penetration into tumor sites.

Purpose of the Study:

  • To develop a stimuli-responsive, double sequential encrypted targeting system for enhanced selectivity in bone cancer treatment.
  • To improve the penetration and efficacy of therapeutic agents by overcoming limitations of static targeting systems.

Main Methods:

  • Design of a dual-targeting system with an initial tissue-specific recognition.
  • Incorporation of a secondary, enzyme-activated targeting group (cathepsin K) for malignant cell recognition.
  • Conformation change strategy to mask and then reveal the targeting agent.

Main Results:

  • The proposed system demonstrates sequential targeting: initial recognition of diseased bone tissue.
  • Activation of the secondary targeting group by overexpressed cathepsin K in malignant tissue.
  • Potential to avoid non-specific binding and the binding-site barrier effect for improved drug penetration.

Conclusions:

  • The double sequential encrypted targeting system offers enhanced selectivity for bone cancer therapy.
  • This strategy can be applied to both conjugated drugs and drug-loaded nanocarriers.
  • Improved targeting efficiency holds promise for advancing bone cancer treatment outcomes.