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After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
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Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
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Modifying peptides to enhance permeability.

Thomas Vorherr1

  • 1Novartis Institutes for Biomedical Research, CH-4056 Basel, Switzerland.

Future Medicinal Chemistry
|June 12, 2015
PubMed
Summary
This summary is machine-generated.

Peptides can now target intracellular locations and be taken orally. This review covers peptide scaffolds, cyclization methods to improve cell permeability, and modifications enhancing oral drug delivery.

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Area of Science:

  • Medicinal Chemistry
  • Drug Delivery
  • Biotechnology

Background:

  • Peptides are increasingly recognized for their potential to target intracellular components.
  • Oral bioavailability of peptide therapeutics remains a significant challenge in drug development.
  • Advancements in peptide modification and delivery systems are crucial for therapeutic applications.

Purpose of the Study:

  • To review current peptide scaffolds for intracellular targeting and oral bioavailability.
  • To explore novel cyclization methodologies for enhanced peptide permeability.
  • To highlight modifications that improve peptide oral absorption and cellular uptake.

Main Methods:

  • Review of existing literature on peptide scaffolds and modifications.
  • Discussion of new cyclization techniques for peptide synthesis.
  • Analysis of methods for assessing peptide permeability and bioavailability.

Main Results:

  • Identification of specific peptide scaffolds suitable for intracellular delivery.
  • Presentation of cyclization strategies that enhance membrane permeability.
  • Highlighting side-chain and backbone modifications that improve cellular uptake.
  • Discussion of emerging techniques for evaluating peptide permeability.

Conclusions:

  • Peptide-based therapeutics show promise for intracellular targets and oral administration.
  • Novel cyclization and modification strategies are key to overcoming bioavailability challenges.
  • Further development of permeability assessment methods is needed for peptide drug discovery.