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Engineering selective molecular tethers to enhance suboptimal drug properties.

Alan Dogan1, Horst von Recum1

  • 1Case Western Reserve University, 10900 Euclid Ave., Cleveland Ohio 44106, United States of America.

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|August 27, 2020
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Summary

Tethering small-molecule drugs to specific groups enhances their properties, like solubility and delivery. This method triples drug affinity and delivery window from cyclodextrin-based polymers without losing efficacy.

Keywords:
AffinityCyclodextrinExtended drug deliveryMicroparticlesRapamycinSelective PEGylation

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Area of Science:

  • Bioconjugation Chemistry
  • Drug Delivery Systems
  • Polymer Science

Background:

  • Small-molecule drugs often have suboptimal properties limiting their in vivo delivery and efficacy.
  • Current methods like high-throughput screening discover drugs with altered properties but lack targeted modulation.
  • Engineering small-molecule bioconjugates offers precise control over drug properties.

Purpose of the Study:

  • To improve drug properties by tethering small-molecule drugs to affinity groups.
  • To enhance the affinity of rapamycin (RAP) for cyclodextrin-based polymers (pCD).
  • To increase the drug delivery window from pCD microparticles.

Main Methods:

  • Site-specific chemical conjugation of rapamycin (RAP) to a high-affinity group.
  • Utilizing cyclodextrin-based polymers (pCD) for drug conjugation and delivery.
  • Evaluating the affinity and delivery window of the modified drug conjugate.

Main Results:

  • The tethered rapamycin (RAP) showed tripled affinity for cyclodextrin-based polymers (pCD).
  • The delivery window of RAP from pCD microparticles was also tripled.
  • The cellular action of rapamycin was not sacrificed by the conjugation process.

Conclusions:

  • Selective tethering of drugs to affinity groups can significantly improve drug conjugate properties.
  • This approach enhances drug affinity and delivery windows in polymer-based systems.
  • The method holds potential for optimizing small-molecule drug delivery in chronic therapies.