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Cyclic Disulfide Liposomes for Membrane Functionalization and Cellular Delivery.

Megan L Qualls1, Jinchao Lou1, Dillon P McBee1

  • 1Department of Chemistry, University of Tennessee, 1420 Circle Drive, Knoxville, TN, 37996, USA.

Chemistry (Weinheim an Der Bergstrasse, Germany)
|June 14, 2022
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Summary

New cyclic disulfide lipids (CDLs) enhance liposome cell entry and allow easy surface functionalization. This liposome platform improves therapeutic delivery by enabling better cell infiltration and customizable membrane decoration for drug delivery applications.

Keywords:
cellular deliverycyclic disulfidesfluorescence microscopylipidsliposomes

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Area of Science:

  • Nanotechnology and Materials Science
  • Biochemistry and Drug Delivery

Background:

  • Liposomes are established nanocarriers for drug delivery, improving therapeutic pharmacokinetics.
  • Key limitations in liposomal drug delivery include inefficient cellular infiltration and difficult surface modification.
  • Enhanced cell entry and facile surface functionalization are critical for advancing liposome technology.

Purpose of the Study:

  • To develop a novel liposome platform using cyclic disulfide lipids (CDLs) for improved cellular delivery.
  • To enable straightforward functionalization of the liposome membrane via thiol-disulfide exchange.
  • To create multifunctional liposomes for enhanced therapeutic applications.

Main Methods:

  • Design and synthesis of two CDLs: CDL-1 (lipoic acid) and CDL-2 (asparagusic acid) appended to lipid scaffolds.
  • Implementation of a fluorescence-based microplate immobilization assay for membrane decoration assessment.
  • Utilisation of fluorescence microscopy to evaluate cellular delivery efficiency of CDL-containing liposomes.

Main Results:

  • The synthesized CDLs facilitated convenient liposome membrane decoration with thiol-functionalized molecules.
  • Incorporation of CDLs into liposomes resulted in significantly enhanced cellular uptake observed via fluorescence microscopy.
  • Demonstrated dual functionality of CDLs for both improved cell entry and surface modification capabilities.

Conclusions:

  • Multifunctional cyclic disulfide lipids (CDLs) represent a promising advancement in liposome design.
  • This CDL platform offers a versatile system for surface decoration and enhanced cellular delivery of therapeutics.
  • The developed liposomes show potential for next-generation drug delivery systems.