4.6 Review

Reconstituted HDL as a therapeutic delivery device

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ELSEVIER
DOI: 10.1016/j.bbalip.2021.159025

Keywords

Reconstituted HDL; Nanodisk; Apolipoprotein; Phospholipid; Bioactive agent; Delivery

Funding

  1. US National Institutes of Health [R37 HL64159]
  2. American Heart Association Predoctoral Fellowship

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Research on pre beta HDL and rHDL has advanced our understanding of Reverse Cholesterol Transport pathway. rHDL can be easily generated in vitro, leading to novel applications such as promoting regression of atherosclerosis and delivering hydrophobic bioactive molecules. This technology is still in its early stages, with the full potential of these nanoparticles yet to be discovered.
Studies of pre beta high density lipoprotein (HDL) and reconstituted HDL (rHDL) have contributed to our understanding of the Reverse Cholesterol Transport pathway. The relative ease with which discoidal rHDL can be generated in vitro has led to novel applications including a) infusion of rHDL into patients to promote regression of atherosclerosis; b) use of rHDL as a miniature membrane for integration of transmembrane proteins in a native-like conformation and c) incorporation of hydrophobic bioactive molecules into rHDL, creating a delivery device. The present review is focused on bioactive agent containing rHDL. The broad array of hydrophobic bioactive molecules successfully incorporated into these particles is discussed, as well as the use of natural lipids and synthetic lipid analogs to confer distinctive binding activity. This technology remains in its infancy with the full potential of these simple, yet elegant, nanoparticles still to be discovered.

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