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Updated: May 17, 2026

Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
Published on: February 8, 2017
HDL drug carriers for targeted therapy
Xing Liu1, Rong Suo, Sheng-Lin Xiong
1Institute of Cardiovascular Research, Key Laboratory for Atherosclerology of Hunan Province, University of South China, Hengyang 421001, China. liuxing0626@163.com
Insights
High-density lipoprotein cholesterol (HDL-C) offers cardiovascular protection through multiple anti-atherosclerosis activities. Exploiting four key mechanisms can enhance HDL
Area of Science:
- Biochemistry
- Cardiovascular Medicine
- Drug Delivery
Background:
- Plasma high-density lipoprotein cholesterol (HDL-C) concentrations are inversely correlated with cardiovascular risk.
- HDL possesses diverse anti-atherosclerosis functions beyond lipid transport, involving proteins, signaling lipids, and microRNAs.
- HDL's therapeutic potential is being explored for targeted drug delivery.
Purpose of the Study:
- To review four mechanisms that can enhance high-density lipoprotein (HDL) function and targeted therapy in vivo.
- To explore the potential of exploiting these mechanisms for improved clinical applications of HDL.
Main Methods:
- Review of literature focusing on four key mechanisms influencing HDL function and drug delivery.
- Discussion of HDL interactions involving caveolae, scavenger receptor class B type I (SR-BI), lecithin-cholesterol acyltransferase (LCAT), and microRNAs (miRNAs).
Main Results:
- Caveolae-mediated recruitment facilitates HDL signal receptor binding.
- SR-BI mediates HDL anchoring and fluidity for signal-lipid interactions.
- LCAT concentrates signaling lipids on the HDL surface.
- HDL particles can deliver specific microRNAs (miRNAs) to target cells.
Conclusions:
- Understanding and exploiting these four mechanisms can enhance HDL's capacity for targeted drug delivery.
- Targeted HDL therapies hold promise for increasing HDL's clinical value in cardiovascular disease management.
Abstract:
Plasma concentrations of high-density lipoprotein cholesterol (HDL-C) are strongly and inversely associated with cardiovascular risk. HDL is not a simple lipid transporter, but possesses multiple anti-atherosclerosis activities because it contains special proteins, signaling lipid, and microRNAs. Natural or recombinant HDLs have emerged as potential carriers for delivering a drug to a specified target. However, HDL function also depends on enzymes that alter its structure and composition, as well as cellular receptors and membrane micro-domains that facilitate interactions with the microenvironment. In this review, four mechanisms predicted to enhance functions or targeted therapy of HDL in vivo are discussed. The first involves caveolae-mediated recruitment of HDL signal to bind their receptors. The second involves scavenger receptor class B type I (SR-BI) mediating anchoring and fluidity for signal-lipid of HDL. The third involves lecithin-cholesterol acyltransferase (LCAT) concentrating the signaling lipid at the surface of the HDL particle. The fourth involves microRNAs (miRNAs) being delivered in the blood to special targets by HDL. Exploitation of these four mechanisms will promote HDL to carry targeted drugs and increase HDL's clinical value.
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