Low density lipoprotein bionanoparticles: From cholesterol transport to delivery of anti-cancer drugs

Abstract

In this review article, we highlight the importance of low-density lipoprotein (LDL) and its implications in the field of drug delivery to cancer cells. LDL is naturally occurring bionanoparticles (BNP) with a size of 18-25 nm. These BNPs specifically transport cholesterol to cells expressing the LDL receptors (LDLRs). Several tumors overexpress LDLRs, presumably to provide cholesterol for sustaining a high rate of membrane synthesis. LDL BNPs are biocompatible and biodegradable, favorably bind hydrophobic and amphiphilic drugs, are taken up by a receptor-mediated mechanism, have a half-life of 2-4 days, and can be rerouted. Drugs can be loaded onto LDL BNPs by surface loading, core loading, and apoprotein interaction. LDL may be used as a drug carrier for treatment of atherosclerosis, cancer, and in photodynamic therapies.

Green design “bioinspired disassembly-reassembly strategy” applied for improved tumor-targeted anticancer drug delivery

“…This might indicate that uptake mechanism of RLNs was a combination of direct transmembrane delivery (Type I or III) and endocytic pathway (Type II or III). Native apolipoprotein mixture, including apoA-I, apoB-100, and apoE, was introduced to insert into the lipid core of RLNs, which was favorable for SR-BI-mediated non-aqueous pathway [40,42] and other lipoprotein receptor-associated endocytic internalization pathways [43]. Results from this study hence supported the hypothesis that cellular internalization of RLNs involved multiple-receptor mediated mechanisms via endogenous apolipoproteins.…”

Binary-copolymer system base on low-density lipoprotein-coupled N-succinyl chitosan lipoic acid micelles for co-delivery MDR1 siRNA and paclitaxel, enhances antitumor effects via reducing drug

“…The stretching vibration peak of carboxyl-hydroxyl from NSC-LA was at 3000 cm 21 , and the bending vibration peaks were at 1400 and 962 cm 21 . The peaks weakened or disappeared after LDL coupling, which suggested that the carboxyl groups of NSC-LA were involved in the reaction.…”

“…LDL receptor (LDLr) is highly expressed in various kinds of cells and tissue, especially in the membrane of cancer cells. 21 LDLr is an essential tool for cancer cells to transport cholesterin to synthesize the cell membrane. In our study, the LDL nanoparticle could be recognized particularly by LDLr and improve the targeting effect.…”

Targeting Tumor Metabolism: A Biochemical Explanation Related to A Systems Biology Lipidomics Based Approach

“…The function of LDL and VLDL is to transport CE from and to the liver and other organs, while HDL removes cholesterol (Ch) from peripheral tissues [43].…”