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. 2023 Jan 29;16(3):1156.
doi: 10.3390/ma16031156.

Lipoproteins as Drug Carriers for Cyclosporine A: Optimization of the Entrapment

Mona M A Abdel-Mottaleb  1 , Lorenza Boi  2   3 , Marina Barra  2   3 , Julie Colin  3 , Luisa Berni  2   3 , Arnaud Béduneau  3 , Brice Moulari  3 , Yann Pellequer  3
Affiliations

Lipoproteins as Drug Carriers for Cyclosporine A: Optimization of the Entrapment

Mona M A Abdel-Mottaleb et al. Materials (Basel). .

Abstract

Lipoproteins are natural nanostructures responsible for the transport of cholesterol and other lipids in the blood. They are characterized by having a lipophilic core surrounded by an amphiphilic shell composed of phospholipids, cholesterol and one or more apolipoproteins. Being endogenous carriers makes them suitable for drug delivery purposes. Here, we investigate the effect of lipoproteins' intricate composition on the entrapment efficiency of a model drug "Cyclosporine A" into the different types of lipoproteins, namely, HDL, LDL and VLDL. It was observed that the protein content of the lipoproteins had the highest effect on the entrapment of the drug with a correlation coefficient of 0.80, 0.81 and 0.96 for HDL, LDL and VLDL respectively. This was even confirmed by the effect of plasma on the association rate of lipoproteins and the drug. The second effective factor is the cholesterol concentration, while triglycerides and phospholipids had a negligible effect.

Keywords: apolipoproteins; cholesterol; cyclosporine A; entrapment; lipoproteins.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
A correlation between the concentration of lipoprotein components and the cyclosporine association rate; (A): triglyceride concentration, (B): phospholipids concentration, (C): total cholesterol concentration, (D): free cholesterol concentration, (E): proteins concentration, (F): esterified cholesterol concentration.
Figure 1
Figure 1
A correlation between the concentration of lipoprotein components and the cyclosporine association rate; (A): triglyceride concentration, (B): phospholipids concentration, (C): total cholesterol concentration, (D): free cholesterol concentration, (E): proteins concentration, (F): esterified cholesterol concentration.
Figure 1
Figure 1
A correlation between the concentration of lipoprotein components and the cyclosporine association rate; (A): triglyceride concentration, (B): phospholipids concentration, (C): total cholesterol concentration, (D): free cholesterol concentration, (E): proteins concentration, (F): esterified cholesterol concentration.
Figure 2
Figure 2
Difference in the association rate of cyclosporine with the different types of lipoproteins before and after separation from the plasma.
See this image and copyright information in PMC

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