Using rifapentine – hen egg lipoprotein conjugate as macrophage-targeted drug delivery carrier against intracellular Staphylococcus aureus. (January 2015)

• Record Type: Journal Article
• Authors: Yang, Jinli; Li, Yuxin; Liu, En; Xininigen, Tang W.; Bai, Wencheng; Han, Runlin
• Is Part Of: Drug delivery. Volume 22:Number 1(2015:Jan.)
• Page Start: 111
• Page End: 116
• Publication Date: 2015-01
• Subjects: Drug delivery systems -- Periodicals; Drug targeting -- Periodicals; 615.05
• DOI: 10.3109/10717544.2014.902145
• Languages: English
• ISSNs: 1071-7544

Abstract

<abstract> <title>Abstract</title> <p> <italic>Context</italic>: Hen egg low-density lipoprotein (heLDL), which is present in large quantities in egg yolk, share a high identity with human apolipoprotein B-100 precursor.</p> <p> <italic>Objective</italic>: This study investigated the use of heLDL as a macrophage-targeted drug delivery carrier against intracellular <italic>Staphylococcus aureus</italic>.</p> <p> <italic>Methods</italic>: Rifapentine (RPT) was incorporated into heLDL (RPT–heLDL). <italic>Staphylococcus aureus</italic> ATCC 29740 and human U937 macrophage were used as intracellular infection models.</p> <p> <italic>Results and conclusion</italic>: The loading efficiency of RPT into the heLDL was 66.10 ± 2.28 μg RPT/mg heLDL. Fluorescence microscopy and oil red O staining results indicated RPT–heLDL can be taken up by U937 macrophages. The cell viability (MTT assay) was increased when the concentration of heLDL was &lt;150 μg/mL. Unloaded heLDL (100 μg/mL) can inhibit the growth of intracellular <italic>S. aureus</italic> compared with the untreated control group after 18 h incubation. RPT–heLDL (6.6 μg/mL RPT, 100 μg/mL heLDL) eliminated 94% of intracellular <italic>S. aureus</italic>, whereas the corresponding dose of free RPT (6.6 μg/mL) induced an 87% reduction. The <italic>in vitro</italic> results of the current study indicated that heLDL might be used as a suitable drug carrier for targeting human macrophages.</p> </abstract>