Abstract：
:Native low-density lipoproteins (LDL) naturally accumulate at atherosclerotic lesions and are thought to be among the main drivers of atherosclerosis progression. Numerous nanoparticular systems making use of recombinant lipoproteins have been developed for targeting atherosclerotic plaque. These innovative formulations often require complicated purification and synthesis procedures which limit their eventual translation to the clinics. Recently, squalenoylation has appeared as a simple and efficient technique for targeting agents to endogenous lipoproteins through a bioconjugation approach. In this study, we have developed a fluorescent squalene bioconjugate to evaluate the biodistribution of squalene-based nanoparticles in an ApoE-/- model of atherosclerosis. By accumulating in LDL endogenous nanoparticles, the squalene bioconjugation could serve as an efficient targeting platform for atherosclerosis. Indeed, in this proof of concept, we show that our squalene-rhodamine (SQRho) nanoparticles, could accumulate in the aortas of atherosclerotic animals. Histological evaluation confirmed the presence of atherosclerotic lesions and the co-localization of SQRho bioconjugates at the lesion sites.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Brusini R,Dormont F,Cailleau C,Nicolas V,Peramo A,Varna M,Couvreur Pdoi
10.1016/j.ijpharm.2020.119282subject
Has Abstractpub_date
2020-05-15 00:00:00pages
119282eissn
0378-5173issn
1873-3476pii
S0378-5173(20)30266-0journal_volume
581pub_type
杂志文章abstract：:The purpose of the present study was to examine the human oral absorption (HOA) predictability of the experimentally determined immobilized artificial membrane (IAM) chromatography capacity factor (log k'IAM) in conjunction with physicochemical descriptors. Transcellular permeation was modeled based on determination o...
journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
pub_type： 临床试验,杂志文章,随机对照试验
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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