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Enhanced Delivery of Nonsoluble Drugs (Rapamycin) by V156K-apoA-I High-Density Lipoprotein_YEUNGNAM UNIV.
Korea Health Industry Development Institute (KHIDI) South Korea flag South Korea
Abstract ID:
Enhanced Delivery of nonsoluble drugs (Rapamycin) by V156K-apoA-I High-Density Lipoprotein
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n Technology Platform


Rapamycin formulation encapsulated in reconstituted high-density lipoprotein containing V156K-apoA-I which is a mutant of apolipoprotein A-I.



n Background and unmet needs


RAPAMYCIN is a fungicide but has recently been reported to promote longevity. It evinces immunosuppressive effects, antitumor activity, and antirestenosis activity in drug-eluting stents. Nevertheless, there have been practical limitations in its physiological study due to its very poor water solubility and bioavailability. To maximize rapamycin’s research applications, it is advantageous to dissolve the compound in a physiological and isotonic solution.


n Discovery and Achievements

- Utility of this technology


We solubilized rapamycin in isotonic solution using reconstituted HDL (rHDL) containing wild-type apoA-I or V156K-apoA-I to maximize the therapeutic application of drugs insoluble in water. After incorporation of rapamycin into rHDL, functional and structural properties were characterized using several antioxidant and antisenescence assays in vitro and in vivo. Furthermore, tissue regeneration activity was tested in a zebrafish model to probe the association between antisenescence activity and facultative regeneration.

- Capsulating ability of V156K-rHDL is superier to that of WT-rHDL






- Antioxidant activity of rapamycin in rHDL (rHDL FRAP assay)


Last Updated Jun 2016
Technology Type MECHANISM
Phase of Development EARLY STAGE

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