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)