Enhanced oral bioavailability of self-Assembling curcumin-vitamin E prodrug-nanoparticles by co-nanoprecipitation with Vitamin E TPGS

Curcumin (CUR), a non-toxic natural compound with potent antitumor activity, was limited in clinical application due to its insolubility and exceedingly low bioavailability. In this study, a novel prodrug-nanoparticles (CSSV/TPGS-NPs) self-assembled by co-nanoprecipitation of curcumin-s-s-vitamin E conjugate and D-alpha-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) was prepared in attempt to solve aforementioned obstacles.

CSSV/TPGS-NPs showed smaller sizes and better stability compared with that of curcumin-s-s-vitamin E conjugate prodrug-nanoparticles (CSSV-NPs). Significantly, the absorption constant and effective permeability of CSSV/TPGS-NPs in different intestinal tracts increased 1.31–2.78 times and 1.81–6.95 times than that of CUR suspension, respectively. Pharmacokinetic study in Sprague Dawley (SD) rats demonstrated that orally administered CSSV/TPGS-NPs displayed a prolonged plasma circulation with 8.06-fold increase in relative bioavailability compared to that of the CUR suspension.

Altogether, conjugation of hydrophobic native curcumin with vitamin E to form CSSV/TPGS-NPs is a promising technology for sustained and controlled drug delivery of curcumin with improved oral bioavailability in vivo.

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Article Information: Huiyun Zhang, Baoding Chen, Yuan Zhu, Congyong Sun, Michael Adu-Frimpong, Jiangnan Yu & Ximing Xu; Drug Development and Industrial Pharmacy, 2020.


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