Dr. Afsaneh Lavasanifar and collaborators have developed a PCBCL–b-PEG-b-PCBCL (PolyGelTM) hydrogel formulation of silibinin which provides enhanced skin permeabiity and delayed release of silibinin under physiological conditions. In vitro and ex vivo findings suggest this PolyGel formulation of silibinin may be useful as a topical therapy for malignant melanoma.
PolyGel incorporated a relatively high amount of silibinin, formed gel upon incubation at temperatures slightly below physiological temperature (34°C), and significantly slowed the release of incorporated drug under physiological conditions. The pattern of silibinin release from PolyGel fit first-order release kinetics. Silibinin-loaded PolyGel potently inhibited the growth of B16-F10 melanoma cells and suppressed pSTAT3 level in these cells. In comparison to a 15uM silibinin-containing Pluronic hydrogel, 15 uM silibinin-loaded PolyGel was equally effective in inhibiting growth of B16-F10 melanoma cells in vitro, but the PolyGel formulation showed 3x (significant) better skin permeation through full thickness mouse skin at 32°C. The PolyGel formulation also showed significantly better thermodynamic stability than the Pluronic formulation.
J Pharm Pharm Sci 21, 143 – 159, 2018 (www.cspsCanada.org)
- This formulation provides high thermodynamic stability and enhanced skin permeability
- May be useful for other topical STAT-3 inhibitors
- Silibinin has been shown to enhance efficacy of doxorubicin
Technology Management Group
TEC Edmonton – University of Alberta