A Novel Microparticle Based Formulation for Topical Delivery of FOL-005, a Small Peptide

Abstract

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Identification of an osteopontin-derived peptide that binds neuropilin-1 and activates vascular cells

“…These observations provide evidence for a pro-angiogenic effect of FOL-026. Earlier experimental and clinical studies have shown that treatment with the FOL-026 analogue FOL-005 as well as osteopontin 4,18 stimulates hair growth but the mechanisms responsible for this effect have been unclear. Yano and coworkers 9 were first to demonstrate that the transition of resting hair follicles into the anagen growth phase is preceded by an increased perifollicular vascularization and that this is activated by an increased expression of VEGF in follicular keratinocytes in the outer root sheath of the hair follicle and FOL-005 has been shown to also accumulate around and affect these cells.…”

“…HUVECs on 6-well plates were starved for 24 hours or for siRNA transfection for 48 hours and dissociated by TrypLE Express (Gibco, Grand Island, NY) to obtain cell suspensions. Cells were seeded at a density of 1.5 x 10 4 / well in 96-well plate pre-coated with Geltrex reduced growth factor basement membrane matrix (Gibco, Grand Island, NY) in Medium 200 complete culture medium containing different concentration of FOL-026 peptide. After 12-18 hours of incubation, random images were recorded by an inverted microscope (Nikon, Eclipse TE2000-U, Kawasaki, Japan).…”

“…Cells with exposure of starvation for 24 hours or siRNA transfection for 48 hours were seeded at a density of 3.5 x 10 4 / inlet into Culture-Insert 2 well (Ibidi, Fitchburg, WI) in 24-well plate and cultured overnight. In the second day, the cell-free gap between two inlets was created by removing the insert and cells were washed by DPBS gently to remove the debris.…”

“…2 We have previously found that a peptide derived from the latter binding site, but with point mutations in the RGD sequence, stimulates hair growth in an animal model by promoting the transition of hair follicles from the telogen to the anagen phase. 4 The effect of this peptide (FOL-005) on hair growth has been investigated in three clinical trials (NCT02793557, NCT03467412, and NCT04774874) providing support for the presence of stimulatory hair growth activity also in humans, and with a good safety profile.…”