RT Journal Article
T1 Micelles of Progesterone for Topical Eye Administration: Interspecies and Intertissues Differences in Ex Vivo Ocular Permeability
A1 Alambiaga Caravaca, Adrián M.
A1 Calatayud Pascual, María Aracely
A1 Rodilla, Vicent
A1 Concheiro Nine, Ángel Joaquín
A1 López Castellano, Alicia
A1 Álvarez Lorenzo, Carmen
K1 Progesterone
K1 Retinitis pigmentosa
K1 Interspecies ocular permeability differences
K1 Polymeric micelles
K1 Soluplus
K1 Pluronic
K1 Ocular drug delivery
K1 Solubility
K1 Hen’s egg-chorioallantoic membrane test (HET-CAM) assay
AB Progesterone (PG) may provide protection to the retina during retinitis pigmentosa, but its topical ocular supply is hampered by PG poor aqueous solubility and low ocular bioavailability. The development of efficient topical ocular forms must face up to two relevant challenges: Protective barriers of the eyes and lack of validated ex vivo tests to predict drug permeability. The aims of this study were: (i) To design micelles using Pluronic F68 and Soluplus copolymers to overcome PG solubility and permeability; and (ii) to compare drug diffusion through the cornea and sclera of three animal species (rabbit, porcine, and bovine) to investigate interspecies differences. Micelles of Pluronic F68 (3–4 nm) and Soluplus (52–59 nm) increased PG solubility by one and two orders of magnitude, respectively and exhibited nearly a 100% encapsulation efficiency. Soluplus systems showed in situ gelling capability in contrast to the low viscosity Pluronic F68 micelles. The formulations successfully passed the hen’s egg-chorioallantoic membrane test (HET-CAM) test. PG penetration through rabbit cornea and sclera was faster than through porcine or bovine cornea, although the differences were also formulation-dependent. Porcine tissues showed intermediate permeability between rabbit and bovine. Soluplus micelles allowed greater PG accumulation in cornea and sclera whereas Pluronic F68 promoted a faster penetration of lower PG doses
PB MDPI
YR 2020
FD 2020
LK http://hdl.handle.net/10347/23815
UL http://hdl.handle.net/10347/23815
LA eng
NO Alambiaga-Caravaca, A.M.; Calatayud-Pascual, M.A.; Rodilla, V.; Concheiro, A.; López-Castellano, A.; Alvarez-Lorenzo, C. Micelles of Progesterone for Topical Eye Administration: Interspecies and Intertissues Differences in Ex Vivo Ocular Permeability. Pharmaceutics 2020, 12, 702
NO This research was funded by MINECO [SAF2017-83118-R] (Spain), Agencia Estatal de Investigación (AEI, Spain), Xunta de Galicia [AEMAT ED431E 2018/08], and European Regional Development Fund (FEDER). Predoctoral grants CEU Cardenal Herrera University FPI CEU-UCH, mobility grant CEINDO international doctoral school, CEU-Cardenal Herrera University [INDI 19/28]
DS Minerva
RD 24 abr 2026