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Micelles of Progesterone for Topical Eye Administration: Interspecies and Intertissues Differences in Ex Vivo Ocular Permeability

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Departamento de Farmacia, Facultad de Ciencias de la Salud, Instituto de Ciencias Biomédicas, Universidad Cardenal Herrera-CEU, CEU Universities, C/Santiago Ramón y Cajal, s/n., Alfara del Patriarca, 46115 Valencia, Spain
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Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+D Farma Group, Facultad de Farmacia, and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2020, 12(8), 702; https://doi.org/10.3390/pharmaceutics12080702
Received: 17 June 2020 / Revised: 14 July 2020 / Accepted: 23 July 2020 / Published: 26 July 2020
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. View Full-Text
Keywords: progesterone; retinitis pigmentosa; interspecies ocular permeability differences; polymeric micelles; Soluplus; Pluronic; ocular drug delivery; solubility; hen’s egg-chorioallantoic membrane test (HET-CAM) assay progesterone; retinitis pigmentosa; interspecies ocular permeability differences; polymeric micelles; Soluplus; Pluronic; ocular drug delivery; solubility; hen’s egg-chorioallantoic membrane test (HET-CAM) assay
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MDPI and ACS Style

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. https://doi.org/10.3390/pharmaceutics12080702

AMA Style

Alambiaga-Caravaca AM, Calatayud-Pascual MA, 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(8):702. https://doi.org/10.3390/pharmaceutics12080702

Chicago/Turabian Style

Alambiaga-Caravaca, Adrián M.; Calatayud-Pascual, María A.; Rodilla, Vicent; Concheiro, Angel; López-Castellano, Alicia; Alvarez-Lorenzo, Carmen. 2020. "Micelles of Progesterone for Topical Eye Administration: Interspecies and Intertissues Differences in Ex Vivo Ocular Permeability" Pharmaceutics 12, no. 8: 702. https://doi.org/10.3390/pharmaceutics12080702

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