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

Autor: Adrián M. Alambiaga-Caravaca, M.A. Calatayud-Pascual, Vicent Rodilla, Alicia López-Castellano, Carmen Alvarez-Lorenzo, Angel Concheiro
Přispěvatelé: Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica, UCH. Departamento de Farmacia, Producción Científica UCH 2020
Jazyk: angličtina
Rok vydání: 2020
Předmět:
genetic structures
Interspecies ocular permeability differences
Pharmaceutical Science
lcsh:RS1-441
02 engineering and technology
Progesterona - Uso terapéutico
progesterone
030226 pharmacology & pharmacy
Micelle
ocular drug delivery
Progesterone - Therapeutic use
Article
Retinitis pigmentaria - Tratamiento
lcsh:Pharmacy and materia medica
03 medical and health sciences
interspecies ocular permeability differences
0302 clinical medicine
Cornea
retinitis pigmentosa
medicine
Permeability
Hen’s egg-chorioallantoic membrane test (HET-CAM) assay
Permeabilidad
Solubility
Progesterone
polymeric micelles
Soluplus
Ocular drug delivery
Chemistry
solubility
Penetration (firestop)
Pluronic
Poloxamer
Retinitis pigmentosa - Treatment
021001 nanoscience & nanotechnology
Eye - Diseases - Treatment
hen’s egg-chorioallantoic membrane test (HET-CAM) assay
eye diseases
Sclera
Retinitis pigmentosa
medicine.anatomical_structure
Membrane
Ojos - Enfermedades - Tratamiento
Biophysics
Polymeric micelles
sense organs
0210 nano-technology
Ex vivo
Zdroj: Pharmaceutics
Minerva. Repositorio Institucional de la Universidad de Santiago de Compostela
instname
CEU Repositorio Institucional
Fundación Universitaria San Pablo CEU (FUSPCEU)
Pharmaceutics, Vol 12, Iss 702, p 702 (2020)
Minerva: Repositorio Institucional de la Universidad de Santiago de Compostela
Universidad de Santiago de Compostela (USC)
Volume 12
Issue 8
Popis: 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&ndash
4 nm) and Soluplus (52&ndash
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&rsquo
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.
Databáze: OpenAIRE