RESUMEN
CONTEXT: Pirfenidone (PFD) has exhibited therapeutic potential in the treatment of cell proliferative disorders. The previously developed 0.5% water-based PFD eye drops by our team exhibited antiscarring effectiveness and ocular safety but with a limit of short half-life and poor bioavailability. OBJECTIVE: To increase bioavailability of the water-based PFD eye drops, we prepared a viscous solution by adding hydroxypropyl methylcellulose (HPMC, F4M), which acted as a viscosity-enhancer. Subsequently, we compared the HPMC-based PFD solution with the water-based PFD eye drops. MATERIALS AND METHODS: PFD solution with 1% HPMC (w/v) was prepared, and the viscosities at different shear rates were measured to investigate its rheology. PFD concentrations in the tear, aqueous humor, conjunctiva, cornea, and sclerae of New Zealand rabbits were detected at different time points with high-performance liquid chromatography (HPLC) following single instillation of the 0.5% PFD (w/v) water-based eye drops or HPMC-based solution. RESULTS: Compared with the 0.5% water-based PFD eye drops, the HPMC-based solution increased the PFD levels in tears and prolonged the residence time from 10 to more than 20 min (p < .01). Consequently, the concentrations of PFD in aqueous humor, conjunctiva, cornea, and sclera were elevated to varying degrees until 90 min after topical administration. CONCLUSIONS: The developed formulation possesses a same readily administration and simple preparation as the PFD eye drops; however, the HPMC-based solution exhibited the higher bioavailability.
Asunto(s)
Derivados de la Hipromelosa/síntesis química , Soluciones Oftálmicas/síntesis química , Piridonas/síntesis química , Administración Tópica , Animales , Humor Acuoso/efectos de los fármacos , Humor Acuoso/metabolismo , Evaluación Preclínica de Medicamentos/métodos , Femenino , Derivados de la Hipromelosa/administración & dosificación , Derivados de la Hipromelosa/farmacocinética , Soluciones Oftálmicas/administración & dosificación , Soluciones Oftálmicas/farmacocinética , Soluciones Farmacéuticas/administración & dosificación , Soluciones Farmacéuticas/síntesis química , Soluciones Farmacéuticas/farmacocinética , Piridonas/administración & dosificación , Piridonas/farmacocinética , Conejos , ViscosidadRESUMEN
As a green sustainable material, lignin-derived porous carbon (LPC) exhibits great application potential when used as the anode material in lithium-ion batteries (LIBs), but the applications are limited by the heterogeneity of the lignin precursor. Therefore, it is crucial to reveal the relationship among lignin properties, porous carbon structure and the kinetics of lithium-ion storage. Herein, LPCs from fractionated lignin have been prepared by an eco-friendly and recyclable activator. The structure of the LPCs was regulated by adjusting the molecular weight, linkage abundance and glass transition temperature (Tg) of lignin macromolecules. As the anode material of LIBs, the prepared 3D flower-like LPCE70 could achieve a reversible capacity of 528 mAh g-1 at a current density of 0.2 A g-1 after 200 cycles, 63 % higher than that of commercial graphite. Furthermore, kinetic calculations of lithium-ion storage behavior of LPCs were firstly used to confirm the contribution ratio of diffusion-controlled behavior and capacitive effect. Lignin with a high linkage abundance could yield LPCE70 with the largest interlayer spacing and specific surface area to maximize lithium-ion storage from both diffusion-controlled and capacitive contributions of specific capacities. This work provides a green, facile and effective pathway for value-added utilization of lignin in LIBs.