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1.
Int J Mol Sci ; 25(18)2024 Sep 12.
Artículo en Inglés | MEDLINE | ID: mdl-39337336

RESUMEN

Ophthalmic tacrolimus compounded formulations are usually made from the commercial intravenous presentation, which contains ethanol as a solubilizer due to the low solubility of tacrolimus. The use of cyclodextrins is presented as an alternative to ethanol, an ocular irritant excipient, to avoid its long-term irritant effects. Open-label, sequential, prospective study to compare effectiveness, safety, and adherence of a new formulation of 0.015% tacrolimus with cyclodextrins (TCD) versus 0.03% tacrolimus with ethanol (TE). The ocular evaluation was assessed by ocular signs, corneal staining, subjective questionnaires as Visual Function Questionnaire (VFQ-25) and Visual Analogue Scale (VAS) of symptoms, lacrimal stability, ocular redness, and intraocular pressure. Compliance was assessed by VAS of adherence and empirically (difference between theoretical and actual consumption). Clinical ocular signs and corneal staining score remained stable for most patients 3 months after switching formulations. The TCD formulation did not modify the tear stability and intraocular pressure of the treated patients compared to the TE formulation. TCD eye drops significantly decreased the subjective pain values on VFQ-25 scale and burning sensation on the VAS symptom scale in comparison to TE formulation after 3 months after the change to TCD formulation. The novel tacrolimus in cyclodextrins formulation is a promising alternative for treating inflammatory ocular pathologies refractory to first-line treatments.


Asunto(s)
Soluciones Oftálmicas , Tacrolimus , Tacrolimus/química , Tacrolimus/administración & dosificación , Tacrolimus/efectos adversos , Tacrolimus/uso terapéutico , Humanos , Soluciones Oftálmicas/química , Femenino , Masculino , Estudios Prospectivos , Persona de Mediana Edad , Adulto , Inmunosupresores/química , Inmunosupresores/administración & dosificación , Inmunosupresores/uso terapéutico , Anciano , Composición de Medicamentos , Ciclodextrinas/química , Resultado del Tratamiento , Presión Intraocular/efectos de los fármacos
2.
Int J Pharm ; 662: 124516, 2024 Sep 05.
Artículo en Inglés | MEDLINE | ID: mdl-39067549

RESUMEN

Uveitis is a group of inflammatory ocular pathologies. Endotoxin-Induced Uveitis (EIU) model represent a well-known model induced by administration of Lipopolysaccharide (LPS). The aim is to characterize two models of EIU through two routes of administration with novel noninvasive imaging techniques. 29 rats underwent Intraocular Pressure (IOP) measurements, Optical Coherence Tomography (OCT), proteomic analysis, and Positron Emission Tomography and Computed Tomography (PET/CT). Groups included healthy controls (C), BSS administered controls (Ci), systemically induced EIU with LPS (LPSs), and intravitreally induced EIU with LPS (LPSi) for IOP, OCT, and proteomic studies. For 18F-FDG PET/CT study, animals were divided into FDG-C, FDG-LPSs and FDG-LPSi groups and scanned using a preclinical PET/CT system. LPSi animals exhibited higher IOP post-induction compared to C and LPSs groups. LPSi showed increased cellular infiltrate, fibrotic membranes, and iris inflammation. Proinflammatory proteins were more expressed in EIU models, especially LPSi. PET/CT indicated higher eye uptake in induced models compared to FDG-C. FDG-LPSi showed higher eye uptake than FDG-LPSs but systemic uptake was higher in FDG-LPSs due to generalized inflammation. OCT is valuable for anterior segment assessment in experimental models. 18F-FDG PET/CT shows promise as a noninvasive biomarker for ocular inflammatory diseases. Intravitreal induction leads to higher ocular inflammation. These findings offer insights for future inflammatory disease research and drug studies.


Asunto(s)
Modelos Animales de Enfermedad , Presión Intraocular , Lipopolisacáridos , Tomografía Computarizada por Tomografía de Emisión de Positrones , Proteómica , Tomografía de Coherencia Óptica , Uveítis , Animales , Uveítis/inducido químicamente , Uveítis/diagnóstico por imagen , Uveítis/metabolismo , Tomografía de Coherencia Óptica/métodos , Tomografía Computarizada por Tomografía de Emisión de Positrones/métodos , Proteómica/métodos , Lipopolisacáridos/toxicidad , Presión Intraocular/efectos de los fármacos , Ratas , Masculino , Fluorodesoxiglucosa F18/administración & dosificación , Endotoxinas/toxicidad , Ratas Sprague-Dawley
3.
Pharmaceutics ; 15(11)2023 Nov 05.
Artículo en Inglés | MEDLINE | ID: mdl-38004568

RESUMEN

BACKGROUND: Cystinosis is a rare genetic disorder characterized by the accumulation of cystine crystals in several tissues and organs causing, among others, severe eye symptoms. The high instability of cysteamine eye drops makes it difficult to develop formulations with an acceptable shelf life to be prepared in hospital pharmacy departments. Previously, a new compounded formulation of cysteamine eye drops in hyaluronic acid (HA) packaged in innovative single-dose systems was developed. METHODS: Long-term stability at -20 °C of this formulation was studied considering the content of cysteamine, pH, osmolality, viscosity, and microbiological analysis. The oxygen permeability of single-dose containers was also studied and an ocular biopermanence study was conducted in healthy volunteers measuring lacrimal stability and volume parameters. RESULTS: Data confirm that cysteamine concentration remained above 90% for 120 days, all parameters remaining within the accepted range for ophthalmic formulations. The permeability of the containers was reduced over time, while ocular biopermanence was maintained despite the freezing process and storage time. CONCLUSIONS: 0.55% cysteamine hydrochloride formulation in HA and packaged in single-dose containers preserved at -20 °C is stable for 120 days protected from light, presenting high potential for its translation into clinical practice when commercial presentations are not available.

4.
Farm Hosp ; 46(6): 335-339, 2022 11 25.
Artículo en Inglés | MEDLINE | ID: mdl-36520572

RESUMEN

OBJECTIVE: To determine and compare the physicochemical and microbiological stability of two 25 IU/mL insulin eye drop formulations made with normal saline and a balanced salt solution, respectively, stored for 120 days under various conditions. METHOD: Eye drops were compounded in triplicate with 100 IU/mL Actrapid®  insulin and either normal saline or a balanced salt solution as vehicles, and  they were stored alternatively at room temperature (25 °C), in a refrigerator  (2-8 °C) or in a freezer (-20 °C) for 120 days. Insulin concentrations were  determined by ultra-high resolution liquid chromatography, and osmolality and  pH values were measured at days 0, 3, 7, 15, 30, 60, 90 and 120. Likewise,  samples were extracted for microbiological studies on days 0, 30, 60, 90 and  120. RESULTS: The formulation made with normal saline maintained insulin concentrations above 90% of the baseline level after 120 days across all  temperature conditions. In the case of the balanced salt solution- based eye drops, insulin concentration when stored at room temperature or in the freezer remained stable after 120 days, although insulin concentration when stored in the refrigerator fell below 90% on day 90 of the  study. Osmolality and pH values remained constant in both formulations and across all storage conditions. No microbiological growth was observed in any of the samples. CONCLUSIONS: 25 IU/mL insulin eye drops made with normal saline remain  stable for 120 days whether they are stored at room temperature, in a  refrigerator or in a freezer, provided that they are protected from light. When  made with a balanced salt solution, they remain stable for 120 days at room  temperature and in a freezer, their shelf life being reduced to 90 days in the  case of storage in a refrigerator.


OBJETIVO: Determinar y comparar la estabilidad físico-química y microbiológica de dos colirios de insulina 25 UI/ml elaborados con suero fisiológico o balanced salt solution bajo diferentes condiciones de  conservación durante 120 días.Método: Los colirios se elaboraron por triplicado con insulina Actrapid® 100  Ul/ml y balanced salt solution o suero fisiológico como vehículo, y fueron  conservados a temperatura ambiente (25 °C), en nevera (2-8 °C) o congelador  (­20 °C) durante 120 días. Se determinó la concentración de  insulina mediante cromatografía liquida de ultra alta resolución, la osmolalidad  y el pH a días 0, 3, 7, 15, 30, 60, 90 y 120. Asimismo, se extrajeron muestras  para estudios microbiológicos en los días 0, 15, 30, 60, 90 y 120. RESULTADOS: La formulación elaborada con suero fisiológico mantuvo la  concentración de insulina por encima del 90% con respecto a la inicial tras 120  días de estudio en todas las condiciones de temperatura. En el caso del  colirio elaborado con balanced salt solution, la concentración se mantuvo  estable en ambiente y congelador tras 120 días, aunque en nevera descendió  por debajo del 90% a día 90 de estudio. Los valores de osmolalidad y pH se  mantuvieron constantes en ambas formulaciones y condiciones de  conservación. No se observó crecimiento microbiológico en ninguna de las  muestras retiradas. CONCLUSIONES: El colirio de insulina 25 UI/ml elaborado con suero fisiológico  es estable 120 días, conservado tanto a temperatura ambiente como en nevera  o congelador, protegido de la luz. Con balanced salt solution  permanece estable 120 días a temperatura ambiente y congelador, reduciéndose el periodo de validez a 90 días en el caso de la conservación en nevera.


Asunto(s)
Úlcera de la Córnea , Humanos , Soluciones Oftálmicas/uso terapéutico , Estabilidad de Medicamentos , Insulina/uso terapéutico , Solución Salina , Temperatura , Almacenaje de Medicamentos
5.
Pharmaceutics ; 14(10)2022 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-36297629

RESUMEN

Cystinosis is a rare genetic disorder characterized by the accumulation of cystine crystals in different tissues and organs causing, among other symptoms, severe ocular manifestations. Cysteamine eye drops are prepared in hospital pharmacy departments to facilitate access to treatment, for which vehicles that provide adequate biopermanence, as well as adaptable containers that maintain its stability, are required. Difficulties related to cysteamine preparation, as well as its tendency to oxidize to cystamine, show the importance of conducting rigorous galenic characterization studies. This work aims to develop and characterize an ophthalmic compounded formulation of cysteamine prepared with hyaluronic acid and packaged in innovative single-dose systems. For this task, the effect of different storage temperatures and the presence/absence of nitrogen on the physicochemical stability of the formulation and its packaging was studied in a scaled manner, until reaching the optimal storage conditions. The results showed that 0.55% cysteamine, prepared with hyaluronic acid and packaged in single-dose containers, is stable for 30 days when stored at -20 °C. In addition, opening vials every 4 h at room temperature after 30 days of freezing maintains the stability of the cysteamine formulation for up to 16 h. Moreover, ocular biopermanence studies were conducted using molecular imaging, concluding that the biopermanence offered by the vehicle is not affected by the freezing process, where a half-life of 31.11 min for a hyaluronic acid formulation stored for 30 days at -20 °C was obtained, compared with 14.63 min for 0.9% sodium chloride eye drops.

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