scholarly journals Evaluation of in vitro Penetration of Fluticasone Propionate from MP-AzeFlu and Fluticasone Propionate Nasal Spray Through EpiAirway™606 Tissues Using Vertical Diffusion Cells

2020 ◽  
Vol Volume 13 ◽  
pp. 187-192
Author(s):  
William E Berger ◽  
Claus Bachert ◽  
Robert Allara ◽  
Arkady Koltun ◽  
Ferdinand Kopietz ◽  
...  
Keyword(s):  
Fluticasone Propionate ◽  
Nasal Spray ◽  
Vertical Diffusion ◽  
Diffusion Cells

scholarly journals A stepwise protocol for drug permeation assessment that combines heat-separated porcine ear epidermis and vertical diffusion cells

2018 ◽  
Vol 72 (1) ◽  
pp. 47-53 ◽  
Author(s):  
Ivana Pantelic ◽  
Tanja Ilic ◽  
Bojan Markovic ◽  
Sanela Savic ◽  
Milica Lukic ◽  
...  
Keyword(s):  
Evaluation Method ◽  
In Vitro Test ◽  
Formulation Development ◽  
Vertical Diffusion ◽  
Synthetic Membranes ◽  
Drug Permeation ◽  
Diffusion Cells ◽  
Drug Sample ◽  
Model Drug

After decades long absence of an official consensus on the most appropriate evaluation method for in vitro skin performance of topical semisolid drugs, United States Pharmacopoeia (USP 39) finally suggested three types of testing equipment; however, all these provide data on drug release using inert synthetic membranes. Considering the need for a readily available membrane that would be more structurally similar to human skin, this paper provides a detailed protocol of a method for drug permeation assessment that uses heat-separated porcine ear epidermis and modified Franz diffusion cells. Phases that were shown to be critical for variability of the results are identified (e.g., membrane preparation), and process parameters optimized. Applicability of the method was tested on four cream samples loaded with aceclofenac as a model drug. Sample compositions were designed in such a way to provide ?large? variations (variation of the main stabilizer: natural-origin versus synthetic emulsifier) and relatively ?minor? variations (co-solvent variation: none/isopropanol/glycerol). The developed protocol is a straightforward and reliable in vitro test for the evaluation of rate and extent of drug delivery into/through the skin. Moreover, this protocol may be routinely applied even in averagely equipped laboratories during formulation development or preliminary bioequivalence assessment of generic topical semisolids.

Deposition characteristics of a novel intranasal formulation of azelastine hydrochloride plus fluticasone propionate in an anatomic model of the human nasal cavity

2020 ◽  
Vol 41 (4) ◽  
pp. 265-270
Author(s):  
Eli O. Meltzer ◽  
Claus Bachert ◽  
Michael J. Mayer ◽  
Ferdinand Kopietz ◽  
Arkady Koltun ◽  
...  
Keyword(s):  
Fluticasone Propionate ◽  
Nasal Cavity ◽  
Nasal Spray ◽  
Cavity Model ◽  
Brand Name ◽  
Dosing Regimen ◽  
Optimal Drug ◽  
The Common ◽  
The Individual

Background: Intranasal antihistamines and steroids should be delivered in a volume and with a technique that allow for optimal drug retention within the entire nasal cavity, maximize local absorption by the nasal mucosa, and, subsequently, increase the potential for the most desirable local availability and therapeutic effect. Objective: This in vitro evaluation simulated nasal medication deposition and evaluated the extent of runoff. MP-AzeFlu, a novel intranasal formulation of azelastine hydrochloride (AZE) plus fluticasone propionate (FP), was compared with sequential sprays of available commercial products with the individual medication components. Methods: A model of a normal adult human nasal cavity was used to visualize deposition of nasal spray products. A single spray of MP-AzeFlu (0.137 mL [137 μg of AZE/50 μg of FP]) or single sequential sprays of AZE nasal spray (0.137 mL [137 μg]) followed by brand name or generic FP nasal spray (0.100 mL [50 μg]) were manually actuated into the model. The interior was coated with a water-sensitive dye that changes to magenta when exposed to aqueous-based formulations. A slight vacuum was applied during spray delivery to simulate sniffing. The results were photographed by using anterior and lateral views. Results: Three replicates of MP-AzeFlu showed no dripping from the front of the nostril or backflow from the nasal cavity. However, three replicates of AZE nasal spray, followed by a brand name or generic FP nasal spray, showed significant dripping from the front of the nostril and backflow from the nasal cavity. Conclusion: A single spray of MP-AzeFlu resulted in no runoff compared with sequential dosing of the two other therapeutic products. Product runoff is likely due to the volume exceeding the capacity of the nasal cavity model. Furthermore, the common clinical dosing regimen of two sprays per nostril of each of the individual components would promote even greater increased undesirable flooding and leakage.

scholarly journals Comparison of In Vitro Release Rates of Acyclovir from Cream Formulations Using Vertical Diffusion Cells

2014 ◽  
Vol 15 (4) ◽  
pp. 994-999 ◽  
Author(s):  
Sumalatha Nallagundla ◽  
Srinivas Patnala ◽  
Isadore Kanfer
Keyword(s):  
In Vitro Release ◽  
Release Rates ◽  
Vertical Diffusion ◽  
Diffusion Cells ◽  
Vitro Release

scholarly journals Dexamethasone-Loaded Lipomers: Development, Characterization, and Skin Biodistribution Studies

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 533
Author(s):  
Eloy Pena-Rodríguez ◽  
Maria Lajarin-Reinares ◽  
Aida Mata-Ventosa ◽  
Sandra Pérez-Torras ◽  
Francisco Fernández-Campos
Keyword(s):  
In Vitro Release ◽  
Human Keratinocytes ◽  
Topical Administration ◽  
In Vitro Cytotoxicity ◽  
Hair Follicles ◽  
Vertical Diffusion ◽  
Biodistribution Studies ◽  
Follicular Targeting ◽  
Depot Effect

Follicular targeting has gained more attention in recent decades, due to the possibility of obtaining a depot effect in topical administration and its potential as a tool to treat hair follicle-related diseases. Lipid core ethyl cellulose lipomers were developed and optimized, following which characterization of their physicochemical properties was carried out. Dexamethasone was encapsulated in the lipomers (size, 115 nm; polydispersity, 0.24; zeta-potential (Z-potential), +30 mV) and their in vitro release profiles against dexamethasone in solution were investigated by vertical diffusion Franz cells. The skin biodistribution of the fluorescent-loaded lipomers was observed using confocal microscopy, demonstrating the accumulation of both lipomers and fluorochromes in the hair follicles of pig skin. To confirm this fact, immunofluorescence of the dexamethasone-loaded lipomers was carried out in pig hair follicles. The anti-inflammatory (via TNFα) efficacy of the dexamethasone-loaded lipomers was demonstrated in vitro in an HEK001 human keratinocytes cell culture and the in vitro cytotoxicity of the nanoformulation was investigated.

scholarly journals Antioxidant-Loaded Mucoadhesive Nanoparticles for Eye Drug Delivery: A New Strategy to Reduce Oxidative Stress

Processes ◽  
2021 ◽  
Vol 9 (2) ◽  
pp. 379
Author(s):  
Sandra Cordeiro ◽  
Beatriz Silva ◽  
Ana Margarida Martins ◽  
Helena Margarida Ribeiro ◽  
Lídia Gonçalves ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Hyaluronic Acid ◽  
Zeta Potential ◽  
Retinal Pigment ◽  
Release Kinetic ◽  
Efficient Treatment ◽  
Non Invasive ◽  
Diffusion Cells ◽  
Franz Diffusion Cells

There are several approaches to treat ocular diseases, which can be invasive or non-invasive. Within the non-invasive, new pharmaceutical strategies based on nanotechnology and mucoadhesive polymers are emerging methodologies, which aim to reach an efficient treatment of eye diseases. The aim of this work was the development of novel chitosan/hyaluronic acid nanoparticle systems with mucoadhesive properties, intended to encapsulate antioxidant molecules (e.g., crocin) aiming to reduce eye oxidative stress and, consequently, ocular disease. An ultraviolet (UV) absorber molecule, actinoquinol, was also added to the nanoparticles, to further decrease oxidative stress. The developed nanoparticles were characterized and the results showed a mean particle size lower than 400 nm, polydispersity index of 0.220 ± 0.034, positive zeta potential, and high yield. The nanoparticles were also characterized in terms of pH, osmolality, and viscosity. Mucoadhesion studies involving the determination of zeta potential, viscosity, and tackiness, showed a strong interaction between the nanoparticles and mucin. In vitro release studies using synthetic membranes in Franz diffusion cells were conducted to unravel the drug release kinetic profile. Ex vitro studies using pig eye scleras in Franz diffusion cells were performed to evaluate the permeation of the nanoparticles. Furthermore, in vitro assays using the ARPE-19 (adult retinal pigment epithelium) cell line showed that the nanoparticles can efficiently decrease oxidative stress and showed low cytotoxicity. Thus, the developed chitosan/hyaluronic acid nanoparticles are a promising system for the delivery of antioxidants to the eye, by increasing their residence time and controlling their delivery.

Effect of fluticasone propionate aqueous nasal spray versus oral prednisone on the hypothalamic-pituitary-adrenal axis

1998 ◽  
Vol 102 (2) ◽  
pp. 191-197 ◽  
Author(s):  
Ramón Vargas ◽  
Robert J. Dockhorn ◽  
Steven R. Findlay ◽  
Phillip E. Korenblat ◽  
Elizabeth A. Field ◽  
...  
Keyword(s):  
Fluticasone Propionate ◽  
Nasal Spray ◽  
Oral Prednisone ◽  
Hypothalamic Pituitary Adrenal Axis ◽  
Hypothalamic Pituitary Adrenal ◽  
Adrenal Axis ◽  
Pituitary Adrenal Axis
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