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.

Quantification of the Distribution of Azelastine HCl/Fluticasone Propionate Nasal Spray in an Anatomical Model of the Human Nasal Cavity

2015 ◽  
Vol 135 (2) ◽  
pp. AB218 ◽  
Author(s):  
Alexander D'Addio ◽  
Nancy Ruiz ◽  
Michael Mayer ◽  
William E. Berger ◽  
Eli O. Meltzer
Keyword(s):  
Fluticasone Propionate ◽  
Nasal Cavity ◽  
Nasal Spray ◽  
Anatomical Model

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

Structure of spliceosomal UsnRNPs

1992 ◽  
Vol 50 (1) ◽  
pp. 460-461
Author(s):  
Reinhard Lührmann ◽  
Sven-Erik Behrens ◽  
Berthold Kastner
Keyword(s):  
Immunoaffinity Chromatography ◽  
Mrna Splicing ◽  
Splicing Factors ◽  
Nuclear Extracts ◽  
U2 Snrnp ◽  
Specific Proteins ◽  
The Common ◽  
The Individual ◽  
Stable Formation

The major snRNPs, Ul, U2, U4/U6 and U5, are essential trans-acting factors in the pre-mRNA splicing process. They assemble with a pre-mRNA and a number of other non-snRNP splicing factors prior to the splicing reaction to form an active spliceosome. We are interested in investigating the biochemical composition of UsnRNPs and their ultrastructure as well as their function in splicing. In HeLa cell nuclear extracts the spliceosomal UsnRNPs exhibit differential association behaviour depending on the salt concentration. Thus, at high salt (420 mM) the majority of the Ul, U2, U4/U6 snRNPs migrates on sucrose gradients at 10-12S, while U5 snRNP sediments at 20S. Under in vitro splicing conditions (i.e. at about 100 mM salt), U5 and U4/U6 snRNPs form a 25 S [U4/U6.U5]tri-snRNP-complex and U2 snRNPs sediment at about 17 S.We have isolated the various types of UsnRNPs under native conditions using mainly immunoaffinity chromatography procedures. Today we can distinguish more than 35 distinct snRNP proteins. They can be grouped into two classes. The first class comprises eight common snRNP proteins which are present in each of the spliceosomal UsnRNPs. In addition, the individual snRNPs contain snRNP-specific proteins. These include three (70k, A, C) for the 12 S Ul snRNP, two (A′, B″ for the 12 S U2 snRNP, an additional eight for the 17 S U2 snRNP and eight for the 20 S U5 snRNP. The 25 S [U4/U6.U5]tri-snRNP-complex contains, in addition to the common proteins and the U5-specific proteins, a third group of six proteins which are essential for the stable formation of the tri-snRNP-complex. Thus, the different S-values of a particular snRNP particle result from differences in the population of snRNP-specific proteins associated with that particle.

The Red Neuronal Pigment in the Nervous System of the Mussel, Mytilus Edulis: Localization and Its Effect on Lateral Ciliary Activity with Spectral and Analytical Changes

1981 ◽  
Vol 39 ◽  
pp. 494-495
Author(s):  
Anthony A. Paparo ◽  
Judith A. Murphy
Keyword(s):  
Nervous System ◽  
Mytilus Edulis ◽  
Neuronal Cell ◽  
Ciliary Activity ◽  
Neuronal Cell Bodies ◽  
The Central Nervous System ◽  
Intracellular Organelles ◽  
The Common ◽  
The Individual ◽  
Cryostat Sections

The purpose of this study was to localize the red neuronal pigment in Mytilus edulis and examine its role in the control of lateral ciliary activity in the gill. The visceral ganglia (Vg) in the central nervous system show an over al red pigmentation. Most red pigments examined in squash preps and cryostat sec tions were localized in the neuronal cell bodies and proximal axon regions. Unstained cryostat sections showed highly localized patches of this pigment scattered throughout the cells in the form of dense granular masses about 5-7 um in diameter, with the individual granules ranging from 0.6-1.3 um in diame ter. Tissue stained with Gomori's method for Fe showed bright blue granular masses of about the same size and structure as previously seen in unstained cryostat sections.Thick section microanalysis (Fig.l) confirmed both the localization and presence of Fe in the nerve cell. These nerve cells of the Vg share with other pigmented photosensitive cells the common cytostructural feature of localization of absorbing molecules in intracellular organelles where they are tightly ordered in fine substructures.

Formulation and Evaluation of Fish Oil-based Rizatriptan Microemulsion for Intranasal Migraine Treatment

2015 ◽  
Vol 8 (3) ◽  
pp. 2972-2978
Author(s):  
Kanchan P Upadhye ◽  
Divya Senpal ◽  
Minakshee Nimbalwar ◽  
Gouri Dixit
Keyword(s):  
Fish Oil ◽  
Nasal Cavity ◽  
Residence Time ◽  
Stability Study ◽  
Migraine Treatment ◽  
Existence Region ◽  
Microemulsion Based Gel ◽  
Micro Emulsion ◽  
Pseudoternary Phase Diagram

In the present study microemulsion based intranasal gel of rizatriptan using fish oil was prepared for treatment and management of migraine to sustain the drug release and improve the drug residence time in nasal cavity. Fish oil is reported to have antimigraine activity hence it has been used in the present formulation along with cremophore EL as surfactant and Transcutol P as co-surfactant. The pseudoternary phase diagram plotted with these components shown the microemulsion existence region in ratio of (1:9-9:1) surfactant and co-surfactant. The optimized micro-emulsion contained fish oil (45.29%), cremophore E/transcutol P (2:1) and was characterized for pH (6.3±0.02), viscosity (114 ± 3.00cp), % transmittance (99.5 ± 1.01), refractive index (1.335±0.01),). The prepared microemulsion gels were optimized and characterized for in-vitro studies, pH, drug content, rheological studies and stability study. The release of rizatriptan from micro-emulsion gel prepared from carbopol 934 (98.01%) was found to be higher and prolonged than plain gel. Thus, microemulsion based gel was able to prolong drug releaseand improve drug residence time in the nasal cavity. 

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