<p>Determination of the Permeation and Penetration of Flurbiprofen into Cadaveric Human Pharynx Tissue</p>

Abstract

Objective: Flurbiprofen 8.75 mg spray and lozenge have a rapid onset of action for sore throat relief, suggesting local action, although tissue penetration and the mechanism of local relief have not been determined. This investigation aimed to quantify the permeation and penetration of flurbiprofen, applied as local pharmaceutical forms, into full-thickness cadaveric human mucosal pharynx tissue, representing the clinical scenario as far as possible. Methods: A validated high-performance liquid chromatography method quantified the permeation and penetration of flurbiprofen (spray and lozenge formulations) into human cadaveric pharynx tissue using a micro Franz cell model mimicking physiological and anatomical conditions. Full-thickness mucosal pharynx tissue, consisting of oral epithelium, basement membrane, and lamina propria, was utilized to imitate the in vivo setting. Flurbiprofen was analyzed on the surface of the pharynx tissue, within the pharynx tissue and in receiver fluid, over 60 mins. Results: Flurbiprofen was detected in receiver fluid from 10 mins following spray application and was quantifiable from 20 mins. Flurbiprofen from lozenge was detected from 10 mins and was above the limit of quantitation in receiver fluid from 40 mins. Flurbiprofen recovered from the surface of the pharynx tissue was 24.45% and 8.48% of applied dose for spray and lozenge, respectively. Flurbiprofen recovered within pharynx tissue was 46.50% and 54.65% of applied dose for spray and lozenge, respectively. For flurbiprofen lozenge, recovery within pharynx tissue was 6-fold higher relative to recovery from the pharynx tissue surface. Conclusion: Flurbiprofen from spray and lozenge formulations penetrated human cadaveric pharynx tissue, indicating that flurbiprofen can reach all layers of the pharynx mucosal tissue, including the underlying lamina propria, which contains blood vessels and nerve fibers that contribute to pain during sore throat. This suggests that flurbiprofen may have a local mechanism of action for sore throat, although this has yet to be determined.

Penetration of Flurbiprofen from a Locally Applied Sore Throat Lozenge and Spray into Cadaveric Human Pharynx Tissue: A Novel ex vivo Model and Microautoradiography Method

“…This study reaffirmed the findings of our previous study, which demonstrated that flurbiprofen from a throat spray solution and a dosing solution prepared from a lozenge formulation is capable of penetrating the pharynx tissue, 24 while allowing visualization of radiolabeled flurbiprofen penetration across all layers of the pharynx tissue. Radiolabeled flurbiprofen was detected in the deepest sections of the human cadaveric pharynx tissue.…”

“…15 This effect is considered to be due to the local absorption which has been previously demonstrated through the buccal mucosa and ex vivo cadaveric human pharynx tissue. [21][22][23][24] This research builds on a previous study, which involved the development of a method to quantify permeation and penetration of flurbiprofen through the human pharynx tissue in an ex vivo model using a Franz diffusion cell method, 25 followed by quantification of the permeation and penetration of flurbiprofen in the human pharynx tissue, 23,24 and development of a model to replicate absorption from lozenge and throat spray using a Franz diffusion cell.…”

Pain Symptoms in Patients with Coronavirus Disease (COVID-19): A Literature Review

“…Sore throat refers to the pain caused by inflammation of tissues located behind the throat, 44 and up to 80% of the cases is caused by viruses (eg, coronavirus, influenza, and rhinovirus). 45 , 46 Internationally, sore throat complaints account for 1–4% of all primary care reports.…”

Rationale for the use of NSAIDs with antiseptic action for sore throat in the complex therapy of infectious and inflammatory diseases

“…в 2020 г. с помощью метода высокоэффективной жидкостной хроматографии и модели микроклеток Франца смогли количественно оценить проникновение флурбипрофена в ткани глотки человеческого трупа. Была доказана способность флур бипрофена проникать во все слои слизистой оболочки глотки, включая подлежащую пластинку собственной оболочки с кровеносными сосудами и нервными волокнами [34].…”