Formulation and Permeation Kinetic Studies of Flurbiprofen Gel

Ayoub, RK; Murtaza, Ghulam; Imran, Muhammad; Khan, SA; Mir, Showkat R.; Khan, AK; Azhar, S; Mehmood, Zafar; Sajjad, Ansari; Shah, Snh

doi:10.4314/tjpr.v14i2.2

Cited by 9 publications

(9 citation statements)

References 3 publications

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“…44 In addition, previous studies have used synthetic membranes to determine the permeation of flurbiprofen or ibuprofen gel; however, although easily resourced, inexpensive, and structurally simpler, they do not reflect what may happen in vivo. 32,45,46 An important limitation of our study was the use of cadaver tissue, which may result in drug penetration speed that does not truly reflect live tissue, where a blood supply is present. In addition, the absence of inflammation and the lack of a mucosal barrier may modify drug penetration.…”

Section: Discussionmentioning

confidence: 99%

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

Turner¹,

Wevrett²,

Edmunds³

et al. 2020

CPAA

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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.

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Section: Discussionmentioning

confidence: 99%

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

Turner¹,

Wevrett²,

Edmunds³

et al. 2020

CPAA

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“…Many studies have demonstrated poor dermal and transdermal delivery of chrysin and quercetin [5,[8][9][10][11]17]. The literature reports that solvents commonly used in cosmetics and dermatological products can influence release and skin penetration processes [17][18][19][20][21][22][23][24]. In the present study, the influence of two solvents -PG and PEG 400on the release and the skin retention of two flavonoidschrysin and quercetinwas investigated.…”

Section: Discussionmentioning

confidence: 97%

“…While the dissolution of the flavonoids in the solvents may be assumed to be the main determinant of the release rate, the skin retention appears to be additionally impacted by interactions of the used solvents with the skin barrier . The ability of the used solvent to penetrate into the skin and to interact with that barrier seemed to be necessary for providing an enhancement of the skin retention.…”

Section: Discussionmentioning

confidence: 99%

“…The interaction of PG with the skin is quite different from that of PEG 400. PG easily penetrates into the lipid materials of the stratum corneum and is recognized as an excellent permeation enhancer increasing both the stratum corneum permeability and skin/base partition coefficients . On the contrary, PEG tends to remain on the skin surface as its penetration into the skin is very poor due to its highly hydrophilic nature .…”

Section: Discussionmentioning

confidence: 99%

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The effect of additives on release and in vitro skin retention of flavonoids from emulsion and gel semisolid formulations

Dyja

Jankowski²

2017

Intern J of Cosmetic Sci

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“…It is not currently plausible to investigate the penetration of flurbiprofen into human pharynx tissue in vivo and, as such, alternative methods of investigation must be used. The Franz diffusion cell method has been used previously to mimic physiological and anatomical conditions to allow the study of diffusion through various tissues, 31 , 32 including human pharynx tissue. 23 , 25 This ex vivo model was developed to mimic the clinical scenario as closely as possible, 25 using full-thickness cadaveric pharynx tissue, which provides a close match to the physiological and anatomical conditions of the human pharynx.…”

Section: Discussionmentioning

confidence: 99%

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

Turner¹,

Wevrett²,

Edmunds³

et al. 2021

CPAA

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Objective: Flurbiprofen 8.75 mg lozenge and spray are used for symptomatic relief of sore throat, with a rapid onset of analgesia suggesting a localized mechanism of action. Building on previous studies, this investigation aimed to use microautoradiography to visualize the depth penetration of radiolabeled flurbiprofen into human pharynx tissue using an ex vivo model. Quantification of flurbiprofen in the tissue was performed to provide a quantitative representation of flurbiprofen distribution through the tissue. Methods: Cadaveric human pharynx tissue was mounted between the donor and receiver compartments of a Franz diffusion cell. After that 8.75 mg spray and dissolved lozenge formulations, containing radiolabeled flurbiprofen, were added to the donor compartment of a Franz diffusion cell. After incubation for one hour, the pharynx tissue was removed, processed, and sectioned both horizontally and vertically. The sections were placed within an imaging cassette to determine the penetration of radiolabeled flurbiprofen visually, before being solubilized to quantify the amount of flurbiprofen present in each section. Results: In the horizontally sectioned samples, flurbiprofen was present in the top layers of all replicates and decreased in intensity throughout the tissue. Of the applied dose, 48.0--99.9% of flurbiprofen was detected in the top one-third of the pharynx tissue, closest to the dosing site, and 0-14.8% of flurbiprofen was detected within the deepest third of pharynx tissue, furthest from the dosing site. In the vertically sectioned tissue samples, radiolabeled flurbiprofen was found at a high intensity at the dosing site and reduced in intensity throughout the thickness of the tissue. Lateral penetration of flurbiprofen was also seen in tissue dosed with the spray. Conclusion:Our findings demonstrate that lozenge and spray formulations of flurbiprofen can penetrate throughout the layers of cadaveric human pharynx tissue in an ex vivo model, as visualized by microautoradiography.

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Formulation and Permeation Kinetic Studies of Flurbiprofen Gel

Abstract: cps, respectively. No irritation or lesions (erythma, redness and ulceration)

Cited by 9 publications

References 3 publications

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

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

The effect of additives on release and in vitro skin retention of flavonoids from emulsion and gel semisolid formulations

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

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