Characterization of the Percutaneous Absorption of Ketoprofen Using the Franz Skin Finite Dose Model

Bassani, August S; Banov, Daniel; Phan, Ha

doi:10.1080/00325481.2016.1144448

Cited by 8 publications

(8 citation statements)

References 12 publications

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“…10 While Lipoderm has, to date, not been subject to the same scrutiny as PLO, it has been shown to facilitate better transdermal absorption of select pharmaceuticals, such as ketoprofen. 15 Transdermal quetiapine delivery has not been quantitatively studied in a PLO delivery vehicle to our knowledge, so a direct comparison cannot be made. Interestingly, Thomas and Holroyd reported symptomatic improvement in a case series of elderly patients with dementia who were prescribed quetiapine and venlafaxine formulated in PLO, though serum levels of either drug were not collected.…”

Section: Discussionmentioning

confidence: 99%

A Lack of Systemic Absorption Following the Repeated Application of Topical Quetiapine in Healthy Adults

Kayhart

Lapid

Nelson

et al. 2018

Am J Hosp Palliat Care

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In the absence of suitable oral or intravenous access for medication administration and when the intramuscular medications are undesirable, alternative routes for drug delivery may be considered. Antipsychotics administered via an inhaled, intranasal, rectal, or topical route have been described in the literature. Topically administered antipsychotics have been previously reported to produce negligible systemic absorption despite being used in clinical practice for nausea and behavioral symptoms associated with dementia. Additionally, the American Academy of Hospice and Palliative Medicine recommends against the use of topical medications that lack supporting literature. Three studies have assessed the systemic absorption of different antipsychotics after administration of only a single, topically applied dose. To evaluate whether the repeated administration of a topically applied antipsychotic may result in detectable serum levels in an accumulating fashion, a pharmacokinetic study was conducted. Five healthy, adult participants consented to receive extemporaneously prepared topical quetiapine in Lipoderm every 4 hours for a total of 5 doses. Blood samples were drawn at baseline and hours 2, 4, 8, 12, 16, and 24, and serum quetiapine concentrations were measured using high-performance liquid chromatography. Quetiapine was undetectable in every sample from 3 participants. Two participants had minimally detectable serum quetiapine levels no sooner than hour 12 of the study period. Extemporaneously prepared quetiapine in Lipoderm resulted in nonexistent or minimal serum level following repeated topical administration. The use of topically applied quetiapine should still be questioned.

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Section: Discussionmentioning

confidence: 99%

A Lack of Systemic Absorption Following the Repeated Application of Topical Quetiapine in Healthy Adults

Kayhart

Lapid

Nelson

et al. 2018

Am J Hosp Palliat Care

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“…The European Union Reference Laboratory (UELR ECVAM) has recommended the use of the human EpiDerm system (EPI-200) as an alternative to the commonly used Draize test. 6,7 The model, purchased from MatTek (Ashland, MA), contained normal human-derived epidermal keratinocytes. The three-dimensional system was maintained with the special culture media provided by the manufacturer.…”

Section: Cytotoxicity Assaymentioning

confidence: 99%

“…Although both gels facilitated the percutaneous absorption of ketoprofen across human cadaver trunk skin, the Lipoderm formulation showed faster rate and higher mean total absorption of ketoprofen than when in PLO. 6 Lipoderm, however, is an aqueous compounding base, which may provide a shorter default beyond-use date (BUD) for active pharmaceutical ingredients (API). This concern underscores the importance of finding an alternative base that provides a longer default BUD.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of the in vitro human skin percutaneous absorption of ketoprofen in topical anhydrous and aqueous gels

Ip,

Song,

Banov

et al. 2024

Skin Research and Technology

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BackgroundKetoprofen is a nonsteroidal anti‐inflammatory drug used for the treatment of acute and chronic pain associated with inflammatory conditions. This study aims to evaluate the in vitro percutaneous absorption of ketoprofen 10% formulated in proprietary anhydrous and aqueous gels using the Franz skin finite dose model.Materials and MethodsThe anhydrous gel was initially characterized for cytotoxicity using EpiDerm skin tissue model by cell proliferation assay and Western blot analysis. The Ultra Performance Liquid Chromatography method for measuring ketoprofen was validated and the stability of ketoprofen 10% in the anhydrous gel formulation was evaluated at 5°C and 25°C for 181 days. The percutaneous absorption of ketoprofen was determined using donated human skin. The tissue sections were mounted within Franz diffusion cells. A variable finite dose of each ketoprofen formulation in either anhydrous or aqueous gel was applied to the skin sections and receptor solutions were collected at various time points.ResultsCell proliferation assay showed minimal cell death when EpiDerm skin tissue was exposed to the anhydrous gel for 24 h; the levels of protein markers of cell proliferation were not affected after 17‐h exposure. Ketoprofen was stable in the anhydrous gel when stored at 5°C and 25°C. When compounded in the anhydrous and aqueous gels, ketoprofen had mean flux rate of 2.22 and 2.50 μg/cm2/h, respectively, after 48 h. The drug was distributed to the epidermis and dermis sections of the skin. Both the anhydrous and aqueous gels facilitated the percutaneous absorption of ketoprofen without statistically significant differences.ConclusionThe anhydrous gel can be used as a base to facilitate the transdermal delivery of ketoprofen. Although the anhydrous and aqueous gels can deliver a similar amount of ketoprofen, the anhydrous gel (water activity below 0.6) allows for extended default beyond‐use‐date of compounding preparations.

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“…The chemical composition of the compounding bases for topical formulations plays a key role in the penetration of the APIs across the skin barrier. [11][12][13][14] Lipoderm and Lipoderm HMW, also referred to as phospholipid bases, are proprietary compounding bases likely to increase the permeation of drugs. Lipoderm HMW, in particular, was designed to deliver HMW drugs into and through the skin.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of a compounding phospholipid base for the percutaneous absorption of high molecular weight drugs using the Franz finite dose model

Banov,

Song,

Carvalho

et al. 2024

Skin Research and Technology

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BackgroundPermeation‐enhancing compounding bases are aimed to facilitate the penetration of the active pharmaceutical ingredients (APIs) across the skin barrier.ObjectivesThe purpose of this study was to evaluate the percutaneous absorption of radiolabeled human insulin (14C‐isototpe) when incorporated in a proprietary phospholipid base designed to deliver APIs with high molecular weights (HMW). The aim was not to claim the transdermal delivery of insulin with potential therapeutic applications in diabetes but, instead, to evaluate the ability of the compounding phospholipid base to deliver HMW drugs.MethodsThe percutaneous absorption of 14C‐insulin was determined using human torso skin and the Franz skin finite dose model. Two topical test formulations were prepared for in vitro evaluation: insulin 1% in phospholipid base (standard) and insulin 1% in phospholipid base HMW. The rate of percutaneous absorption (mean flux) and the distribution of 14C‐insulin through the skin were evaluated for both topical test formulations. A two‐way ANOVA was used to determine statistical differences.ResultsThe 14C‐insulin was distributed into the stratum corneum, epidermis and dermis. Mean flux values showed a rapid penetration upon application and the maximum flux was achieved at 30 min, followed by a slow decline. Subsequently, a slower decline was observed for the topical test formulation including the phospholipid base HMW.ConclusionThe phospholipid base HMW facilitates the percutaneous absorption of HMW drugs across human cadaver skin and, therefore, it may potentially be a useful option for compounding pharmacists and practitioners when considering the skin for the percutaneous delivery of large drugs.

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Characterization of the Percutaneous Absorption of Ketoprofen Using the Franz Skin Finite Dose Model

Cited by 8 publications

References 12 publications

A Lack of Systemic Absorption Following the Repeated Application of Topical Quetiapine in Healthy Adults

A Lack of Systemic Absorption Following the Repeated Application of Topical Quetiapine in Healthy Adults

Evaluation of the in vitro human skin percutaneous absorption of ketoprofen in topical anhydrous and aqueous gels

Evaluation of a compounding phospholipid base for the percutaneous absorption of high molecular weight drugs using the Franz finite dose model

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