The Effect of Formulation Excipients on the Penetration and Lateral Diffusion of Ibuprofen on and within the Stratum Corneum Following Topical Application to Humans

Gee, Carol Maying; Watkinson, Adam C.; Nicolazzo, Joseph A.; Finnin, Barrie C.

doi:10.1002/jps.23850

Cited by 17 publications

(7 citation statements)

References 35 publications

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“…Permeation of lidocaine, on the contrary, was diminished to alcohol supplementation to the vehicle compared to pure PBS which served as control. There are also various reports about permeation enhancements of sulfoxides like DMSO [19,21,22], which can increase lipid fluidity and promote drug partition [23,24] or polyols like PG [17,25,26], which are described to solvate α-keratin and occupy hydrogen bonding sites [27,28]. IPM exhibits a direct action on the stratum corneum , permeates into liposome bilayers and increases fluidity of membranes [19,29], but even this aliphatic fatty acid esters diminished lidocaine permeation through equine skin (53,54) comparable to PG.…”

Section: Discussionmentioning

confidence: 99%

The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin

Stahl

Kietzmann

2014

BMC Vet Res

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BackgroundThe effect of physical and chemical permeation enhancers on in vitro transdermal permeation of lidocaine was investigated in the horse.Therefore, the effect of six vehicles (phosphate-buffered saline (PBS), 50% ethanol, 50% propylene glycol, 50% isopropylalcohol, 50% isopropylalcohol/isopropylmyristate and 50% dimethylsulfoxide) was examined as well as the effect of microneedle pretreatment with different needle lengths on transdermal drug delivery of lidocaine.The skin was obtained from the thorax of six Warmblood horses and was stored up to two weeks at - 20°C. Franz-type diffusion cells were used to study the transdermal permeation through split skin (600 μm thickness). The amount of lidocaine in the receptor fluid was determined by UV–VIS high-performance liquid chromatography.ResultsAll investigated vehicle supplementations diminished the transdermal flux of lidocaine through equine skin in comparison to pure PBS except dimethylsulfoxide, which resulted in comparable permeation rates to PBS. The maximum flux (Jmax) was 1.6-1.8 fold lower for lidocaine applied in 50% ethanol, propylene glycol, isopropylalcohol and isopropylalcohol/isopropylmyristate. A significant higher Jmax of lidocaine was observed when lidocaine was applied in PBS onto microneedle pretreated skin with similar permeation rates in both needle lengths. After 6 hours, 1.7 fold higher recovery rates were observed in the microneedle pretreated skin samples than in the untreated control samples. The lagtimes were reduced to 20–50% in the microneedle pretreated skin samples.ConclusionMicroneedles represent a promising tool for transdermal lidocaine application in the horse with a rapid systemic bioavailability.

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Section: Discussionmentioning

confidence: 99%

The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin

Stahl

Kietzmann

2014

BMC Vet Res

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“…Вместе с тем для создания терапевтической концентрации препарата в тканях необходимо его применение вместе с веществами, облегчающими его проникновение через кожу. С этой целью широко используется диизопропаноламин [23], входящий в состав лекарственной формы геля Дип Рилиф. Диизопропаноламин обеспечивает создание электрически нейтрального комплекса и глубокое проникновение активной субстанции в ткани-мишени.…”

Section: локальное трансдермальное применение лекарственных средствunclassified

Drugs for Local Transdermal Use in Treating Patients With Dorsalgia

2017

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Под термином «дорсопатии» (ДП) в настоящее время подразумевают болевые синдромы в области спины невисцеральной этиологии, связанные с дегенеративными заболеваниями позвоночника. Важнейшей разновидностью дорсопатий является дорсалгия-боль в спине, которая, по определению экспертов ВОЗ, в конце XX в. приобрела характер неинфекционной эпидемии, поскольку ею страдают в течение жизни около 80% населения. Дорсалгия (ДА)-исключительно распространенный в популяции скелетно-мышечный болевой синдром. Для лечения пациентов с ДА широко используются нестероидные противовоспалительные препараты (НПВП), оказывающие выраженные противоболевой и противовоспалительный эффекты. Их назначение зачастую ассоциировано с риском развития побочных эффектов, возрастающим у пожилых пациентов с полиморбидностью, нуждающихся в одновременном приеме нескольких лекарственных препаратов. Альтернативой системного применения НПВП в ряде случаев может явиться локальное введение трансдермальных форм лекарственных препаратов. Рассматривается возможность применения препаратов Дип Рилиф и Дип Хит у больных с ДА в зависимости от особенностей клинической картины заболевания. Приводятся результаты исследований, посвященных изучению биодоступности препаратов, их эффективности и переносимости.

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“…The phosphorimaging method is complementary to two other recently developed techniques in which either fluorescence after photo-bleaching (FRAP) [18] or high resolution infrared (IR) spectroscopy [19] was used to obtain similar information on lateral transport rates in skin. Development of these molecular imaging procedures overcomes many of limitations imposed by previous methods that rely on the analysis of dissected tissues [20][21][22][23][24][25].…”

Section: Introductionmentioning

confidence: 99%

A quantitative radioluminographic imaging method for evaluating lateral diffusion rates in skin

Rush

Miller

Smith

et al. 2015

Journal of Controlled Release

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The Effect of Formulation Excipients on the Penetration and Lateral Diffusion of Ibuprofen on and within the Stratum Corneum Following Topical Application to Humans

Cited by 17 publications

References 35 publications

The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin

The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin

Drugs for Local Transdermal Use in Treating Patients With Dorsalgia

A quantitative radioluminographic imaging method for evaluating lateral diffusion rates in skin

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