Comparative evaluation of rivastigmine permeation from a transdermal system in the Franz cell using synthetic membranes and pig ear skin with in vivo-in vitro correlation

Simon, Alice; Amaro, María Inês; Healy, Anne Marie; Cabral, Lúcio Mendes; Sousa, Valéria Pereira de

doi:10.1016/j.ijpharm.2016.08.052

Cited by 135 publications

(78 citation statements)

References 38 publications

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“…Then the skin was allowed to hydration by phosphate buffer pH 7.4. [32][33][34] Skin integrity was evaluated based on skin electrical impedance measurements (see below). Only undamaged skin pieces were used in the permeation experiments.…”

Section: Methodsmentioning

confidence: 99%

Enhancement of ibuprofen solubility and skin permeation by conjugation with l-valine alkyl esters

et al. 2020

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New ibuprofen derivatives were made via conjugation with L-valine alkyl esters (ValOR), where R was changed from an ethyl to a hexyl group. The ionic structure was confirmed using NMR and FTIR. Specific rotation, solubility in commonly used solvents, thermal properties including phase transitions temperatures, and thermal stability were also determined. The ionic structure with a protonated amine group on an L-valine ester and melting points below 100 C allowed inclusion of these ibuprofen derivatives into the pharmaceutically active protic ionic liquids. The ibuprofen salt solubility in deionised water and two buffer solutions at pH 5.4 and 7.4 were established and compared with the parent acid solubility. The octanol/water (buffer) partition coefficient, permeation through porcine skin, and accumulation in the skin were also measured. Ibuprofen pairing with L-valine alkyl esters [ValOR][IBU], caused higher solubility and a greater drug molecule absorption through biological membranes. log P was lower for ibuprofen salts than for the acid and it increased with a longer L-valine ester cation alkyl chain. In vitro porcine skin tests showed that ibuprofen salts with a propyl or isopropyl ester in L-valine are particularly relevant for topical application. They provide transport for ibuprofen through the skin at much higher rate than the unmodified acid and a higher permeated ibuprofen concentration, which can improve efficacy. Thus, synthesised ibuprofen derivatives could be used as drug carriers in transdermal systems to provide better drug bioavailability, and they can be also be the source of exogenous L-valine.

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Section: Methodsmentioning

confidence: 99%

Enhancement of ibuprofen solubility and skin permeation by conjugation with l-valine alkyl esters

et al. 2020

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“…Onde D é a constante de difusão, k B a constante de Boltzman, T a temperatura absoluta, ηa viscosidade e r o raio da partícula esférica. Na literatura é descrito que partículas de QT-TPP com tamanho médio de até 500 nm apresentam permeabilidade cutânea, porém partículas de tamanhos menores difundem-se mais rapidamente (HASANOVIC et al, 2009;SCHNEIDER et al, 2009 (SIMON et al, 2016;UCHIDA et al, 2015). A figura 10 apresenta os resultados obtidos.…”

Section: Resultsunclassified

Movimento Oculomotor E Algumas Patologias

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et al. 2019

Teorias E Métodos Da Biofísica

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“…The Strat-M™ membrane simulated the skin membrane better than the other artificial membranes. The Strat-M™ membrane had an in vitro-in vivo correlation of 0.991, whereas the other artificial membrane had 0.92 [106]. The Strat-M™ membrane possess synthetic lipids between the polymer layers, which have a porous structure with a thickness around 325 µm.…”

Section: Strat-m™ and Other Artificial Membranesmentioning

confidence: 99%

Alternatives to Biological Skin in Permeation Studies: Current Trends and Possibilities

et al. 2020

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The transdermal route of drugs has received increased attention in recent years due to numerous advantages over the oral and injectable routes, such as avoidance of the hepatic metabolism, protection of drugs from the gastrointestinal tract, sustained drug delivery, and good patient compliance. The assessment of ex vivo permeation during the pharmaceutical development process helps in understanding the product quality and performance of a transdermal delivery system. Generally, excised human skin relevant to the application site or animal skin is recommended for ex vivo permeation studies. However, the limited availability of the human skin and ethical issues surrounding the use of animal skin rendered these models less attractive in the permeation study. In the last three decades, enormous efforts have been put into developing artificial membranes and 3D cultured human skin models as surrogates to the human skin. This manuscript provides an insight on the European Medicines Agency (EMA) guidelines for permeation studies and the parameters affected when using Franz diffusion cells in the permeation study. The need and possibilities for skin alternatives, such as artificially cultured human skin models, parallel artificial membrane permeability assays (PAMPA), and artificial membranes for penetration and permeation studies, are comprehensively discussed.

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Comparative evaluation of rivastigmine permeation from a transdermal system in the Franz cell using synthetic membranes and pig ear skin with in vivo-in vitro correlation

Abstract: 25In the present study, in vitro permeation experiments in a Franz diffusion cell were performed 26 using different synthetic polymeric membranes and pig ear skin to evaluate a rivastigmine

Cited by 135 publications

References 38 publications

Enhancement of ibuprofen solubility and skin permeation by conjugation with l-valine alkyl esters

Enhancement of ibuprofen solubility and skin permeation by conjugation with l-valine alkyl esters

Movimento Oculomotor E Algumas Patologias

Alternatives to Biological Skin in Permeation Studies: Current Trends and Possibilities

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