Effect of the transfer activator on functional properties of the bromocain matrix transdermal therapeutic systems

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This paper demonstrates a chemical way of enhancing transdermal delivery using immunomodulator glucosaminylmuramyl dipeptide (GMDP) as an example. Objective: to study in vitro the effect of various components of the microemulsion composition on GMDP diffusion through the skin from a transdermal therapeutic system (TTS). Materials and methods. Medicinal substance – glucosaminylmuramyl dipeptide (Peptek, Russia). Excipients and raw materials: sodium chloride, purified water, sodium dodecyl sulfate, docusate sodium, oak bark, apricot kernel oil, alpha-tocopheryl acetate and Decaglyn PR-20 emulsifier. Equipment: Heidolph DIAX 900 mechanical disperser (Germany) and Hielscher UIS250V ultrasonic homogenizer (Germany). GMDP diffusion from TTS through unpreserved rabbit skin was studied on diffusion tester Copley (UK). GMDP in aqueous solutions was determined by reversed-phase high-performance liquid chromatography (RP-HPLC) on an Agilent 1200 chromatography system (Agilent Technologies, USA). Results. A microemulsion system composed of 20% docusate sodium in an oil phase and an oak bark decoction as an aqueous phase was developed. This made it possible to increase GMDP transdermal delivery by ~70% in comparison with the basic composition. Conclusion. The characteristic parameters of microemulsion components of GMDP contained in TTS, influencing GMDP diffusion through unpreserved rabbit skin in vitro, were determined. Introducing relative indicators would be advisable in order to correctly evaluate the results of different series of in vitro experiments with biological objects.

Section: Influence Of Microemulsion Components On Transdermal Deliverunclassified

Influence of microemulsion components on transdermal delivery of immunomodulator glucosaminylmuramyl dipeptide

Кузнецова¹,

Kuryleva²,

Salomatina³

et al. 2020

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“…Ранее было показано, что присутствие в эмульсионной матрице докузатнатриевой соли в качестве переносчика ЛВ увеличивает скорость чрескожной диффузии [8].…”

Section: таблица 1 расчет относительного среднеквадратичного отклоненunclassified

The cyclosporine transdermal transfer possibility study on model systems

Кузнецова¹,

Kuryleva²,

Salomatina³

et al. 2019

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Aim: to develop the emulsion transdermal therapeutic system (TTS) of cyclosporine and the research of its diffusion from TTS.Materials and methods. The quantitative evaluation of cyclosporine in model media was performed on liquid chromatograph Agilent 1100 G1311 with spectrophotometric detector G1315B (Germany). For the production of the emulsion matrix, the Heidolph DIAX900 disperser (Germany) and the ultrasonic homogenizer Hielscher UIS250V (Germany) were used. The cyclosporine diffusion from TTS through Strat-M membrane (25 mm in diameter, Merck Millipore) was studied using Copley diffusion analyser (Great Britain).Results. Using the developed method of micro-HPLC, it was established that the amount of cyclosporine passed through the Strat-M membrane over 24 hours from 10 sm2 TTS, containing 173 mg of the substance, was 5.9 mg. The estimated blood concentration is ~ 50 ng/ml which corresponds to the therapeutic maintenance blood concentration during organ transplantation (50–75 ng/ml).Conclusion. The model studies demonstrate the possibility of the cyclosporine transdermal transfer.

“…Диффузию инсулина из ТТС через неконсервированную кожу кролика изучали in vitro в стеклянных ячейках Франца [16] при непрерывном перемешивании при 32 °С на анализаторе диффузии лекарственных препаратов HDT 1000 (Copley Scientifi c Ltd., Великобритания) (рис. 3) с последующей регистрацией спектров поглощения рабочих растворов на спектрофотометре UV-2600 (Shimadzu, Япония).…”

Section: изучение скорости диффузии инсулина в ячейках францаunclassified

Microneedles as a Way to Increase the Transdermal Insulin Delivery

Кузнецова

Ryzhikova

Salomatina

et al. 2017

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Aim: to prove the possibility of increasing the diffusion of insulin through the skin in vitro with pre-applying microneedles.Materials and methods. Microemulsion for transdermal therapeutic system of insulin has been used in vitro studies. Genetically engineered human insulin has been used in this research. Applicators with silicon microneedles (40 and 150 microns long) have been used to enhance the diffusion fl ux of drug substance. The dynamics of insulin release from the transdermal therapeutic systems through the rabbit skin has been studied in glass Franz diffusion cells in analyzer diffusion of drugs HDT 1000 (Copley Scientifi c Ltd., UK). Insulin has been labeled with fl uorescein isothiocyanate to separate the insulin absorption spectrum from the spectra of native skin proteins at spectrophotometer measurements.Results. The amounts of insulin delivered through the skin in vitro after previous application of microneedles of 40 and 150 microns are 282.5 ± 61.1 and 372.3 ± 7.0 microgram, respectively. This is 1.4 and 1.9 times more than in the transdermal system without microneedles.Conclusion.The conditions for increasing the diffusion of insulin through the skin in a model transdermal therapeutic system with microneedles (length – 150 microns, duration of pre-application – 1 hour) have been found.