Development of a transdermal formulation based on nanocellulose

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Introduction. In many countries, dosage forms of dosed, continuous administration of medicinal substances (MS) into the bloodstream through the skin have been developed; they are able to bypass the gastrointestinal tract (GIT) and do not have the disadvantages of injection. In transdermal therapeutic systems, the permeability, as well as the release of MS, occurs due to the polymer layers of the membrane. Nanocellulose is one of the promising materials among polymeric compounds for creating films; it is characterized by good stability, large surface area, optimal mechanical and optical properties. Objective: to develop the compositions of transdermal formulations based on nanocellose and medicinal substances (5 items). Material and methods. Nanofibrillar cellulose (cotton, wood, linen) was obtained by high-intensity mechanical processing of cotton, wood and linen cellulose fibers, on an APV2000-Lab high-pressure homogenizer, working pressure of homogenization 110 MPa. Substances of dexpanthenol, acyclovir, roxithromycin, tetracycline, levomycetin were provided by «Tatkhimfarmpreparaty» JSC. The rate of release of the active substance from the film was carried out in accordance with the requirements of GPM.1.4.2.0017.15 «Dissolution for transdermal patches». The amount of released MS was estimated by UV spectrophotometry using a Shimadzu instrument (Japan). Results. Films of the composition nanocellulose (cotton) - dimethyl sulfoxide - ethyl alcohol - medicinal substance were obtained; they were dense, stable, with dissolved and evenly distributed medicinal substance, without drying out and cracks. Evaluation of the drug release from the film showed that tetracycline, acyclovir, levomycetin are well released, in contrast to them, roxithromycin is not released, and presumably forms bonds with the film components. Conclusion. The obtained results of the development of a transdermal formulation and the evaluation of the release of MS make it possible to recommend nanofibrillar cellulose for further research as a component for creating soft dosage forms.

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作者简介

Lydia Spatlova

Kazan National Research Technological University

Email: lidamet@inbox.ru
Associate Professor 俄罗斯联邦,

Vladimir Petrov

Kazan National Research Technological University

Email: ptrv@kstu.ru
Professor 俄罗斯联邦,

Marat Gibadullin

Kazan National Research Technological University

Email: gibalullinmr@corp.knrtu.ru
Associate Professor 俄罗斯联邦,

Natalia Averyanov

Kazan National Research Technological University

编辑信件的主要联系方式.
Email: natalia.v.averianova@gmail.com
Associate Professor 俄罗斯联邦,

参考

  1. Dufresne A. Nanocellulose: a new ageless bionanomaterial. Materials today. 2013; 16 (6): 220-7.
  2. Петров В.А., Гибадуллин М.Р., Аверьянова Н.В. Получение наноразмерной целлюлозы области ее применения. Вестник Казанского технологического университета. 2014; 17 (20): 58-60.
  3. Яремчук А.А., Хишова О.М., Половко Н.П. Изучение осмотических свойств декспантенола. Режим доступа http://dspace.nuph.edu.ua/bitstream/123456789/7643/1/114.pdf
  4. Петров А.А., Аверьянова Н.В. Гибадуллин М.Р., Хамматов И.А. Структурные особенности микрофибриллярной целлюлозы из различного сырья. Вестник технологического университета. 2013; 16 (23): 50-1.

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2. Рис. 1. Электронные микрофотографии пленок наноцеллюлозы, полученной из: а) древесной целлюлозы, б) льняной целлюлозы, в) хлопковой целлюлозы

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3. Рис. 2. Пленки состава наноцеллюлоза: а) древесная – декспантенол, б) льняная – декспантенол, в) хлопковая – декспантенол

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4. Рис. 3. Пленки состава наноцеллюлоза (хлопоквая)-ДМСО-этиловый спирт – лекарственное вещество: 1 – ацикловир, 2 – рокситромицин, 3-тетрациклин, 4 – левомицетин

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5. Рис. 4. УФ-спектр высвобождения ацикловира из пленки наноцеллюлоза (хлопковая) – декспантенол при временах 1–5 мин, 2–15 мин, 3–30 мин, 4–45 мин, 5–60 мин с различными лекарственными веществами: а) ацикловир; б) левомицетин; в) тетрациклин; г) рокситромицин

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