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Разработка и регистрация лекарственных средств

Расширенный поиск

Интраназальное введение как способ доставки лекарств в головной мозг (обзор)

https://doi.org/10.33380/2305-2066-2021-10-4-117-127

Полный текст:

Аннотация

Введение. Интраназальная доставка лекарственных средств напрямую из носа в мозг является одним из многообещающих направлений для лечения заболеваний головного мозга, включающих нейродегенеративные расстройства, инсульт, опухоли головного мозга и т. д.

Текст. Доставка лекарства через нос имеет ряд преимуществ, среди которых быстрое наступление фармакологического эффекта, возможность обхода гематоэнцефалического барьера, снижение вероятности возникновения побочных эффектов, а также быстрый и неинвазивный способ введения. Однако существенными недостатками данного пути является сравнительно быстрое вымывание с поверхности слизистой оболочки, плохое проникновение лекарства через слизистую носа, мукоцилиарный клиренс и действие протеолитических ферментов. В настоящее время для преодоления вышеуказанных ограничений используются различные направления, среди которых следует отметить разработку систем доставки из носа в мозг, представляющих собой мукоадгезивные, мукус-проникающие и гелеобразующие системы, способствующие удерживанию или проникновению лекарств через слизистую оболочку. При этом значительную роль при конструировании такого рода систем занимают высокомолекулярные соединения. В частности, мукоадгезивные системы могут быть получены из катионных и анионных полимеров. Недавние исследования также показали проявление мукоадгезивных свойств у интерполиэлектролитных комплексов. Увеличение мукоадгезивных свойств полимеров при конструировании систем доставки лекарств может быть также достигнуто путем присоединения к ним различных функциональных групп, таких как тиолы, малеимиды, акрилаты, метакрилаты, катехолы и т. д. Мукус-проникающие системы могут быть получены путем ПЭГилирования наночастиц, а также функционализацией с помощью некоторых поли-(2-оксазолинов), поливинилового спирта и др., что было показано на других слизистых оболочках организма. Наконец, увеличение проникновения возможно достичь путем использования муколитических средств в комбинации с неионогенными поверхностно-активными веществами. Другим подходом для увеличения эффективности доставки лекарств из носа в мозг является использование гелеобразующих систем. В частности, актуальным является гелеобразование in situ. Данный вид гелей на первом этапе представляет собой раствор, в дальнейшем в ответ на химическое и физическое воздействие происходит фазовый переход, сопровождающийся образованием геля. В зависимости от внешней стимуляции фазового перехода различают термо-, рН-, ионообратимые и другие системы, показавшие свою эффективность для доставки в мозг путем интраназального введения.

Заключение. Эффективная интраназальная доставка лекарственных средств и терапевтических агентов в мозг может быть достигнута путем использования мукоадгезивных, мукус-проникающих и гелеобразующих систем и/или их комбинаций.

Об авторах

Н. Н. Порфирьева
Институт фармации, ФГБОУ ВО Казанский ГМУ Минздрава России
Россия

420126, Республика Татарстан, Казань, ул. Фатыха Амирхана, д. 16



И. И. Семина
Центральная научно-исследовательская лаборатория, ФГБОУ ВО Казанский ГМУ Минздрава России
Россия

420012, Республика Татарстан, Казань, ул. Толстого, д. 6



Р. И. Мустафин
Институт фармации, ФГБОУ ВО Казанский ГМУ Минздрава России; Центральная научно-исследовательская лаборатория, ФГБОУ ВО Казанский ГМУ Минздрава России
Россия

Мустафин Руслан Ибрагимович

420126, Республика Татарстан, г. Казань, ул. Фатыха Амирхана, д. 16; 420012, Республика Татарстан, Казань, ул. Толстого, д. 6



В. В. Хуторянский
Институт фармации, ФГБОУ ВО Казанский ГМУ Минздрава России; Reading School of Pharmacy, University of Reading
Россия

420126, Республика Татарстан, г. Казань, ул. Фатыха Амирхана, д. 16; Whiteknights, PO box 224, Reading RG66AD



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Для цитирования:


Порфирьева Н.Н., Семина И.И., Мустафин Р.И., Хуторянский В.В. Интраназальное введение как способ доставки лекарств в головной мозг (обзор). Разработка и регистрация лекарственных средств. 2021;10(4):117-127. https://doi.org/10.33380/2305-2066-2021-10-4-117-127

For citation:


Porfiryeva N.N., Semina I.I., Moustafine R.I., Khutoryanskiy V.V. Intranasal Administration as a Route to Deliver Drugs to the Brain (Review). Drug development & registration. 2021;10(4):117-127. (In Russ.) https://doi.org/10.33380/2305-2066-2021-10-4-117-127

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