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A novel formulation of zolpidem for direct nose-to-brain delivery: synthesis, encapsulation and intranasal administration to mice

Borodina T. N., Marchenko I., Trushina D. B., Volkova Y., Shirinian V., Zavarzin I., Kondrakhin E., Kovalev G., Kovalchuk M., Bukreeva T.
Journal of Pharmacy and Pharmacology
Vol.70, Issue9, P. 1164-1173
Опубликовано: 2018
Тип ресурса: Статья

DOI:10.1111/jphp.12958

Аннотация:
Objectives: Anxiolytic drug zolpidem was incorporated into the microcontainers based on mesoporous calcium carbonate particles modified by diethylaminoethyl-dextran/hyaluronic acid shell. The release of zolpidem in saline solution and in polymer film modelling nasal mucosa was investigated. The anxiolytic effect of zolpidem upon intranasal administration of microcontainers and free medicine was determined by in vivo experiments on mice. Methods: The structures of all compounds during zolpidem synthesis were established using nuclear magnetic resonance spectroscopy. The loading efficacy and release kinetics of zolpidem were analysed by spectrophotometry. Surface morphology of formulation was investigated by scanning electron microscopy. To determine the effect of zolpidem-loaded containers administration by the intranasal route in vivo experiments was carried out applying the open field test. Key findings: Nasal administration of zolpidem in the form of the microcontainers based on meso
Ключевые слова:
anxiolytic effect; intranasal delivery; microcontainers; zolpidem
alginic acid; calcium carbonate; hyaluronic acid; polymer; sodium chloride; zolpidem; hypnotic sedative agent; zolpidem; animal experiment; Article; controlled study; drug coating; drug determination; drug efficacy; drug formulation; drug release; drug structure; drug synthesis; in vivo study; male; microcontainer; microencapsulation; mouse; nonhuman; nose mucosa; nuclear magnetic resonance spectroscopy; open field test; scanning electron microscopy; spectrophotometry; structure analysis; tranquilizing activity; animal; Bagg albino mouse; brain; drug delivery system; drug effect; drug formulation; intranasal drug administration; procedures; synthesis; Administration, Intranasal; Animals; Brain; Drug Compounding; Drug Delivery Systems; Hypnotics and Sedatives; Male; Mice; Mice, Inbred BALB C; Nasal Mucosa; Zolpidem
Язык текста: Английский
ISSN: 2042-7158
Borodina T. N. Tat`yana Nikolaevna 1982-
Marchenko I.
Trushina D. B. Dar`ya Borisovna 1989-
Volkova Y.
Shirinian V.
Zavarzin I.
Kondrakhin E.
Kovalev G.
Kovalchuk M.
Bukreeva T.
Бородина Т. Н. Татьяна Николаевна 1982-
Марченко И.
Трушина Д. Б. Дарья Борисовна 1989-
Волкова Y.
Шириниан В.
Заварзин И.
Кондрахин Е.
Ковалев Г.
Ковалчук М.
Букреева Т.
A novel formulation of zolpidem for direct nose-to-brain delivery: synthesis, encapsulation and intranasal administration to mice
Текст визуальный непосредственный
Journal of Pharmacy and Pharmacology
Pharmaceutical Press
Vol.70, Issue9 P. 1164-1173
2018
Статья
anxiolytic effect intranasal delivery microcontainers zolpidem
alginic acid calcium carbonate hyaluronic acid polymer sodium chloride zolpidem hypnotic sedative agent zolpidem animal experiment Article controlled study drug coating drug determination drug efficacy drug formulation drug release drug structure drug synthesis in vivo study male microcontainer microencapsulation mouse nonhuman nose mucosa nuclear magnetic resonance spectroscopy open field test scanning electron microscopy spectrophotometry structure analysis tranquilizing activity animal Bagg albino mouse brain drug delivery system drug effect drug formulation intranasal drug administration procedures synthesis Administration, Intranasal Animals Brain Drug Compounding Drug Delivery Systems Hypnotics and Sedatives Male Mice Mice, Inbred BALB C Nasal Mucosa Zolpidem
Objectives: Anxiolytic drug zolpidem was incorporated into the microcontainers based on mesoporous calcium carbonate particles modified by diethylaminoethyl-dextran/hyaluronic acid shell. The release of zolpidem in saline solution and in polymer film modelling nasal mucosa was investigated. The anxiolytic effect of zolpidem upon intranasal administration of microcontainers and free medicine was determined by in vivo experiments on mice. Methods: The structures of all compounds during zolpidem synthesis were established using nuclear magnetic resonance spectroscopy. The loading efficacy and release kinetics of zolpidem were analysed by spectrophotometry. Surface morphology of formulation was investigated by scanning electron microscopy. To determine the effect of zolpidem-loaded containers administration by the intranasal route in vivo experiments was carried out applying the open field test. Key findings: Nasal administration of zolpidem in the form of the microcontainers based on meso