A novel formulation of zolpidem for direct nose-to-brain delivery : synthesis, encapsulation and intranasal administration to mice. / Borodina, Tatiana; Marchenko, Irina; Trushina, Daria; Volkova, Yulia; Shirinian, Valerii; Zavarzin, Igor; Kondrakhin, Evgeny; Kovalev, Georgy; Kovalchuk, Mikhail; Bukreeva, Tatiana.
In: Journal of Pharmacy and Pharmacology, Vol. 70, No. 9, 09.2018, p. 1164-1173.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - A novel formulation of zolpidem for direct nose-to-brain delivery
T2 - synthesis, encapsulation and intranasal administration to mice
AU - Borodina, Tatiana
AU - Marchenko, Irina
AU - Trushina, Daria
AU - Volkova, Yulia
AU - Shirinian, Valerii
AU - Zavarzin, Igor
AU - Kondrakhin, Evgeny
AU - Kovalev, Georgy
AU - Kovalchuk, Mikhail
AU - Bukreeva, Tatiana
N1 - Publisher Copyright: © 2018 Royal Pharmaceutical Society
PY - 2018/9
Y1 - 2018/9
N2 - 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 mesoporous calcium carbonate particles modified by diethylaminoethyl-dextran/hyaluronic acid shell has a pronounced anxiolytic effect on the behaviour of the animals in the open field test. Conclusions: The polyelectrolyte shell deposited together with zolpidem enhances the loading efficacy of the microcontainers. In vivo experiments on mice demonstrate increase in anxiolytic effect of zolpidem in microcontainers compared with upon intranasal administration of free medicine.
AB - 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 mesoporous calcium carbonate particles modified by diethylaminoethyl-dextran/hyaluronic acid shell has a pronounced anxiolytic effect on the behaviour of the animals in the open field test. Conclusions: The polyelectrolyte shell deposited together with zolpidem enhances the loading efficacy of the microcontainers. In vivo experiments on mice demonstrate increase in anxiolytic effect of zolpidem in microcontainers compared with upon intranasal administration of free medicine.
KW - anxiolytic effect
KW - intranasal delivery
KW - microcontainers
KW - zolpidem
UR - http://www.scopus.com/inward/record.url?scp=85051105425&partnerID=8YFLogxK
U2 - 10.1111/jphp.12958
DO - 10.1111/jphp.12958
M3 - Article
C2 - 29956328
AN - SCOPUS:85051105425
VL - 70
SP - 1164
EP - 1173
JO - Journal of Pharmacy and Pharmacology
JF - Journal of Pharmacy and Pharmacology
SN - 0022-3573
IS - 9
ER -
ID: 88199912