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Cited by 60Advanced Drug Delivery SystemsInhalation and Respiratory Drug DeliveryAdvancements in Transdermal Drug Delivery

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Nose-to-brain delivery of drug nanocrystals by using Ca2+ responsive deacetylated gellan gum based in situ-nanogel

Huang, Guiting, Xie, Jin, Shuai, Shuyuan, Wei, Shaofeng, Chen, Yingchong, Guan, Zhiyu, Zheng, Qin, Yue, Pengfei, Wang, Changhong·2021·International Journal of Pharmaceutics
DOI 10.1016/j.ijpharm.2020.120182
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Abstract

The objective of this study is to use a carbohydrate polymer deacetylated gellan gum (DGG) as matrix to design nanocrystals based intranasal in situ gel (IG) for nose-to -brain delivery of drug. The harmine nanocrystals (HAR-NC) as model drug were prepared by coupling homogenization and spray-drying technology. The HAR-NC was redispersed in the (DGG) solutions and formed the ionic-triggered harmine nanocrystals based in situ gel (HAR-NC-IG). The crystal state of HAR remained unchanged during the homogenization and spray-drying. And the HAR-NC-IG with 0.5% DGG exhibited excellent in situ-gelation ability, water retention property and in vitro release behavior. The bioavailability in brain of intranasal HAR-NC-IG were 25-fold higher than that of oral HAR-NC, which could be attributed to nanosizing effect of HAR-NC and bioadhesive property of DGG triggered by nasal fluid. And the HAR-NC-IG could significantly inhibit the expression of acetylcholinesterase (AchE) and increase the content of acetylcholin (ACh) in brain compared with those of reference formulations (p < 0.01). The DGG based nanocrystals-in situ gel was a promising carrier for nose-to-brain delivery of poorly soluble drug, which could prolong the residence time and improve the bioavailability of poorly soluble drugs in brain.

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Metadata

Authors
Huang, G., Xie, J., Shuai, S., Wei, S., Chen, Y., Guan, Z., Zheng, Q., Yue, P., & Wang, C.
Affiliations
  • Jiangxi University of Traditional Chinese Medicine (CN)
  • Shanghai University of Traditional Chinese Medicine (CN)
Corresponding author
  • Yue, Pengfei
  • Wang, Changhong
ORCID
Venue
International Journal of Pharmaceutics
Publisher
Elsevier BV
Published
2021-02
Volume
594
Pages
120182
ISSN
0378-5173 (ISSN-L)
DOI
10.1016/j.ijpharm.2020.120182
OpenAlex
W3113261592
Cited by
60
References
1
Citations by year
2026: 7 · 2025: 10 · 2024: 14 · 2023: 14 · 2022: 10 · 2021: 5
FWCI
2.82
Type
journal article
Language
en
Open access
closed
Licence
Locations
  • International Journal of Pharmaceutics (publishedVersion)
  • PubMed (publishedVersion)
Funders
National Natural Science Foundation of China
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
Keywords
nose-to-brain delivery, harmine, in situ gel, drug nanocrystals, intranasal drug delivery, poorly water-soluble drugs, brain bioavailability, acetylcholinesterase inhibition, acetylcholine, spray drying, homogenization, bioadhesion, nasal fluid
MeSH terms
Nanogels, Brain, Gels, Polysaccharides, Bacterial, Nanoparticles

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