Guiting Huang, Jin Xie, Shuyuan Shuai, Shaofeng Wei, Yingchong Chen, Zhiyu Guan, Qin Zheng, Pengfei Yue, Changhong Wang
International journal of pharmaceutics 2021 Feb 01The 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. Copyright © 2020 Elsevier B.V. All rights reserved.
Guiting Huang, Jin Xie, Shuyuan Shuai, Shaofeng Wei, Yingchong Chen, Zhiyu Guan, Qin Zheng, Pengfei Yue, Changhong Wang. Nose-to-brain delivery of drug nanocrystals by using Ca2+ responsive deacetylated gellan gum based in situ-nanogel. International journal of pharmaceutics. 2021 Feb 01;594:120182
PMID: 33346126
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