期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 594, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2020.120182
关键词
Deacetylated gellan gum; Nanocrystals; In situ gel; Nose-to-brain; Bioavailability
资金
- Scientific Research Foundation for the National Natural Science Foundation of China [81760715]
- Province Natural Science Foundations of Jiangxi [20202ACB206011, 20202BAB216038]
- youth talent support program of Jiangxi University of traditional Chinese medicine [1141900605]
This study successfully utilized a carbohydrate polymer deacetylated gellan gum (DGG) as matrix to design nanocrystals-based intranasal in situ gel (IG) for nose-to-brain drug delivery, showing excellent therapeutic efficacy.
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 (HARNC) 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 HARNC, 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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