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Andrographolide-loaded nanoparticles for brain delivery: formulation, charcterization and in vitro permeability using hCMEC/D3 cell line

Guccione, Clizia and Oufir, Mouhssin and Piazzini, Vieri and Eigenmann, Daniela Elisabeth and Jähne, Evelyn Andrea and Zabela, Volha and Faleschini, Maria Teresa and Bergonzi, Maria Camilla and Smiesko, Martin and Hamburger, Matthias and Bilia, Anna Rita. (2017) Andrographolide-loaded nanoparticles for brain delivery: formulation, charcterization and in vitro permeability using hCMEC/D3 cell line. European Journal of Pharmaceutics and Biopharmaceutics, 119. pp. 253-263.

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Official URL: http://edoc.unibas.ch/56582/

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Abstract

Andrographolide (AG) is a major diterpenoid of the Asian medicinal plant Andrographis paniculata which has shown exciting pharmacological potential for the treatment of inflammation-related pathologies including neurodegenerative disorders. Conversely, the low bioavailability of AG still represents a limiting factor for its use. To overcome these limitations, AG was loaded into human serum albumin based nanoparticles (HSA NPs) and poly ethylcyanoacrylate nanoparticles (PECA NPs). HSA NPs were prepared by thermal (HSAT AG NPs) and chemical cross-linking (HSAC AG NPs), while PECA AG NPs were produced by emulsion-polymerization. NPs were characterized in terms of size, zeta (ζ)-potential, polydispersity, and release studies of AG. In addition, the ability of free AG and AG-loaded in PECA and HSAT NPs to cross the blood-brain barrier (BBB) was assessed using an in vitro BBB model based on human cerebral microvascular endothelial cell line (hCMEC/D3). For BBB drug permeability assays, a quantitative UPLC-MS/MS method for AG in Ringer HEPES buffer was developed and validated according to international regulatory guidelines for industry. Free AG did not permeate the BBB model, as also predicted by in silico studies. HSAT NPs improved by two-fold the permeation of AG while maintaining the integrity of the cell layer, while PECA NPs temporarily disrupted BBB integrity.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Molecular Modeling (Vedani)
05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmazeutische Biologie (Hamburger)
UniBasel Contributors:Hamburger, Matthias and Eigenmann, Daniela and Smiesko, Martin and Oufir, Mouhssin and Jähne, Evelyn and Faleschini, Maria Teresa and Zabela, Volha
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Elsevier
ISSN:0939-6411
e-ISSN:1873-3441
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:09 May 2018 06:54
Deposited On:09 May 2018 06:54

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