Lipid nanoconstructs for superior hepatoprotection: In vitro assessments as predictive tool for in vivo translation

[Display omitted] To investigate comparative in vitro and in vivo performance of lipid vesicular and particulate systems in escalating oral bioavailability for superior hepatoprotection. Systems were fabricated using easy to scale up process and novel excipients to deliver Silibinin. In vitro charac...

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Bibliographic Details
Published in:International journal of pharmaceutics 2020-04, Vol.579, p.119176, Article 119176
Main Authors: Dhawan, V., Sutariya, B., Lokras, A., Thamm, J., Saraf, M., Warawdekar, U., Fahr, A., Nagarsenker, M.
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Biological Availability
Carbon Tetrachloride
Chemical and Drug Induced Liver Injury - prevention & control
Drug Liberation
Drug Stability
Excipients - chemistry
Female
GeluPearl
Hepatoprotection
In Vitro Techniques
LeciPlex
Lipid nanosystems
Lipids - chemistry
Liver
Liver - enzymology
Nanotechnology - methods
Oral bioavailability
Particle Size
Permeability
Rats
Silibinin
Silybin - blood
Silybin - chemistry
Silybin - pharmacokinetics
Silybin - pharmacology
Solubility
Surface Properties
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Summary:[Display omitted] To investigate comparative in vitro and in vivo performance of lipid vesicular and particulate systems in escalating oral bioavailability for superior hepatoprotection. Systems were fabricated using easy to scale up process and novel excipients to deliver Silibinin. In vitro characterization followed by pharmacokinetic and pharmacodynamic evaluation in rats was conducted to establish a correlation. Nanoformulations resulted in 20 fold increase in solubilisation and significant increase in permeation. 2.5 fold increase in bioavailability was evident in vivo. Vesicles demonstrated greatest hepatoprotective potential in efficacy study. The findings establish a link between in vitro and in vivo performance to rank order lipid nanoartchitects. Concurrently, a significant potential in therapeutic intervention of hepatotoxicity is envisaged as elucidated.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2020.119176