Lipid nanoconstructs for superior hepatoprotection: In vitro assessments as predictive tool for in vivo translation
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Lipid nanoconstructs for superior hepatoprotection : In vitro assessments as predictive tool for in vivo translation. / Dhawan, V.; Sutariya, B.; Lokras, A.; Thamm, J.; Saraf, M.; Warawdekar, U.; Fahr, A.; Nagarsenker, M.
In: International Journal of Pharmaceutics, Vol. 579, 119176, 2020.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Lipid nanoconstructs for superior hepatoprotection
T2 - In vitro assessments as predictive tool for in vivo translation
AU - Dhawan, V.
AU - Sutariya, B.
AU - Lokras, A.
AU - Thamm, J.
AU - Saraf, M.
AU - Warawdekar, U.
AU - Fahr, A.
AU - Nagarsenker, M.
PY - 2020
Y1 - 2020
N2 - Aim: To investigate comparative in vitro and in vivo performance of lipid vesicular and particulate systems in escalating oral bioavailability for superior hepatoprotection. Materials and methods: 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. Results: 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. Conclusion: 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.
AB - Aim: To investigate comparative in vitro and in vivo performance of lipid vesicular and particulate systems in escalating oral bioavailability for superior hepatoprotection. Materials and methods: 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. Results: 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. Conclusion: 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.
KW - GeluPearl
KW - Hepatoprotection
KW - LeciPlex
KW - Lipid nanosystems
KW - Liver
KW - Oral bioavailability
KW - Silibinin
U2 - 10.1016/j.ijpharm.2020.119176
DO - 10.1016/j.ijpharm.2020.119176
M3 - Journal article
C2 - 32119898
AN - SCOPUS:85080985550
VL - 579
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
M1 - 119176
ER -
ID: 238013530