Bioactive Luteolin Entrapped Chitosan-PLGA Nanoparticles: Formulation Optimization to In-Vivo Preclinical Evaluation.

Autor: Zafar, Ameeduzzafar, Alruwaili, Nabil K., Imam, Syed Sarim, Alsaidan, Omar Awad, Alharbi, Khalid Saad, Alzarea, Sami I., Yasir, Mohd, Afzal, Muhammad, Alshehri, Sultan, Alanazi, Abdullah S.
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Zdroj: Journal of Cluster Science; Jan2023, Vol. 34 Issue 1, p437-449, 13p
Abstrakt: Diabetes mellitus is an incurable metabolic disease characterized by a change in blood glucose level. Luteolin (LT) is a bioactive flavonoid and reported for potential antidiabetic activity. LT loaded chitosan (CH)—polylactic co-glycolic acid (PLGA) nanoparticles (NPs) were prepared by emulsification—evaporation process and further optimized by Box-Behnken design using CH (A), PLGA (B), and polyvinyl alcohol (C) as formulation variables and their effect evaluated on particle size (Y1), drug loading (Y2), and entrapment efficiency (Y3). CH-PLGA-LT-NPs showed a particle size of 273.43 ± 5.24 nm, DL of 15.25 ± 2.43%, and EE of 65.28 ± 1.76%. The zeta potential was found to be positive with spherical surface morphology. CH-PLGA-LT-NPs exhibited sustained drug release (68.23 ± 6.17%) than LT-dispersion (29.66 ± 4.2%). The permeation study and pharmacokinetic study results revealed 3.19 fold as well as 2.63 fold (AUC0-t) enhancement in pure LT. CH-PLGA-LT-NPs also exhibited a significant (P < 0.05) reduction in blood glucose level in streptozotocin-induced diabetic rats than LT-dispersion. CH-PLGA-LT-NPs also showed notable improvement in biochemical parameters as compared to diabetic control and LT-dispersion group. The results concluded that LT-CH-PLGA-NPs is a good alternative to the treatment of diabetes. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index