Chrysin nanocapsules with dual anti-glycemic and anti-hyperlipidemic effects: Chemometric optimization, physicochemical characterization and pharmacodynamic assessment.

Autor: El-Hussien D; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy and Drug Technology, Heliopolis University, Cairo, Egypt., El-Zaafarany GM; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Egypt., Nasr M; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Egypt. Electronic address: drmahanasr@pharma.asu.edu.eg., Sammour O; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Egypt.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2021 Jan 05; Vol. 592, pp. 120044. Date of Electronic Publication: 2020 Nov 04.
DOI: 10.1016/j.ijpharm.2020.120044
Abstrakt: Chrysin is a flavonoid with various biological and therapeutic properties. However, its poor oral bioavailability and solubility are challenging barriers against its therapeutic use, which can be circumvented via encapsulation in a suitable nanocarrier. Therefore, the aim of this work was to prepare polymeric chrysin nanocapsules based on polylactic-glycolic acid PLGA with improved oral therapeutic potential, by optimization of their physicochemical properties using response surface methodology. Diabetes was induced in an animal model using streptozotocin to assess the anti-hyperglycemic activity of the selected formulation, and hyperlipidemia was induced in another animal model using a high fat diet to assess its anti-hyperlipidemic activity. Results revealed that the selected chrysin nanocapsular formulation exhibited particle size of 176 ± 2.10 nm, polydispersity index of 0.22 ± 0.01, negative zeta potential, drug entrapment efficiency of 87.10% ± 6.71, a controlled release of chrysin over a period of 24 h, and a significant physical stability after storage for 3 months. Compared to chrysin suspension, the selected nanocapsular formulation exhibited marked anti-hyperglycemic effect for up to 24 h, as well as superior anti-hyperlipidemic potential for 28 days. These improvements in chrysin therapeutic action after its encapsulation into polymeric nanocapsules delineate it as a promising remedy for oral treatment of diabetes and hyperlipidemia.
(Copyright © 2020 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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