Cover Image

Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment

Aim: Diabetic (type-2) is a metabolic disease characterized by increased blood glucose level from the normal level. In the present study, apigenin (AG) loaded lipid vesicles (bilosomes: BIL) was prepared, optimized and evaluated for the oral therapeutic efficacy. Experimental: AG-BIL was prepared by...

Full description

Saved in:
Bibliographic Details
Main Authors: Ameeduzzafar Zafar (Author), Nabil K. Alruwaili (Author), Syed Sarim Imam (Author), Nasser Hadal Alotaibi (Author), Khalid Saad Alharbi (Author), Muhammad Afzal (Author), Raisuddin Ali (Author), Sultan Alshehri (Author), Sami I. Alzarea (Author), Mohammed Elmowafy (Author), Nabil A. Alhakamy (Author), Mohamed F. Ibrahim (Author)
Format: Book
Published: Elsevier, 2021-03-01T00:00:00Z.
Subjects:
article
Online Access:Connect to this object online.
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Aim: Diabetic (type-2) is a metabolic disease characterized by increased blood glucose level from the normal level. In the present study, apigenin (AG) loaded lipid vesicles (bilosomes: BIL) was prepared, optimized and evaluated for the oral therapeutic efficacy. Experimental: AG-BIL was prepared by a thin-film evaporation method using cholesterol, span 60 and sodium deoxycholate. The prepared formulation was optimized by 3-factor and 3-level Box-Behnken design using particle size, entrapment efficiency and drug release as a response. The selected formulation further evaluated for ex-vivo permeation, in vivo pharmacokinetic and pharmacodynamics study. Results: The optimized AG bilosomes (AG-BILopt) has shown the vesicle size 183.25 ± 2.43 nm, entrapment efficiency 81.67 ± 4.87%. TEM image showed a spherical shape vesicle with sharp boundaries. The drug release study revealed a significant enhancement in AG release (79.45 ± 4.18%) from AG-BILopt as compared to free AG-dispersion (25.47 ± 3.64%). The permeation and pharmacokinetic studies result revealed 4.49 times higher flux and 4.67 folds higher AUC0-t than free AG-dispersion. The antidiabetic activity results showed significant (P < 0.05) enhancement in therapeutic efficacy than free AG-dispersion. The results also showed marked improvement in biochemical parameters. Conclusion: Our findings suggested, the prepared apigenin loaded bilosomes was found to be an efficient delivery in the therapeutic efficacy in diabetes.
Item Description:1319-0164
10.1016/j.jsps.2021.02.003

Similar Items