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

Abstract

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 AUC 0-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.

Development and optimization of curcumin analog nano-bilosomes using 21.31full factorial design for anti-tumor profiles improvement in human hepatocellular carcinoma:in-vitroevaluation,in-vivosafety assay

“…They can act as solubilizing and permeation-enhancing agent. Sodium cholate (SC) is one of the most commonly used bile salts due to its nontoxic nature and high permeation enhancing capacity and hence it was utilized to prepare PIP BLs (Zafar et al., 2021 ).…”

“…The prolonged PIP release from the investigated BLs vesicles might be due to the advantage of using BLs as colloidal particulate nanostructures. They act as drug reservoirs supplying a prolonged release of the entrapped active molecule (Mohsen et al., 2020 ; Zafar et al., 2021 ; 2021 ). Additionally, the use of cholesterol in preparing the vesicles can decrease the permeability or the liberation of the entrapped drug via reducing vesicle membrane fluidity (Mohsen et al., 2020 ).…”

Formulation, Optimization and Evaluation of Luteolin-Loaded Topical Nanoparticulate Delivery System for the Skin Cancer

“…The prepared luteolin nanovesicles (LT-NVs) were prepared by a solvent evaporationfilm hydration method. BBD optimization techniques give the maximum variables at different levels along with a lower number of experimental runs [41]. The formulations were optimized using phospholipid (A), edge activator (B) and sonication time (C) as independent variables.…”

Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity

“…Among them, bilosomes (BSs) are novel vesicular drug carriers containing bile salt [ 4 ]. The use of negatively charged bile salt (sodium-deoxycholate) enhances the stability of BS as well as permeation through the SC of the skin by the fluidizing effect [ 9 ]. Different bilosomes have been prepared and evaluated for in vitro and in vivo studies [ 10 , 11 , 12 ].…”