Liposomes for oral delivery of Berberine

Optimization of Hyaluronate-Based Liposomes to Augment the Oral Delivery and the Bioavailability of Berberine

To improve Brb permeability and bioavailability, this study presents a newly developed formulation, namely Brb hyaluronate-based liposomes, prepared by using film hydration method and characterized by dynamic light scattering measurements, entrapment efficiency percentage (EE%), transmission electron microscope (TEM), in vitro drug release and physical stability. Results of pharmacokinetics studies indicated the potential of the liposomal formulation to increase the oral bioavailability of Brb and to accelerate its entry into the bloodstream. The obtained results are accredited to the lipophilic nature of the prepared system, resembling the structural features of bio-membrane, in addition to their small size that enhances intestinal penetration. 

Transmission electron microscope of berberine hyaluronate based liposomes, showing the nearly spherical shape (A) and the multi-lamellar structure of the vesicles bilayer (B) of the prepared liposomes.
Three-dimensional (3D) response surface plots showing the effect of the independent variables on liposomes particle size and entrapment efficiency percent: A—total lipid amount (mg), B—berberine (mg), C—hyaluronic acid (mg).
Plasma concentration profiles of berberine in rats after oral administrations of 50 mg/kg of berberine in various formulations. Each point represents mean ± standard deviation (N = 6).

Different formulation variables (lipid, drug and hyaluronic acid amounts) have a significant effect on the physicochemical characteristics of the prepared system using film hydration method. The presence of hyaluronic acid as a main component in liposomes preparation was able to slow berberine diffusion from the vesicles.Oral administration of Brb hyaluronate-based liposomes to rats could improve lipophilicity and bioavailability of the investigated system compared to Brb solution and Brb liposomes prepared without hyaluronic acid.

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