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

Abstract

Various perspectives had been utilized to enhance the poor intestinal permeability and bioavailability of drugs with low water solubility. Berberine (Brb) is a unique molecule that possesses multiple therapeutic activities such as antimicrobial, anti-inflammatory, antioxidant and anti-hyperglycemic effects. 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. The bioavailability of the selected formulations was assessed in vivo after oral administration to rats. The results revealed an enhanced effect of hyaluronic acid on the entrapment efficiency, reaching 78.1 ± 0.1% with mean size 520.7 ± 19.9 nm. Sustained release of Brb was recorded up to 24 h in comparison to Brb solution. Physical stability was maintained for three months at refrigeration temperature. 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.

RETRACTED: QbD-based rivastigmine tartrate-loaded solid lipid nanoparticles for enhanced intranasal delivery to the brain for Alzheimer's therapeutics

“…They should be carefully screened and optimized to get an obligatory product. It gives the least required number of experiments to get appropriate results by optimizing the critical factors and estimating the interactions and quadratic effects of the dependent factors on the properties of RT-SLNs (Kutbi et al, 2021 ).…”

Dietary Phytochemicals Targeting Nrf2 to Enhance the Radiosensitivity of Cancer

“…A promising approach to address low bioavailability and systemic toxicity is the application of drug-loaded nanodrug delivery systems, including microemulsions, nanoemulsions, emulsions, nanoparticles, liposomes, biopolymer microgels, dendrimers, and micelles [ 147 , 148 ]. Recently, several strategies have been developed to enhance the bioavailability of these phytochemicals, for instance, DADS-loaded solid lipid nanoparticles [ 147 ], cordycepin phycocyanin-based micelles [ 148 ], BBR hyaluronate liposomes [ 149 ], BRU-loaded self-microemulsions [ 142 ], EGCG-encapsulated nanoliposomes [ 150 ], AIF-loaded polymeric micelles [ 123 ], and ISL-loaded self-microemulsions [ 151 ]. These novel delivery systems could enhance the bioavailability and targeting characteristic and exhibits a superior pharmacokinetic profile.…”

Enhancing Dissolution and Oral Bioavailability of Ursodeoxycholic Acid with a Spray-Dried pH-Modified Extended Release Formulation

“…Lipid-based carriers with low BA therapeutic drugs could augment intestinal absorption by enhancing the M-cell-mediated uptake, transcellular, and paracellular pathway and by decreasing its efflux mechanism [ 25 , 37 , 38 ]. UDCA showed moderate absorptive permeability (2.5 × 10 −6 cm/s at pH 5.4 and 3.6 × 10 −6 cm/s at pH 7.4) and 4.1-fold higher absorptive permeability than secretory permeability ( Figure 2 ).…”