Berberine Chloride Phytosomes: Development and Evaluation of a Novel Phospholipid Based Delivery System

Background

Phytosomes are an advanced drug delivery system designed to improve the solubility, stability, and bioavailability of plant-based compounds.

Objectives

This study aimed to formulate and characterize berberine chloride-loaded phytosomes using soya lecithin.

Materials and Methods

Berberine chloride was isolated from the ethanolic extract of Berberis aristata roots and characterized by UV, FTIR, TLC, SEM, mass spectroscopy, and ¹H NMR. Phytosomes were prepared in two different ratios, 1:1.5 (Batch A) and 1:2 (Batch B), using the rotary evaporation method. Batch A (1:1.5) was selected based on compound microscopy and physical characters and subjected further to characterization techniques including SEM, FTIR, DSC, particle size analysis, zeta potential, entrapment efficiency, and drug loading.

Results

Compound microscopy of phytosomes showed uniform particle distribution and loss of crystallinity of berberine chloride. SEM confirmed spherical, aggregated phytosomal particles, while FTIR indicated drug-phospholipid interaction through peak shifts. DSC thermograms exhibited endothermic peaks at 214.19ºC, supporting successful complexation and thermal stability. Particle size and zeta potential were found to be 125.7 nm and -24.3 mV, suggesting nanoscale particles with good colloidal stability. Entrapment efficiency and drug loading were 65% and 103.93%, respectively.

Conclusion

The study concluded that berberine chloride phytosomes were successfully developed and characterized, despite lacking a hydroxyl group, complexation occurs through hydrophobic interaction and Van der Waals force with the methoxy group and electrostatic interactions between its quaternary nitrogen and the phospholipid’s phosphate group.