DESIGN AND DEVELOPMENT OF OPTIMIZED BERBERINE CHLORIDE FORMULATION FOR TREATMENT OF DIABETES

Main Article Content

Ms Priya Sharma
Dr Amarjeet Singh
Dr Navjot Singh Sethi

Keywords

Berberine HCl, Diabetes Mellitus, Permeation enhancer, Quality by design, Phospholipid complex

Abstract

Aim: To design and development of optimized berberine chloride formulation by using the phospholipid complexation and permeation enhancer for the treatment of diabetes.


Material and methods: The phospholipid complex was prepared by solvent evaporation method using the soya lecithin, Phospholipid 90G and lipoid S 100. The prepared phospholipid complex was evaluated for the physical appearance, FTIR, percentage of drug complexing efficiency, total drug content and percentage drug loading and in-vitro permeation study. The berberine loaded phospholipid complex using phenyl piperazine and methyl piperazine were used as permeation enhancer. The formulated complex was evaluated physical appearance, pH, FTIR, drug content, permeability study, In-vitro permeation study, stability study and In-vivo pharmacokinetic study.


Results: The preformulation study of Berberine HCl involved investigating various parameters such as organoleptic properties, melting point, partition coefficient, solubility, and absorption maxima. Berberine HCl exhibited a yellow color with a bitter taste, a melting point, partition coefficient. Solubility testing revealed its sparing solubility in methanol and slight solubility in ethanol, water, and phosphate buffer pH 6.8. FTIR analysis confirmed the presence of characteristic functional groups in Berberine HCl. Furthermore, the formation of a complex with phospholipids was indicated by shifts in characteristic peaks. Physical appearance assessments of the berberine HCl-phospholipid complex formulations showed a consistent yellow color. Percentage drug complexation ranged from 56.098% to 80.466%, with solubility in n-octanol and water varying across formulations. In vitro permeability studies demonstrated enhanced berberine HCl permeation from the complexed formulations, notably DBPC14. The stability study indicated no significant changes in physical appearance or drug content over three months. In-vivo pharmacokinetic analysis revealed improved bioavailability and absorption of berberine HCl from the phospholipid complex DBPC14 compared to the pure drug and a mixture with phenyl piperazine. These findings suggest the potential of berberine HCl-phospholipid complexes for enhanced therapeutic outcomes in the treatment of metabolic disorders such as diabetes mellitus.


Conclusion: From the present study, it can be concluded that the importance of optimization of formulation development using quality by design strategy to achieve phospholipid with consistent quality.

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