Preparation and Evaluation of Berberine-Excipient Complexes in Enhancing the Dissolution Rate of Berberine Incorporated into Pellet Formulations

Berberine is used in the treatment of metabolic syndrome and its low solubility and very poor oral bioavailability of berberine was one of the primary hurdles for its market approval. This study aimed to improve the solubility and bioavailability of berberine by preparing pellet formulations containing drug-excipient complex (obtained by solid dispersion). Berberine-excipient solid dispersion complexes were obtained with different ratios by the solvent evaporation method. The maximum saturation solubility test was performed as a key factor for choosing the optimal complex for the drug-excipient.

The properties of these complexes were investigated by FTIR, DSC, XRD and dissolution tests. The obtained pellets were evaluated and compared in terms of pelletization efficiency, particle size, mechanical strength, sphericity and drug release profile in simulated media of gastric and intestine. Solid-state analysis showed complex formation between the drug and excipients used in solid dispersion. The optimal berberine-phospholipid complex showed a 2-fold increase and the optimal berberine-gelucire and berberine-citric acid complexes showed more than a 3-fold increase in the solubility of berberine compared to pure berberine powder.

The evaluation of pellets from each of the optimal complexes showed that the rate and amount of drug released from all pellet formulations in the simulated gastric medium were significantly lower than in the intestine medium. The results of this study showed that the use of berberine-citric acid or berberine-gelucire complex could be considered a promising technique to increase the saturation solubility and improve the release characteristics of berberine from the pellet formulation.

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Materials

Berberine hydrochloride was purchased from Shanghai Yuanye Biological Technology Co., Ltd. (Shanghai, China); microcrystalline cellulose (Avicel PH 101), polyvinylpyrrolidone (PVP K30) and lactose were purchased from Darupakhsh (Tehran, Iran). Phospholipon® 90 G was purchased from Lipoid GmbH (Ludwigshafen, Germany). Gelucire (Gattefossé, Saint-Priest, Cedex, France), citric acid (Sigma-Aldrich, Steinheim, Germany), ) potassium dihydrogen phosphate, sodium hydroxide, ethanol, hydrochloric acid and Aerosil Merck (Germany were used.  All chemical reagents used were of pharmaceutical grade.

Abbaspour, M., Faeznia, F., Zanjanian, P. et al. Preparation and Evaluation of Berberine-Excipient Complexes in Enhancing the Dissolution Rate of Berberine Incorporated into Pellet Formulations. AAPS PharmSciTech 25, 154 (2024). https://doi.org/10.1208/s12249-024-02863-1

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