Berberine nanoparticles with enhanced in vitro bioavailability: characterization and antimicrobial activity

Abstract

BackgroundBerberine is an isoquinoline alkaloid widely used in Ayurveda and traditional Chinese medicine to treat illnesses such as hypertension and inflammatory conditions, and as an anticancer and hepato-protective agent. Berberine has low oral bioavailability due to poor aqueous solubility and insufficient dissolution rate, which can reduce the efficacy of drugs taken orally. In this study, evaporative precipitation of nanosuspension (EPN) and anti-solvent precipitation with a syringe pump (APSP) were used to address the problems of solubility, dissolution rate and bioavailability of berberine.MethodsSemi-crystalline nanoparticles (NPs) of 90–110 nm diameter for APSP and 65–75 nm diameter for EPN were prepared and then characterized using differential scanning calorimetry (DSC) and X-ray powder diffractometry (XRD). Thereafter, drug content solubility and dissolution studies were undertaken. Berberine and its NPs were evaluated for their antibacterial activity.ResultsThe results indicate that the NPs have significantly increased solubility and dissolution rate due to conversion of the crystalline structure to a semi-crystalline form.ConclusionBerberine NPs produced by both APSP and EPN methods have shown promising activities against Gram-positive and Gram-negative bacteria, and yeasts, with NPs prepared through the EPN method showing superior results compared to those made with the APSP method and the unprocessed drug.

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Berberine nanoparticles for promising sonodynamic therapy of a HeLa xenograft tumour

“…However, it has been reported that BBR can have regular nanostructures, known as BBR nanoparticles (BBRNPs), by triggering its self-assembly in neutral buffer. 19 Sahibzada's group rst reported that BBRNPs can be generated via both syringe pumping anti-solvent precipitation (APSP) and evaporative precipitation of nanosuspension (EPN). 20 Here we introduced an easier way to prepare BBRNPs.…”

“…19 Sahibzada's group rst reported that BBRNPs can be generated via both syringe pumping anti-solvent precipitation (APSP) and evaporative precipitation of nanosuspension (EPN). 20 Here we introduced an easier way to prepare BBRNPs. In order to prepare different concentrations of BBRNP stock solution, for instance 2 mL 100 mg mL À1 BBRNP stock, 200 mg of BBR was weighed and mixed with 2 mL of neutral PBS buffer; the resulting turbid liquid was sonicated in a 55 C water bath for 2-5 min until a transparent yellowish solution was generated.…”