Abstract
It is still controversial whether poor aqueous solubility is the most primary reason for the low oral bioavailability of insoluble drugs. Therefore, in this study, berberine-loaded solid polymeric particles (BPs) of varied dissolution profiles with β-cyclodextrin (β-CD) as carrier were fabricated using solution-enhanced dispersion by supercritical fluids (SEDS), and the relationship between dissolution and berberine (BBR) bioavailability was evaluated. Dissolution property was controlled via particle morphology manipulation, which was achieved by adjusting several key operating parameters during the SEDS process. Characterization on BP using infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction indicated that BBR was dispersed in amorphous form, while nuclear magnetic resonance spectroscopy showed that methoxy groups of BBR were included into the cavities of β-CD. In vivo pharmacokinetic studies showed that oral bioavailability increased by about 54% and 86% when the dissolution rate of BBR was increased by 51% and 83%, respectively. The entry speed of BBR into the bloodstream was also advanced with the degree of dissolution enhancement. It seemed that dissolution enhancement gave positive effect to the oral bioavailability of berberine, but this might not be the crucial point. Meanwhile, supercritical CO2 technology is a promising method for pharmaceutical research due to its advantages in regulating drug-dosage properties.
Highlights
Berberine (BBR), a representative quaternary protoberberine isoquinoline alkaloid generally existing in the form of hydrochloride, is one of the most important natural medicines that can be extracted from plants like Coptis sp. or Berberis sp. [1]
Both shapes can be observed in the physical mixture of BBR and β-CD (Figure 1c), as well as in inclusion complexes of BBR (ICB) (Figure 1d)
berberine-loaded solid polymeric particles (BPs) were prepared using supercritical fluids (SEDS), and the dissolution property of BBR was controlled by manipulating the particle morphology
Summary
Berberine (BBR), a representative quaternary protoberberine isoquinoline alkaloid generally existing in the form of hydrochloride, is one of the most important natural medicines that can be extracted from plants like Coptis sp. or Berberis sp. [1]. BBR was early considered in clinics as an effective and safety agent widely used for the treatment of diarrhea and gastroenteritis [2], due to its pharmacological antibacterial [3], anti-inflammatory [4,5] and antiparasitic [6] properties. 1%) seriously limits the clinical utilization of these pharmacological qualities, and poor adsorption in the intestine is generally considered the main affecting factor, except for the first-pass effect in the liver [13]. The poor absorption of BBR may be attributed to the drug’s physicochemical properties, including self-aggregation, poor permeability, low dissolution, and physiological factors like P-glycoprotein-mediated efflux [13].
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