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Characterization and Bioavailability Study of Baicalin-mesoporous Carbon Nanopowder Solid Dispersion.

Li Cui1, E Sune1, Jie Song1

  • 1Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu, P.R. China; Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Province Academy of Chinese Medicine, Nanjing, Jiangsu, P.R. China.

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|November 22, 2016
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Summary

Mesoporous carbon nanopowder (MCN) significantly enhances baicalin (BA) dissolution and oral bioavailability. This novel MCN-based solid dispersion (SD) system shows no intestinal or renal toxicity in rats.

Keywords:
Baicalindissolutionmesoporous carbon nanopowderoral bioavailabilitysolid dispersion

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Pharmacology

Background:

  • Baicalin (BA), a key compound from *Scutellaria baicalensis*, exhibits diverse biological activities.
  • Poor water solubility and low oral bioavailability limit baicalin's therapeutic efficacy.
  • Developing effective drug delivery systems is crucial for improving baicalin's performance.

Purpose of the Study:

  • To enhance the dissolution and oral bioavailability of baicalin (BA).
  • To utilize a novel mesoporous carbon nanopowder (MCN) as a drug carrier for baicalin.
  • To evaluate the safety and efficacy of the MCN-based drug delivery system.

Main Methods:

  • Solid dispersions (SDs) of baicalin (BA) and mesoporous carbon nanopowder (MCN) were prepared using solvent evaporation.
  • Formulation characterization involved SEM, DSC, and XRD analyses.
  • In-vitro dissolution, pharmacokinetic studies in rats, and toxicity assessments were performed.

Main Results:

  • The BA dissolution rate from MCN-based SDs (1:6 BA/MCN ratio) was significantly increased compared to pure BA.
  • Oral administration of MCN-BA SDs resulted in a 1.83-fold increase in the area under the concentration-time curve (AUC) in rats.
  • The MCN-BA system led to a higher Cmax and a shorter Tmax compared to pure BA, with no observed intestinal or renal toxicity of MCN.

Conclusions:

  • Mesoporous carbon nanopowder (MCN) effectively enhances the oral bioavailability of baicalin (BA).
  • MCN-based solid dispersions (SDs) offer a promising strategy for improving the delivery of poorly soluble drugs.
  • The MCN carrier demonstrated safety, with no observed toxicity in the gastrointestinal tract.