Page 152 - 2025中醫藥與天然藥物聯合學術研討會-中醫藥與天然藥物的挑戰Ｘ機遇與未來大會手冊

PC-34

Preparation, physicochemical properties and water solubility improvement

of baicalin nanoparticles

,1
#,1
2
Sung-Yu MA, Y u -Ting Tsai, Feng-Lin Yen, Tzu-Hui Wu*
1

1 Department of Pharmacy and Master Program, College of Pharmacy and Health, Tajen
University, Pingtung, Taiwan
2 Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical
University, Kaohsiung, Taiwan
* E-mail: u93070@tajen.edu.tw

Abstract
Scutellaria baicalensis is a widely used traditional Chinese medicinal herb, and its active
constituent baicalin, a flavone glycoside extracted from S. baicalensis, exhibits potent
antioxidant properties along with diverse pharmacological activities. However, its poor water
solubility and limited permeability result in poor dissolution and low oral bioavailability. The
aim of this study was to develop a rapidly dissolving baicalin nanoparticles delivery system by
the solid dispersion method. In this study, baicalin, hydroxypropyl-β-cyclodextrin (HPBCD),
and polyvinylpyrrolidone K30 (PVP-K30) were combined at different ratios using the solid
dispersion method in ethanol. By adjusting the proportion of HPBCD and PVP-K30, which
served as carriers in the nanoformulation process, the optimal composition for enhancing water
solubility was determined. The baicalin nanoparticles (BANP) were subsequently evaluated for
water solubility, yield, dissolution rate, and encapsulation efficiency using high-performance
liquid chromatography (HPLC). Furthermore, the physicochemical properties of BANP were
characterized through particle size analysis, disintegration rate, transmission electron
microscopy (TEM), scanning electron microscopy (SEM), and Fourier transform infrared
spectroscopy (FT-IR). The present results demonstrated that a 1:5:8 ratio of baicalin, HPBCD,
and PVP-K30 led to an approximately 23-fold reduction in particle size, and showed a
pronounced flake-like morphology under SEM. Furthermore, HPLC analysis revealed an
approximately 360-fold enhancement in water solubility, indicating that this ratio represents an
optimal formulation when controlling excipient dosage. In summary, we believe that baicalin
nanoparticles can increase water solubility, which will be beneficial to the further development
of health products and medicines.

Keywords: Baicalin; Hydroxypropyl-β-cyclodextrin; Polyvinylpyrrolidone K30; Nanoparticle