Abstract:
OBJECTIVE To prepare the berberine hydrochloride-loaded niosomes with cholesterol or
β-sitosterol separately, and compare their particle size, characteristics under the optical microscope, encapsulating rate, release profile
in vitro and the stability of two kinds of niosomes.
METHODS Thin-film evaporation method was applied to prepare the niosomes. Optical microscope was used to observe the morphology of the niosomes, and the particle diameter was observed and computed by Motic Images Advanced 3.2 system. HPLC was used to determine the encapsulating rate and loading capacity of the niosomes. The releasing profiles
in vitro of the niosomes were observed and compared with each other, and the effect of temperature on the stability of the niosomes was invesgated.
RESULTS The two kinds of niosomes both showed good sphericity, their particle diameter appenred to be similar. The encapsulating rate of cholesterol and
β-sitosterol niosomes determined by HPLC was 28.5% and 25.21%, and the loading capacity of niosomes was 1.32% and 1.26%, respectively. The releasing study
in vitro showed that the cholesterol niosomes reached an accumulative releasing rate about 50% at 12 h, while the accumulative releasing rate of
β-sitosterol niosomes was higher than 70% in the artificial intestinal juice and in the artificial gastric juice. The encapsulating rate was not affected significantly by the temperature when the niosomes were storage under 8 h and the temperature was lower than 40℃. When the temperature was higher than 40℃, the encapsulating rate decreased significantly in both niosomes.
CONCLUSION The two kinds of niosomes prepared by thin-film evaporation method have a similar appearance and a high encapsulating rate. The stability is good when the temperature is lower than 40℃. Compared with the cholesterol niosomes, the rate and the amount of drug release from
β-sitosterol niosomes are better. The
β-sitosterol can be used to prepare berberine hydrochloride niosomes.