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1、Supported by Science and Technology Project of Xian City (GG04133).LI Ying-chao (1974-), PhD, attending physician, specialized in pharmaceutical research of liver fibrosis, Tel: 029-85324001, E-mail: l_y_Corresponding author:DONG Lei, medical professor, Tel: 029-87276936- 29368, E-mail: Preparation
2、of solid lipid nanoparticles loaded with traditional Chinese medicine by high-pressure homogenizationLI Ying-chao1, DONG Lei2, JIA Ai1, CHANG Xin-ming1, XUE Hui1 1Department of Gastroenterology, First Affiliated Hospital, Medical College of Xian Jiaotong University, Xian 710061, China; 2Department o
3、f Gastroenterology, Second Affiliated Hospital, Medical College of Xian Jiaotong University, Xian 710004, China Abstract:Objective To investigate the preparation of solid lipid nanoparticles (SLN) loaded with traditional Chinese medicines by high-pressure homogenization, and study the physicochemica
4、l characteristics of the particles produced by this method. Methods The model traditional Chinese medicines, silibinin (SIL) and tetrandrine (TET), were incorporated into SLN separately by high-pressure homogenization. Transmission electron microscope was employed to study the shape of the particles
5、. Particle characterization system and zeta potential analyzer were used to study the diameter and zeta potential of SLN in the suspension. The entrapment efficiency and drug loading were determined with the sephadex gel chromatography and high-performance liguid chromatography. The stability of SLN
6、 was also studied. Results The SIL-SLNs prepared by high-pressure homogenization were spherical and regular. The mean diameter and zeta potential of SIL-SLN in distilled water were 157!8 nm and -35.36!2.68 mV, respectively. The entrapment efficiency was 95.64%, and the drug loading was 4.63%. The TE
7、T-SLN was platelet-shaped, irregular and smaller. The mean diameter and zeta potential of TET-SLN were 47!3 nm and -32.99!2.54 mV, respectively, with drug loading of 4.76%, and up to 97.82% of TET was incorporated. SIL-SLN and TET-SLN had good stability. Conclusion High-pressure homogenization is fe
8、asible for preparing SLN loaded with traditional Chinese medicines. Key words: silibinin; tetrandrine; solid lipid nanoparticles; high-pressure homogeni zation; traditional Chinese medicinesSolid lipid nanoparticles (SLNs) are particles made from solid lipids with a mean diameter of approximately 50
9、 to 1000 nm to serve as an alternative colloidal carrier system for controlled drug delivery!1“. Compared with other particulate carriers SLN has several advantages for drug delivery such as its good biocompatibility!2“, biodegradability!3“, high bioavailability!4“, and effects targeting the liver a
10、nd spleen. In recent years, markedly increasing studies on SLN have been reported, especially with the method of high-pressure homogenization!5“. Nevertheless, only a few investigations have been conducted in regard with the incorporation of effective components of traditional Chinese medicines into
11、 SLN.Silymarin is a purified extract from the milk thistle Silybum marianum (L.) Gaertn, which is composed of a mixture of 4 isomeric flavonolignans, namely silibinin (or silybin, SIL), isosilibinin, silidianin and silychristin. SIL, which constitutes 60%-70% of the silymarin mixture, has been ident
12、ified as the major active component!6“. Tetrandrine (TET) is a bisbenzylisoguinoline alkaloid extracted from the traditional Chinese medicinal herb Radix stephania tetrandrae. SIL and TET possess wide spectrums of pharmacological activities!7-11“. These two effective components of the traditional Ch
13、inese medicines have high lipophilicity and are excellent candidates for SLN encapsulation. By using this drug delivery system, a high bioavailability and an intravenous administration are possible. In the present study, SIL-SLN and TET- SLN were prepared by high-pressure homogenization, and the phy
14、sicochemical characteristics of the particles produced by this method were analyzed.MATERIALS AND METHODS Drugs and reagentsSIL (95%) was purchased from Panjin Green Biological Development Co. Ltd., China. TET (98%) was purchased from Shanchuan Biological Co. Ltd., Xian. Cholesterin (obtained from Z
15、hengxiang Chemical Research Institute, Shanghai) and stearic acid (Tianda Chemical Industry Ltd., Tianjin) were used separately as the lipid materials of SLN. Soybean lecithin was obtained from Auboxing Co. Ltd., Beijing. Sephadex gel-50 was purchased from Tianjin Chemical Industry Ltd. Methanol (HP
16、LC grade) and absolute alcohol was supplied by Xian Chemical Industry Ltd. Glycerin 2006;26(5) 南方医科大学学报(J South Med Univ)541#(Amoy Glycerin Industry Ltd.) was used as a coemulsifier in water phase.Preparation of SIL-SLN SIL (75 mg), cholesterin (1.5 g) and soybean lecithin (1.0 g) were weighed precisely with electronic b
