Triptolide (TP) has been shown to have anti-inflammatory, antifertility, antineoplastic, and immunosuppressive activity. However, its clinical usage is limited to some extent due to its poor water solubility and toxicity. In order to use innovative ways to administer TP and to overcome or alleviate its disadvantages, controlled-release delivery systems such as solid lipid nanoparticle(SLN(s)) have been developed. In the present paper we describe the preparation and some characterization of specialized delivery systems for TP. The transdermal delivery and anti-inflammatory activity were also evaluated. The results indicated that SLN could serve as an efficient promoter of TP penetrating into skin. Furthermore, different formulations were optimized in this study. The best formulation of SLN, consisted of tristearin glyceride, soybean lecithin, and PEG400MS, with a particle size of 123+/-0.9 nm, polydispersity index (PI) of 0.19, and zeta potential of -45 mV. When this SLN dispersion was incorporated into hydrogel, the nanoparticulate structure was maintained, and aggregation and gel phenomena of the particle could be avoided. The cumulative transdermal absorption rate in 12 h was 73.5%, whereas the conventional TP hydrogel was 45.3%. The anti-inflammatory effect is over two-fold higher than that of conventional TP hydrogel. Moreover, this SLN hydrogel consists of pharmaceutically acceptable ingredients, such as soybean lecithin and lipid, and the nanoparticle can improve safety and minimize the toxicity induced by TP.
Aim: To investigate the antihepatocellular carcinoma effects of Chi-Shen extract (CSE) from the water-soluble compounds of Salvia miltiorrhiza and Paeoniae radix. Methods: The effect of CSE on the growth of HepG2 cells (hepatocellular carcinoma cell line) was studied by 3-(4,5)-2,5-diphenyltetrazolium bromide assay. Apoptosis were detected through acridine orange (AO) and ethylene dibromide (EB) staining and DNA fragmentation assay. The effect of CSE on the cell cycle of HepG2 cells was studied by the propidium iodide staining method. The activation of caspases-3, -8 and -9 was examined by immunoassay kits. The transcription of the Bcl-2 family and p53 was detected by RT-PCR. Results: Our data revealed that CSE strongly induced HepG2 cell death in a dose-and time-dependent manner. CSE-induced cell death was considered to be apoptotic by observing the typical apoptotic morphological change by AO/EB staining and DNA fragmentation assay. The induction of HepG2 cell death was caused by an induction of apoptosis for the sub-G 1 proportion increase, the downregulation of Bcl-2, the upregulation of Bax and p53, and the activation of the caspases-3 and -9 pathways. Conclusion: These results clearly demonstrated that CSE was able to inhibit the proliferation of HepG2 cells and cause apoptosis. Moreover, the anticancer effects of CSE were related to the Bcl-2 family pathway and the activation of caspases-3 and -9 in HepG2 cells.
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