Pharmacokinetic and pharmacodynamic study of triptolide-loaded liposome hydrogel patch under microneedles on rats with collagen-induced arthritis

Triptolide (TP), a major active component of Tripterygium wilfordii Hook.F. (TWHF), is used to treat rheumatoid arthritis (RA). However, it has a narrow therapeutic window due to its serious toxicities. To increase the therapeutic index, a new triptolide-loaded transdermal delivery system, named triptolide-loaded liposome hydrogel patch (TP-LHP), has been developed. In this paper, we used a micro-needle array to deliver TP-LHP to promote transdermal absorption and evaluated this treatment on the pharmacokinetics and pharmacodynamics of TP-LHP in a rat model of collagen-induced arthritis (CIA). The pharmacokinetic results showed that transdermal delivery of microneedle TP-LHP yielded plasma drug levels which fit a one-compartment open model. The relationship equation between plasma concentration and time was C=303.59×(e(-0.064t) -e(-0.287t) ). The results of pharmacodynamic study demonstrated that TP-LHP treatment mitigated the degree of joint swelling and suppressed the expressions of fetal liver kinase-1, fetal liver tyrosine kinase-4 and hypoxia-inducible factor-1α in synovium. Other indicators were also reduced by TP-LHP, including hyperfunction of immune, interleukin-1β and interleukin-6 levels in serum. The therapeutic mechanism of TP-LHP might be regulation of the balance between Th1 and Th2, as well as inhibition of the expression and biological effects of vascular endothelial growth factor.

Effects of guizhi tang on inflammatory cytokines in myocardial ischemia and hyperlipidemia rats / 中国中药杂志

<p><b>OBJECTIVE</b>To explore the effects of Guizhi Tang on the inflammatory cytokines in myocardial ischemia and hyperlipidemia rats.</p><p><b>METHOD</b>The early changes of hyperlipid and atherosclerosis are caused by utilizing multiple factors including feeding hyperlipid and propylthiouracil and high doses of vitamin D3 for 12 weeks. Sixty male SD rats were randomly divided in to 5 groups: control group, model group, simvastatin group, low-dosage Guizhi Tang group, high-dosage Guizhi Tang group. At the end of six weeks treatment, pituitrin(pit) is abdominal cavity injected every 24 hours for a total of three times. Detecting the serum levels of SES, CRP, NO, SOD, MDA and the content of cardiac muscle tissue SOD, MDA, The expression of TNF-alpha in cardiac muscle tissue was detected by immunohistochemistry.</p><p><b>RESULT</b>Guizhi Tang significantly decreased levels of SES, CRP and MAD, increased levels of NO and SOD, Guizhi Tang markedly decreased the level of protein expression of TNF-alpha in cardiac muscle tissue.</p><p><b>CONCLUSION</b>Guizhi Tang may inhibit the proinflammatory factors and oxidation in myocardial ischemia and hyperlipidemia rats.</p>

Transdermal delivery of Gentiana macrophylla complex components system under micro-needle conditions / 药学学报

The purpose of this study is to investigate the transdermal delivery characteristics of Gentiana macrophylla complex components system through different parts of the skin under micro-needles conditions. Two-chamber diffusion cells were used, different parts of isolated skin and micro-needle pretreated isolated mouse skin were applied separately, high performance liquid chromatography (HPLC) similarity evaluation methods were used to evaluate transdermal delivery characteristics of Gentiana macrophylla complex components system on receiving pool and the permeation rate and penetration amount of Gentiopicroside at different parts of mouse skin. In the 24 h, the similarity between receiving fluid which was on passive transdermal delivery and micro-needle transdermal delivery conditions and original fluid were ranged from 83.0% to 98.9%; By the micro-needle pretreatment with different parts of the mouse skin, the time that Gentiana macrophylla complex components system though abdominal skin to the receiving fluid which reached 90% similarity compared with that of original fluid was 4 h, which was 18 h at back skin and 12 h at neck skin separately. Micro-needles can be used as the ideal ingredients for traditional Chinese medicine complex transdermal delivery; transdermal absorption time delay could be greatly reduced and its bioavailability was improved. The permeation rate and similarity to original liquid of Chinese medicine complex components increased significantly in the abdominal skin relative to the neck and back skin under micro-needle conditions.

Establishment of a rat model of rheumatoid arthritis with kidney deficiency syndrome / 中西医结合学报

To establish a rat model of rheumatoid arthritis (RA) with kidney deficiency syndrome.

Immunoregulatory function of Radix Glycyrrhizae polysaccharide in tumor-bearing mice / 中西医结合学报

Objective: To observe the effects of Radix Glycyrrhizae polysaccharide on regulatory T cells (Treg) in spleen and lymphocyte transformation ratio in tumor-bearing mice so as to explore the mechanisms of its immunoregulatory function. Methods: Fifty BALB/c mice were randomly divided into normal group, untreated group, cyclophosphamide group, Radix Glycyrrhizae polysaccharide group and Radix Glycyrrhizae polysaccharide plus cyclophosphamide group. Except normal group, mice were subcutaneously implanted H22 tumor cells in the right axillary region. After 24 h, mice in normal and untreated group were subcutaneously injected with physiological saline, while mice in the cyclophosphamide group were intraperitoneally injected with cyclophosphamide and mice in Radix Glycyrrhizae polysaccharide group were subcutaneously injected with polysaccharide. Fourteen days later, Treg cells of spleen were detected by flow cytometry and lymphocyte transformation ratio was detected by methyl thiazolyl tetrazolium method. Results: The proportion of Treg cells was significantly higher in the untreated group than in the normal group, and was lower in the Radix Glycyrrhizae polysaccharide group than in the untreated group (P