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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.
ABSTRACT
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.
ABSTRACT
<p><b>OBJECTIVE</b>To prepare flexible nanoliposomes of Ginkgolid B (GB) and study the transdermal diffusion law.</p><p><b>METHOD</b>Flexible nanoliposomes of GB were prepared by film dispersion method, and the shape and particle size of nanoliposomes were analyzed. GB permeation tests in vitro through the skin of rats were performed in modified Franz diffusion cell. The accumulated permeation amounts of GB alcoholic solution, flexible nanoliposomes of GB and ordinary nanoliposomes of GB were compared.</p><p><b>RESULT</b>The average encapsulation percentage, the particle size, and the Zata potential of the flexible nanoliposomes were (89.52 +/- 1.76)%, and was (208.3 +/- 25.49) nm, and was -49.2 mV, respectively. The accumulated permeation amount of flexible nanoliposomes in 8 hours was 189.97 microg x cm(-2), and its transdermal permeability in 8 hours was 23.75 microg x cm(-2) x h(-1).</p><p><b>CONCLUSION</b>The encapsulation percentage of the flexible nanoliposomes is good,and the stability of the GB nanoliposomes is fine. Flexible nanoliposomes can significantly enhance the diffusion rate of GB through the skin of rats.</p>
Subject(s)
Animals , Female , Male , Mice , Ginkgolides , Chemistry , Pharmacokinetics , Lactones , Chemistry , Pharmacokinetics , Liposomes , Chemistry , Pharmacokinetics , Nanoparticles , Chemistry , Particle Size , Permeability , Random Allocation , Skin AbsorptionABSTRACT
According to the analysis of PreQin society and history, it is concluded that influenced by special historical conception and low productivity of that time, ancient doctors were able to know the concept “Brain controls consciousness”. The structure of the Five-Zang Theory of TCM was constructed according to the concept of Five-Element Theory and the similarities between nature and human. So they had to enact “Heart controls consciousness” to complete the function of brain with heart instead. Most details of five-zang theory come from long-term medical practices and daily life, so the structure can guide the medical practices correctly. The concept “Heart controls consciousness” was brought about by many factors. After Qin and Han Dynasties, gradually, people used to keep this routinism. Similar to other historical events, formation of these concepts proposed by ancient physicians and philosophers is inevitable. We should analyze these problems formed in history objectively and completely, but not praise or criticize them blindly.
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Objective Using the effect of microneedle array to investigate the feature and rule of transdermal drug delivery of sinomenine hydrogel patch.Methods The microneedles with different length and sinomenine hydrogel patch were prepared;The isolated rat skin was pretreated by different needle-shapes of microneedle array and different timepoints with the same needle-shape,and then sticked the sinomenine patch.The permeation rates of sinomenine were studied using a Franz diffusion cell and compared with passive diffusion of the rat skin untreated.Sinomenine content was measured by HPLC.Results The permeation rates of sinomenine via the skin pretreated with 100 and 200 ?m microneedles were 40.7 and 52.4 times to those of the untreated.The permeation rates of sinomenine via the skin pretreated 7 min with 200 ?m microneedles is 142.0 times to those of the untreated.When skins were pretreated using 200 ?m microneedles with different force, the drug permeation rates were increased with the force increasing.When the force exceeded 5 N,the drug permeation rates were equilibrium.Conclusion When transdermal drug delivery by using microneedle array-hydrogel patch,the permeation rates increase significantly.The needle-shape,skin pretreating time,and force of the microneedles play the important roles in the transdermal drug delivery.
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Objective To study the effects on electroporation of Qingfengteng cataplasma transdermal absorption and describe the characteristics of animal pharmacokinetics of it.Methods Two-chamber diffusion cell was used and the plasma drug concentration was determined by HPLC.The application of AIC theory to analysis of the compartmentally based model of sinomenine transdermal delivery by electroporation.Results The Cmax,Ka,and AUC0→∞ of electroporation was larger than those of passive diffusion;t1/2(Ka)and tmax of electroporation were reduced compared with passive diffusion.The drug concentration-curve equation were C=2.884?(e-0.056 t-e-0.232 t)and C=2.512?(e-0.058 t-e-0.149 t)for electroporation and passive diffusion,respectively.Conclusion The change of in vivo drug concentration of Qingfengteng calaplasma transdermal absorption by electroporation could be analized in accordance with mammillary one-compartment open model.The etrectroporation technology could sharply enhance the bioavalibility compared with the passive diffusion.
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AIM: To prepare flexible nanoliposomes made from active ingredients,phillyrin and volatile oil,from forsythia suspense and study their transdermal delivery system.METHODS: Flexible nanolipsomes of phill-yrin(WN group) and phillyrin in combination with forsythia volatile oil(OWN group) were prepared by the meth-od of membrane-dispersion.Its appearance and particle sizes were measured.Transdermal experiments were carried out on the modified Franz diffusion pool through in vitro mouse skin.HPLC was applied to determining the phillyrin content to compare transdermal rate and cumulative permeation amount of various flexible nanoliposomes.RESULTS: The particle size of the WN group was(180.7 ? 13.69)nm,the Zata potential was-48.8 mV,the average encapsulation percentage was(82.53 ? 2.68)%;the particle size of the OWN group was(212.3 ? 15.31)nm,Zata potential was-51.2 mV,the average encapsulation percentage was(70.49 ? 1.06)%.The accu-mulated permeation amount of the OWN group in 8 hours was(291.92 ? 23.22) ?g/cm2,its transdermal permea-bility in 8 hours was 36.49 ?g/(cm2.h),which was 6.10 folds that of the WS group and 1.92 folds that of the WN group.This difference had statistical significance(P