Pharmacokinetics of ligustrazine ethosome patch in rats and anti-myocardial ischemia and anti-ischemic reperfusion injury effect

Liu, Xingyan; Liu, Hong; Zeng, Zhigang; Zhou, Weihua; Liu, Jianqiang; He, Zhiwei

doi:10.2147/ijn.s20263

Cited by 37 publications

(19 citation statements)

References 6 publications

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“…[97][98][99] The preparation and evaluation of ethosomal patches are more complicated than for ethosomal gels, as molds are required for their preparation. Based on a literature search, only seven research articles had reported ethosomal patch formulations for several drugs, ie, testosterone, 6 artesunate and febrifugine, 27 ligustrazine, 34,118 valsartan, 37 tizanidine hydrochloride, 119 and insulin. 120 Different polymers were used to prepare the ethosomal patches, including polyvinylpyrrolidone/vinyl acetate, acrylic resin, and hydroxypropyl methylcellulose E15.…”

Section: Ethosomal Gelsmentioning

confidence: 99%

Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties, in vivo studies, and clinical trials

Abdulbaqi

Darwis

Khan

et al. 2016

IJN

329

215

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Ethosomal systems are novel lipid vesicular carriers containing a relatively high percentage of ethanol. These nanocarriers are especially designed for the efficient delivery of therapeutic agents with different physicochemical properties into deep skin layers and across the skin. Ethosomes have undergone extensive research since they were invented in 1996; new compounds were added to their initial formula, which led to the production of new types of ethosomal systems. Different preparation techniques are used in the preparation of these novel carriers. For ease of application and stability, ethosomal dispersions are incorporated into gels, patches, and creams. Highly diverse in vivo models are used to evaluate their efficacy in dermal/transdermal delivery, in addition to clinical trials. This article provides a detailed review of the ethosomal systems and categorizes them on the basis of their constituents to classical ethosomes, binary ethosomes, and transethosomes. The differences among these systems are discussed from several perspectives, including the formulation, size, ζ-potential (zeta potential), entrapment efficiency, skin-permeation properties, and stability. This paper gives a detailed review on the effects of ethosomal system constituents, preparation methods, and their significant roles in determining the final properties of these nanocarriers. Furthermore, the novel pharmaceutical dosage forms of ethosomal gels, patches, and creams are highlighted. The article also provides detailed information regarding the in vivo studies and clinical trials conducted for the evaluation of these vesicular systems.

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Section: Ethosomal Gelsmentioning

confidence: 99%

Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties, in vivo studies, and clinical trials

Abdulbaqi

Darwis

Khan

et al. 2016

IJN

329

215

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“…Ligustrazine plays a role in expanding blood vessels, increasing both coronary and cerebral blood flow, preventing platelet aggregation, inhibiting thrombosis, and improving microcirculation [2] . It also decreases hematological indices of myocardial ischemia in rats and protects against acute myocardial ischemia and myocardial ischemia-reperfusion injury [3] . Through the study of TMP derivatives, we unexpectedly found that liguzinediol (which has been patented [4] ) has significant positive inotropic effects, which were stronger than those of TMP.…”

Section: Introductionmentioning

confidence: 98%

Liguzinediol improved the heart function and inhibited myocardial cell apoptosis in rats with heart failure

Song

Zhu

et al. 2014

Acta Pharmacol Sin

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Aim: Liguzinediol is a novel derivative of ligustrazine isolated from the traditional Chinese medicine Chuanxiong (Ligusticum wallichii Franch), and produces significant positive inotropic effect in isolated rat hearts. In this study we investigated the effects of liguzinediol on a rat model of heart failure. Methods: To induce heart failure, male SD rats were injected with doxorubicin (DOX, 2 mg/kg, ip) once a week for 4 weeks. Then the rats were administered with liguzinediol (5, 10, and 20 mg·kg -1 ·d -1 , po) for 2 weeks. Hemodynamic examination was conducted to evaluate heart function. Myocardial cell apoptosis was examined morphologically. The expression of related genes and proteins were analyzed using immunohistochemical staining and Western blot assays, respectively. Results: Oral administration of liguzinediol dose-dependently improved the heart function in DOX-treated rats. Electron microscopy revealed that liguzinediol (10 mg·kg -1 ·d -1 ) markedly attenuated DOX-induced injury of cardiomyocytes, and decreased the number of apoptotic bodies in cardiomyocytes. Furthermore, liguzinediol significantly decreased Bax protein level, and increased Bcl-2 protein level in cardiomyocytes of DOX-treated rats, led to an increase in the ratio of Bcl-2/Bax. Moreover, liguzinediol significantly decreased the expression of both cleaved caspase-3 and NF-κB in cardiomyocytes of DOX-treated rats. Administration of digitalis (0.0225 mg·kg -1 ·d -1 ) also markedly improved the heart function and the morphology of cardiomyocytes in DOX-treated rats. Conclusion: Liguzinediol improves the heart function and inhibits myocardial cell apoptosis in the rat model of heart failure, which is associated with regulating Bcl-2, Bax, caspase-3, and NF-κB expression.

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“…Meanwhile, we come to know that TMP also can inhibit the apoptosis of spinal cord injury cells (9) as well as can help in the production of endothelin, which can dilate vessels and increase the effect of blood supply in the ischemic area (10). It can inhibit the aggregation of platelet thus, reducing blood viscosity simultaneously improve microcirculation and regulate the expression of interleukin in order to inhibit inflammation (11). Angiogenesis might be a condition for the growth of primary and metastatic tumors.…”

Section: Introductionmentioning

confidence: 99%

β-elemene enhances anticancer and anti-metastatic effects of osteosarcoma of ligustrazine inï¿½vitro and inï¿½vivo

et al. 2018

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Abstract. The present study aimed to determine the anticancer effects of the combination of β-elemene and ligustrazine in vitro as well as in in vivo. Following evaluation using an MTT assay, β-elemene, ligustrazine and the β-elemene-ligustrazine combination treatments all exhibited the capacity to inhibit the growth of OS-732 cells, with inhibitory rates of 43.3, 54.4, and 75.0%, respectively. Using a flow cytometry assay, it was determined that the β-elemene-ligustrazine combination possessed the highest apoptotic rate (30.6%). Furthermore, β-elemene-ligustrazine combination treatment resulted in the highest downregulation of G protein-coupled receptor 124, vascular endothelial growth factor, matrix metallopeptidase (MMP)-2 and MMP-9 mRNA, and protein expression levels. In addition, the combined treatment led to an increase in the mRNA and protein expression of endostatin, TIMP metallopeptidase inhibitor (TIMP)-1 and TIMP-2 in OS-732 cells. Additionally, β-elemene-ligustrazine caused a decrease in nuclear factor-κB, interleukin-8, C-X-C motif chemokine receptor 4 and urokinase-type plasminogen activator mRNA expression, as well as an increase in caspase-3, caspase-8, and caspase-9 mRNA expression. In vivo, the β-elemene-ligustrazine combination was able to reduce the weight and the bulk of the tumor in BALB/c-nu/nu nude mice compared with any other group. All the results described above regarding changes to mRNA and protein expression were further confirmed in vivo in the tumor tissue of mice. The results of the present study have suggested that the combination of β-elemene-ligustrazine exhibits greater anticancer effects compared with β-elemeneor ligustrazine-alone treatment.

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Pharmacokinetics of ligustrazine ethosome patch in rats and anti-myocardial ischemia and anti-ischemic reperfusion injury effect

Cited by 37 publications

References 6 publications

Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties, in vivo studies, and clinical trials

Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties, in vivo studies, and clinical trials

Liguzinediol improved the heart function and inhibited myocardial cell apoptosis in rats with heart failure

β-elemene enhances anticancer and anti-metastatic effects of osteosarcoma of ligustrazine inï¿½vitro and inï¿½vivo

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