Multivesicular liposome formulation for the sustained delivery of breviscapine

Zhong, Hongshan; Deng, Yihui; Wang, Xiu Min; Yang, Binghua

doi:10.1016/j.ijpharm.2005.04.001

Cited by 63 publications

(22 citation statements)

References 23 publications

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“…Thus, research on E. breviscapus has become a hot topic in recent years. 17) New pharmacological actions of E. breviscapus have been studied and its neuroprotective actions, antibacterial, and antifungal activity have been reported. [18][19][20][21] However, its depigmenting effect has not yet been examined.…”

Section: )mentioning

confidence: 99%

Depigmentation of Melanocytes by (2Z,8Z)-Matricaria Acid Methyl Ester Isolated from Erigeron breviscapus

Luo

Kim

Nguyen

et al. 2009

Biological & Pharmaceutical Bulletin

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To discover an active skin depigmenting agent, we isolated a novel inhibitor of melanin biosynthesis from the methanol extract of Erigeron breviscapus using a bioactivity-guided fractionation and identified it as (2Z,8Z)-matricaria acid methyl ester by means of spectroscopic analysis. The compound showed strong whitening activity in melan-a cell. Compared with arbutin (IC 50 ‫0.4؍‬ mM) as a positive control, the depigmentation IC 50 value for (2Z,8Z)-matricaria acid methyl ester was 25.4 m mM in B16F10 melanoma cell. Moreover, its inhibitory effect on tyrosinase, the key enzyme of melanogenesis, was examined by in vivo and in vitro tyrosinase assay and Western blot. The results indicate that (2Z,8Z)-matricaria acid methyl ester isolated from Erigeron breviscapus is a promising compound that could be useful for treating hyper-pigmentation as skin-whitening agents.Key words melanin; Erigeron breviscapus; (2Z,8Z)-matricaria acid methyl ester; skin whitening Biol.

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Section: )mentioning

confidence: 99%

Depigmentation of Melanocytes by (2Z,8Z)-Matricaria Acid Methyl Ester Isolated from Erigeron breviscapus

Luo

Kim

Nguyen

et al. 2009

Biological & Pharmaceutical Bulletin

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“…Delivery systems have been developed to increase the blood drug concentration and to prolong the circulation time of breviscapine, including multivesicular liposomes [5] , unilamellar vesicles [6] and polymeric nanoparticles [7] . Despite their great success, there are some limitations to these systems.…”

Section: Introductionmentioning

confidence: 99%

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Zheng

Shan

et al. 2013

Acta Pharmacol Sin

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Aim: Breviscapine isolated from the Chinese herb Erigeron breviscapus (Vant) Hand-Mazz is widely used to treat cardiovascular and cerebrovascular diseases. The aim of this study was to improve the pharmacokinetic profiles of breviscapine using nanostructured lipid carrier based on an ionic complex formation. Methods: Breviscapine nanostructured lipid carrier (Bre-NLC) was prepared using the thin film homogenization method. The morphology of Bre-NLCs was determined using transmission electron microscopy. The mean particle size, polydispersity index, zeta-potential analysis and entrapment efficiency were analized. In vitro release was studied using the dialysis method. In vitro stability was studied in fresh plasma and liver slurry of rats. In vivo pharmacokinetics was analyzed in rats after intravenous injection of a dose equivalent to breviscapine (10 mg/kg). Results: The Bre-NLCs were spherical with a mean particle size of ~170 nm, a zeta potential of ~20 mV and a high entrapment efficiency of ~89%. Compared with a commercially available solution, a substantial decrease in the cumulative release of breviscapine was found for the Bre-NLCs. The NLC has a significantly protective effect against the liver enzyme degradation of breviscapine. After intravenous administration in rats, the Bre-NLCs exhibited a 32 times increase in the AUC 0-t and a 12 times increase in T 1/2 as compared to the commercially available breviscapine solution. Conclusion:The results demonstrate that the NLC has great potential to use as a novel sustained release system for breviscapine.

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“…9) Clinic observations indicate that breviscapine can ameliorate ischemia-induced cognitive impairment and cerebral infarction. 12,13,43) The curative dosage of breviscapine (0.5 mg/kg, i.v.…”

Section: Discussionmentioning

confidence: 99%

Protective Effects of Breviscapine on Ischemic Vascular Dementia in Rats

Xiong

Liu

Wang

et al. 2006

Biological & Pharmaceutical Bulletin

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With an increase of elderly population, aging-related diseases such as hypertension, arteriosclerosis and different forms of dementia are also increased. 1) One of these diseases is vascular dementia (VD). VD is a step-wise deterioration in intellectual powers that appear as different areas of the brain are damaged by loss of blood supply.2,3) The conventional concept of VD is that of multi-infarct dementia, 3,4) arising from chronic cerebral ischemia and various vascular changes in the brain.5) It is reported that the reduction in cerebral blood flow and abnormal energy metabolism occurred in chronic cerebral ischemia can induce the accumulation of NO and ROS which lead to neurons injury in selective, vulnerable regions of the brain, especially the hippocampus and cerebral cortex, accompanied by cognitive decline and some motor disorders. [6][7][8] In oriental medicine, many traditional Chinese drugs have been used clinically for treatment of ischemic cerebrovascular disease. 9) Breviscapine is extracted from the traditional Chinese drug Erigeron Breviscapus (vant.) Hand.-Mazz and mainly composed of Scutellarein, Plantaginin and Pyromeconic acid. 10,11) The injection preparation of breviscapine has been used in clinic to treat cardiovascular diseases, cerebral infarction and stroke in China. 3,10,11) The clinical reports suggested that the injection of breviscapine (0.5 mg/kg, i.v. gtt, qd, 15 d) possess neuroprotective action and improves learning and memory in cerebrovascular diseases.12,13) Although the curative effect of breviscapine in cerebral infarction and cerebral ischemia is obvious, there is no data available for this drug in treatment of VD. In this study, the effects of chronic treatment with breviscapine on the learning deficits, neuronal injury and antioxidative properties in VD rats were investigated. MATERIALS AND METHODS Animal Models and Drug AdministrationThe vascular dementia models were made from the male Wistar rats (6 weeks, 230Ϯ10 g), which were obtained from the Experimental Animals Center of Tongji Medical College, Huazhong University of Science and Technology. Wistar rats were subjected to permanent occlusion of bilateral common carotid arteries to induce chronic cerebral ischemia and mimic the VD models.14) The experimental protocols were approved by the Committee of Animal Care of Huazhong University of Science and Technology.The injection of breviscapine (Bre, Bath No. z5302066, China) was purchased from Kunming Long-Jin Pharmaceutical Co., Ltd. Tacrine (9-amino-1,2,3,4-tetrahydroacridine HCl), a reference drug for behavioral test, was purchased from Sigma (St. Louis, MO, U.S.A.) and dissolved in physiological saline. Fifteen days after surgery, the male Wistar rats were randomly divided into three groups, e.g., sham-operated group, model group, Bre-treated group and tacrine-treated group. The Bre-treated group was administered with breviscapine (2 mg/kg, i.p., equal 0.33 mg/kg adult dose, once a day). Tacrine was administered intraperitoneally at a dosage of 3 mg/kg. The sham-ope...

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Multivesicular liposome formulation for the sustained delivery of breviscapine

Cited by 63 publications

References 23 publications

Depigmentation of Melanocytes by (2Z,8Z)-Matricaria Acid Methyl Ester Isolated from Erigeron breviscapus

Depigmentation of Melanocytes by (2Z,8Z)-Matricaria Acid Methyl Ester Isolated from Erigeron breviscapus

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Protective Effects of Breviscapine on Ischemic Vascular Dementia in Rats

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