scholarly journals Preparation, Characterization, and Dissolution RateIn VitroEvaluation of TotalPanaxNotoginsenoside Nanoparticles, Typical Multicomponent Extracts from Traditional Chinese Medicine, Using Supercritical Antisolvent Process

2015 ◽  
Vol 2015 ◽  
pp. 1-12 ◽  
Author(s):  
Ying Zhang ◽  
Xiuhua Zhao ◽  
Wengang Li ◽  
Yuangang Zu ◽  
Yong Li ◽  
...  

TotalPanaxnotoginsenosides nanoparticles, typical multicomponent extracts from traditional Chinese medicine, were prepared with a supercritical antisolvent (SAS) process using ethanol as solvent and carbon dioxide as antisolvent. The optimum conditions were determined to be as follows: TPNS solution concentration of 2.5 mg/mL, TPNS solution flow rate of 6.6 mL/min, precipitation temperature of 40°C, and precipitation pressure of 20 MPa. Under the optimum conditions, TPNS nanoparticles with a MPS of 141.5 ± 18.2 nm and total saponins amounts (TSA) of 78.9% were obtained. The TPNS nanoparticles obtained were characterized by scanning electron microscopy (SEM), dynamic light scattering (DLS), Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimeters (DSC), and high performance liquid chromatography (HPLC). The results showed that the chemical and crystal structure of the obtained TPNS nanoparticles has not changed. Dissolutionin vitrostudies showed that the solubility and dissolution rate of notoginsenosides R1 and ginsenoside Rb1 in TPNS nanoparticles are higher than these in raw TPNS, with no obvious difference in Rg1. These results suggest that TPNS nanoparticles can be helpful to the improvement of its bioavailability for the treatment of cardiovascular diseases.

Nanomaterials ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 322 ◽  
Author(s):  
Lin-Fei Chen ◽  
Pei-Yao Xu ◽  
Chao-Ping Fu ◽  
Ranjith Kumar Kankala ◽  
Ai-Zheng Chen ◽  
...  

Due to its hydrophobicity, fisetin (FIS) often suffers from several limitations in terms of its applicability during the fabrication of pharmaceutical formulations. To overcome this intrinsic limitation of hydrophobicity, we demonstrate here the generation of poly (vinyl pyrrolidone) (PVP)-encapsulated FIS nanoparticles (FIS-PVP NPs) utilizing a supercritical antisolvent (SAS) method to enhance its aqueous solubility and substantial therapeutic effects. In this context, the effects of various processing and formulation parameters, including the solvent/antisolvent ratio, drug/polymer (FIS/PVP) mass ratio, and solution flow rate, on the eventual particle size as well as on distribution were investigated using a 23 factorial experimental design. Notably, the FIS/PVP mass ratio significantly affected the morphological attributes of the resultant particles. Initially, the designed constructs were characterized systematically using various techniques (e.g., chemical functionalities were examined with Fourier-transform infrared (FTIR) spectroscopy, and physical states were examined with X-ray diffraction analysis (XRD) and differential scanning calorimetry (DSC) techniques). In addition, drug release as well as cytotoxicity evaluations in vitro indicated that the nanosized polymer-coated particles showed augmented performance efficiency compared to the free drug, which was attributable to the improvement in the dissolution rate of the FIS-PVP NPs due to their small size, facilitating a higher surface area over the raw form of FIS. Our findings show that the designed SAS process-assisted nanoconstructs with augmented bioavailability, have great potential for applications in pharmaceutics.


2020 ◽  
Vol 16 ◽  
Author(s):  
Ya-nan Zhu ◽  
Shuo Zhang ◽  
Min Zhang ◽  
Xiao-xia Meng ◽  
Peng-jiao Wang ◽  
...  

: Polyethylene glycol 400 (PEG400), as a good traditional Chinese medicine solvent, diluent and solubilizer, is widely used as a main pharmaceutical excipient in traditional Chinese medicine compound preparations containing active ingredient baicalin. PEG400 could increase the solubility and release of baicalin in vivo, but it was unknown if PEG400 affected the absorption and distribution of baicalin or not. At present, the effects of PEG400 after oral administration of baicalin on the pharmacokinetic characteristics and tissue distribution behaviors of baicalin itself and its main flavonoid metabolites baicalein-6-O-β-glucopyranoside (B6G) and baicalein were investigated by a rapid, efficient and sensitive ultra-high performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS) method. Moreover, we respectively studied the effects of PEG400 on the activities and protein expressions of two subtypes UDP-glucuronyltransferase 1 A8/A9 (UGT1A8 and UGT1A9) of UDP-glucuronosyltransferases (UGTs) in vitro and vivo experiments to determine the partial mechanisms by which PEG400 altered the pharmacokinetics and tissue distribution behaviors of the three flavonoid metabolites. The results showed that PEG400 significantly increased the Cmax and AUC0-t values (P<0.05 or P<0.01) of baicalin and B6G while baicalein could not be quantified due to its extremely low concentration (lower the LLOQ) in plasma. Baicalin, B6G and baicalein were mainly distributed in the stomach, small intestine, kidney and liver. PEG400 changed the distribution of three flavonoid metabolites in various tissues and also increased the activities and expressions of UGT1A8 and UGT1A9. In conclusion, PEG400 significantly altered the pharmacokinetic characteristics and tissue distribution behaviors of three flavonoid metabolites. This may partly result from PEG400 upregulation of the activities and expressions of the drug biphasic metabolic enzymes UGT1A8 and UGT1A9, which provided a material basis.


2015 ◽  
Vol 30 (6) ◽  
pp. 602-612 ◽  
Author(s):  
Lee E. Hullender Rubin ◽  
Michael S. Opsahl ◽  
Klaus E. Wiemer ◽  
Scott D. Mist ◽  
Aaron B. Caughey

Pathogens ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 532
Author(s):  
Hae-Soo Yun ◽  
Sylvatrie-Danne Dinzouna-Boutamba ◽  
Sanghyun Lee ◽  
Zin Moon ◽  
Dongmi Kwak ◽  
...  

In traditional Chinese medicine, Ranunculus japonicus has been used to treat various diseases, including malaria, and the young stem of R. japonicus is consumed as a food in the Republic of Korea. However, experimental evidence of the antimalarial effect of R. japonicus has not been evaluated. Therefore, the antimalarial activity of the extract of the young stem of R. japonicus was evaluated in vitro using both chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) strains; in vivo activity was evaluated in Plasmodium berghei-infected mice via oral administration followed by a four-day suppressive test focused on biochemical and hematological parameters. Exposure to extracts of R. japonicus resulted in significant inhibition of both chloroquine-sensitive (3D7) and resistant (Dd2) strains of P. falciparum, with IC50 values of 6.29 ± 2.78 and 5.36 ± 4.93 μg/mL, respectively. Administration of R. japonicus also resulted in potent antimalarial activity against P. berghei in infected mice with no associated toxicity; treatment also resulted in improved hepatic, renal, and hematologic parameters. These results demonstrate the antimalarial effects of R. japonicus both in vitro and in vivo with no apparent toxicity.


2014 ◽  
Vol 42 (05) ◽  
pp. 1071-1098 ◽  
Author(s):  
Mao-Xing Li ◽  
Xi-Rui He ◽  
Rui Tao ◽  
Xinyuan Cao

In the present review, the literature data on the chemical constituents and biological investigations of the genus Pedicularis are summarized. Some species of Pedicularis have been widely applied in traditional Chinese medicine. A wide range of chemical components including iridoid glycosides, phenylpropanoid glycosides (PhGs), lignans glycosides, flavonoids, alkaloids and other compounds have been isolated and identified from the genus Pedicularis. In vitro and in vivo studies indicated some monomer compounds and extracts from the genus Pedicularis have been found to possess antitumor, hepatoprotective, anti-oxidative, antihaemolysis, antibacterial activity, fatigue relief of skeletal muscle, nootropic effect and other activities.


Blood ◽  
2008 ◽  
Vol 111 (4) ◽  
pp. 2354-2363 ◽  
Author(s):  
Sven Baumann ◽  
Stefanie C. Fas ◽  
Marco Giaisi ◽  
Wolfgang W. Müller ◽  
Anette Merling ◽  
...  

Herbs have successfully been used in traditional Chinese medicine for centuries. However, their curative mechanisms remain largely unknown. In this study, we show that Wogonin, derived from the traditional Chinese medicine Huang-Qin (Scutellaria baicalensis Georgi), induces apoptosis in malignant T cells in vitro and suppresses growth of human T-cell leukemia xenografts in vivo. Importantly, Wogonin shows almost no toxicity on T lymphocytes from healthy donors. Wogonin induces prolonged activation of PLCγ1 via H2O2 signaling in malignant T cells, which leads to sustained elevation of cytosolic Ca2+ in malignant but not normal T cells. Subsequently, a Ca2+ overload leads to disruption of the mitochondrial membrane. The selective effect of Wogonin is due to its differential regulation of the redox status of malignant versus normal T cells. In addition, we show that the L-type voltage-dependent Ca2+ channels are involved in the intracellular Ca2+ mobilization in T cells. Furthermore, we show that malignant T cells possess elevated amounts of voltage-dependent Ca2+ channels compared with normal T cells, which further enhance the cytotoxicity of Wogonin for malignant T cells. Taken together, our data show a therapeutic potential of Wogonin for the treatment of hematologic malignancies.


RSC Advances ◽  
2017 ◽  
Vol 7 (6) ◽  
pp. 3408-3412 ◽  
Author(s):  
Long Ma ◽  
Haiyan Liu ◽  
Lingpei Meng ◽  
Ping Qin ◽  
Botao Zhang ◽  
...  

Triterpenoidal saponins fraction isolated from a traditional Chinese medicine Conyza blinii H. Lév. demonstrates anti-cancer activity both in vitro and in vivo.


Author(s):  
M. Shunmugasundaram ◽  
A. Praveenkumar ◽  
L. Ponraj Sankar ◽  
S. Sivasankar

Mechanical properties of materials are enhanced by different methods to increase the usage of the materials. In this research spray pyrolysis method is employed to increase the mechanical characteristics of three different materials. The tin oxide is chosen as coated material and aluminium, brass, mild steel are selected as substrate materials. The 500nm thin film is developed over the substrate materials by spray pyrolysis. The substrate temperature are chosen as 300? C for aluminium, 400? C for brass and mildsteel. Nozzle to substrate distance is 0.4 m, substrate temperature is 300? C for aluminium and 400? C for solution concentration as 0.2 mole and solution flow rate is 1ml/min are selected for constant deposition parameters. The hardness and tensile strength result clearly shows that strength is increased by adding the coating over the surface. The material is heated above crystallization temperature and SnO2 increases the tensile and hardness strength of the materials. The triangular metrological microscope is used to examine the microstructure of non coated and coated substrate materials. The microstructural analysis is showed that the uncoated surface of the substrate material is full of rough and pores. And displays that the tin oxide coated surface of the substrates after the initial deposition disclosed a surface with a agglomeration of tin oxide in homogeneous and uniform than the uncoated substrates.


2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
Xiu Juan Xin ◽  
Jiahong Zou ◽  
Tao Zou ◽  
Huoli Shang ◽  
Li Yun Sun

Vitiligo is a kind of skin dysfunction on melanogenesis. The highly prevalent, chronic, and distinctive complexion changes on patients have imposed enormous psychic and economic burden on both individuals and society. Traditional Chinese Medicine (TCM) is a kind of precious source on chronic disease treatment, including skin dysfunctional diseases. In our previous study, a new compound named apigenin-7-butylene glucoside has been authenticated and purified from a prescription of Chinese traditional medicine formula which has been used clinically in vitiligo treatment. The aim of this work is to evaluate the effects of this compound on melanogenesis using melanoma cell B16-F10 in vitro. The results showed that apigenin-7-butylene glucoside had almost no cytotoxicity on B16-F10 cells within a lower dose of 5.0 μg ml-1 and enhanced the melanin level to about 41% and tyrosinase activity to 1.32-fold when compared with controls. The compound showed minor cytotoxicity to B16-F10 cells at the higher concentration of 10 μg ml-1 and 50 μg ml-1, the inhibition rate was 8.4% and 11.8%, and the melanin level and tyrosinase activity showed a decreased trend because of the lower cell number at the higher concentrations. The results indicated that apigenin-7-butylene glucoside was safe to B16-F10 cells within a lower concentration, <5.0 μg ml-1. Incubated with 5.0 ug ml-1of apigenin-7-butylene glucoside for 48 hours, the mRNA and protein levels of Tyr, Trp-1, and Trp-2 genes were all increased except Mitf in B16-F10 cells. The stimulation of apigenin-7-butylene glucoside on melanogenesis of B16-F10 cells through Tyr, Trp-1, and Trp-2 pathway highlighted the potential usage of the compound in vitiligo treatment.


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