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Micronization of curcumin with biodegradable polymer by supercritical anti-solvent using micro swirl

Kimthet Chhouk, Wahyudiono, Hideki Kanda, Shin-Ichro Kawasaki, Motonobu Goto

《化学科学与工程前沿(英文)》 2018年 第12卷 第1期   页码 184-193 doi: 10.1007/s11705-017-1678-3

摘要: Curcumin is a hydrophobic polyphenol compound exhibiting a wide range of biological activities such as anti-inflammatory, anti-bacterial, anti-fungal, anti-carcinogenic, anti-human immunodeficiency virus, and anti-microbial activity. In this work, a swirl mixer was employed to produce the micronized curcumin with polyvinylpyrrolidone (PVP) by the supercritical anti-solvent process to improve the bioavailability of curcumin. The effects of operating parameters such as curcumin/PVP ratio, feed concentration, temperature, pressure, and CO flow rate were investigated. The characterization and solubility of particles were determined by using scanning electron microscopy, Fourier Transform Infrared spectroscopy, and ultra-violet-visible spectroscopy. The result shows that the optimal condition for the production of curcumin/PVP particles is at curcumin/PVP ratio of 1:30, feed concentration of 5 mg·mL , temperature of 40 °C, pressure of 15 MPa, and CO flow rate of 15 mL·min . Moreover, the dissolution of curcumin/PVP particles is faster than that of raw curcumin.

关键词: micronization     curcumin     polyvinylpyrrolidone     supercritical anti-solvent     swirl mixer    

Curcumin based combination therapy for anti-breast cancer: from

Sunhui Chen,Qiuling Liang,Shuping Xie,Ergang Liu,Zhili Yu,Lu Sun,Meong Cheol Shin,Seung Jin Lee,Huining He,Victor C. Yang

《化学科学与工程前沿(英文)》 2016年 第10卷 第3期   页码 383-388 doi: 10.1007/s11705-016-1574-2

摘要: While drug resistance appears to be an inevitable problem of an increasing number of anticancer drugs in monotherapy, combination drug therapy has become a prosperous method to reduce the administered total drug dosages as well as overcome the drug resistance of carcinoma cells. Curcumin, considered to possess multi-faceted roles in cancer treatment according to its multiple anti-neoplastic mechanisms as a depressor of chemo-resistance, can significantly facilitate its anti-cancer functions and improve therapeutic effects via combination usage with a variety of other drugs with different reaction mechanisms. To explore this possibility, four anti-cancer chemotherapeutic agents that all possess a certain degree of drug resistance problems, including three tyrosine kinase inhibitors (erlotinib, sunitinib and sorafenib) that are acting on different cell pathways and a typical anticancer drug doxorubicin, were combined with curcumin individually to examine the synergistic anti-tumor effect both and . Results revealed that sunitinib combined with curcumin at the molar ratio of 0.46 yielded the most potent synergistic effect , and was therefore chosen for further animal evaluation. To further enhance the anti-cancer effect, bovine serum albumin (BSA) nanoparticles were utilized as a carrier to deliver the selected drug combination . Preliminary findings confirmed our hypothesis of being able to maintain a similar injected drug ratio for prolonged time periods in tested animals by our approach, thereby maximizing the therapeutic potency yet minimizing the toxicity of these drugs. This work could open up a new avenue on combination drug therapy and realization the clinical utility of such drugs.

关键词: curcumin     sunitinib     synergistic effect     bovine serum albumin (BSA)     nano-carriers    

A novel cataplasma matrix of traditional Chinese medicine

Jing TIAN, Xiaolei ZHANG, Xueqin ZHOU,

《化学科学与工程前沿(英文)》 2010年 第4卷 第1期   页码 91-95 doi: 10.1007/s11705-009-0304-4

摘要: The aim of this paper was to develop a cataplasma matrix that can be applicable to both watersoluble and liposoluble drugs. The gellan gum and konjaku were employed as the scaffold materials of the matrix. With polyacrylic acid sodium and oligosaccharides as tacktifier, the formula of the cataplasma matrix was optimized in the orthogonal method as: gellan gum 0.4 g, xanthan€gum 0.03 g, konjac glue 0.1 g, glycerin 4 g, Gluco-Adhesive T (GAT) 6 g, Gluco-Adhesive E (GAE) 6 g, polyacrylic acid sodium 0.22 g, and sorbitol 3 g. The 180° peel strength, the tensile strength and the elongation at break was 3.043 N, 0.275 MPa and 91.05%, respectively. Furthermore, the drug-compatibilities of the matrix were investigated with baicalin, berberine and curcumin, which were used as the models of hydrophilic, poor-water-soluble and hydrophobic ingredients. The drug contents could reach 4.12% , 2.42% and 3.75%, while the release rate were measured as, 361.79, 55.85 and 104.41 μg·cm·hfor baicalin, berberine and curcumin, respectively. These results indicated that the obtained matrix had good drug-compatibility and drug-release properties for different ingredients.

关键词: drug-release     applicable     berberine     curcumin     different    

Establishment and drug sensitivity evaluation of murine ascites hepatocarcinoma cell line with high lymphatic metastatic potential (Hca-P/L

Hongying ZHANG, Jianwu TANG, Wenting ZHU, Chunxiu HU, Guowang XU

《医学前沿(英文)》 2009年 第3卷 第2期   页码 119-129 doi: 10.1007/s11684-009-0022-9

摘要: In order to provide a sensitive cell line model for investigating the mechanisms underlying the lymphatic metastasis of tumors and the effect of medicine against cells, a new murine ascites hepatocarcinoma cell line with high lymphatic metastatic potential (Hca-P/L ) was established and the effect of curcumin on biological behavior of Hca-P/L was observed. Murine ascites hepatocarcinoma cell strain with low lymphatic metastatic potential (Hca-P) was subcutaneously inoculated into the medioventral line of a mouse 615 and the first generation of metastatic tumor cells of inguinal lymph node (Hca-P/L ) was obtained. Then, Hca-P/L was screened by the route of mouse foot pad subcutaneously → lymph node → scale-up culture → mouse foot pad subcutaneously for five times consecutively. The sensitivity of two murine ascites hepatocarcinoma cell lines (Hca-P and Hca-P/L ) and two anchorage-dependent human hepatocarcinoma cell lines (SMC7721 and HepG ) to curcumin were studied by use of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay after these cells had been pretreated by curcumin at the concentration of 15-240 μmol/L for 48 h. After pretreatment by curcumin at the maximum non-cytotoxic dose of 15 μmol/L , the effect of curcumin against cell proliferation of Hca-P and Hca-P/L was observed by inverted microscope, cell growth curve and cell population doubling time; the effects of curcumin on cell cycles of Hca-P/L and Hca-P were studied by flow cytometry (FCM). The results showed Hca-P/L spreading to the lymph nodes at multiple sites in mice was screened from Hca-P. The lymph node metastatic rate was 100%. Curcumin had significant growth inhibiting effect on both murine ascites and human hepatocarcinoma cell lines in a dose-dependent manner ( <0. 05). At concentrations of 30-120 μmol/L, curcumin had more inhibition on murine ascites hepatocarcinoma cell lines than on human anchorage-dependent hepatocarcinoma cell lines. At concentrations of 60-240 μmol/L, curcumin had more inhibition on Hca-P/L with (the 50% inhibitory concentration) IC of 51.48 μmol/L than on Hca-P with IC of 90.87 μmol/L. After pretreatment by curcumin at the maximum non-cytotoxic dose of 15 mol/L for 7 days, the proliferations of Hca-P/L and Hca-P were inhibited ( <0.05) in a time-dependent manner ( <0.01) and the population doubling time of Hca-P/L and Hca-P was prolonged ( <0.01), and curcumin had more inhibition on Hca-P/L than on Hca-P ( <0.05). After pretreatment by 15 μmol/L curcumin for 48 h, the morphous of Hca-P/L was influenced more seriously than that of Hca-P and the cell cycle was redistributed with Hca-P/L being blocked in the S phase and Hca-P in the S and G /M phases. Hca-P/L was validated to be more sensitive to curcumin than Hca-P. Hca-P/L is a novel sensitive cell line model for investigating the mechanisms underlying tumor lymphatic metastasis and the effect of the medicine against cells.

关键词: murine ascites hepatocarcinoma cell line     metastasis     curcumin     drug sensitivity    

标题 作者 时间 类型 操作

Micronization of curcumin with biodegradable polymer by supercritical anti-solvent using micro swirl

Kimthet Chhouk, Wahyudiono, Hideki Kanda, Shin-Ichro Kawasaki, Motonobu Goto

期刊论文

Curcumin based combination therapy for anti-breast cancer: from

Sunhui Chen,Qiuling Liang,Shuping Xie,Ergang Liu,Zhili Yu,Lu Sun,Meong Cheol Shin,Seung Jin Lee,Huining He,Victor C. Yang

期刊论文

A novel cataplasma matrix of traditional Chinese medicine

Jing TIAN, Xiaolei ZHANG, Xueqin ZHOU,

期刊论文

Establishment and drug sensitivity evaluation of murine ascites hepatocarcinoma cell line with high lymphatic metastatic potential (Hca-P/L

Hongying ZHANG, Jianwu TANG, Wenting ZHU, Chunxiu HU, Guowang XU

期刊论文