JOURNAL OF CHEMICAL THERMODYNAMICS
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2020
·
IF 2.888
Jiao Sha,Teng Ma,Rui Zhao,Pengshuai Zhang,Renren Sun,Gaoliang Jiang,Yameng Wan,Haixia He,Xinding Yao,Yu Li,Tao Li,Baozeng Ren
In this work, the solubility of doxifluridine in methanol, ethanol, n-propanol, n-butanol, isobutanol, n-Pentanol, n-hexanol, n-octanol, (±)-2-ethyl-1-hexanol, acetone, dimethyl formamide (DMF), dimethyl sulfoxide (DMSO) were experimentally determined by a laser dynamic method within the temperature range from 278.15 K to 333.15 K at 101.3 kPa. The measured results demonstrated that the experimental solubility of doxifluridine in all selected pure solvents increased with the rise of temperature. It was also found that the order of the mole fraction solubility of doxifluridine in the twelve mono-solvents was: DMSO > DMF > methanol > acetone > ethanol > n-propanol > n-butanol > n-pentanol > n-hexanol ≈ isobutanol > n-octanol > (±)-2-ethyl-1-hexanol. In order to facilitate the industrial application and other studies, the experimental data of solubility were fitted well using the λh equation, the van't Hoff equation, the modified Apelblat equation, the NRTL model and the UNIQUAC model. Moreover, the apparent thermodynamic properties of doxifluridine in all mono-solvents were investigated by the famous modified Van't Hoff equation from the solubility data.
研究领域:
药学
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物理化学
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产品关联
DOI
高影响因子
RSC Advances
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2014
·Vol. 4
·期 35
·18171-18177
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IF 3.708
Shuying Yu,Wenhua Yang,Sheng Chen,Mengjie Chen,Yezhuo Liu,Zhengzhong Shao,Xin Chen
Silk protein is a very promising biomedical material due to its renewability, nontoxicity, biocompatibility, and biodegradability. In this communication, we report our attempt to use regenerated silk fibroin (RSF) as a drug-carrier to encapsulate hydrophilic anti-cancer drug floxuridine (FUDR). The FUDR-loaded RSF nanospheres with the average sizes ranging from 210 to 510 nm are prepared by using a facile and clean method developed in this laboratory previously based on the self-assembly of silk protein. The maximum drug loading is about 6.8% and the release time of such a kind of FUDR-loaded RSF nanospheres is more than 2 days. The FUDR-loaded RSF nanospheres are found to be able to adhere to the Hela cells easily. The FUDR loaded in the RSF nanospheres exhibits the similar curative effect to kill or inhibit Hela cells to the free FUDR. All these results imply that such a kind of biomacromolecule based anti-cancer drug nanocarrier has a great potential for the lymphatic chemotherapy in clinical applications.
研究领域:
生物医学材料
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肿瘤学
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药剂学
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DOI
高影响因子
BIOCONJUGATE CHEMISTRY
·
2015
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IF 4.513
Minxi Hu,Ping Huang,Yao Wang,Yue Su,Linzhu Zhou,Xinyuan Zhu,Deyue Yan
Combination chemotherapy has been widely applied in cancer treatment; however, the cocktail administration of combination chemotherapy could cause the nonuniform biodistribution of anticancer agents, thus impairing the therapeutic efficacy. In the present study, to address this concern, we proposed a novel strategy of preparing self-assembled nanoparticles from amphiphilic drug–drug conjugate for synergistic combination chemotherapy. The conjugate was synthesized by two-step esterification of hydrophobic camptothecin (CPT) and hydrophilic floxuridine (FUDR) through a linker compound. Because of its amphiphilic nature, the CPT-FUDR conjugate self-assembled into stable nanoparticles which could simultaneously release fixed dosage of the two drugs in cancer cells. In vitro studies demonstrated synergistic anticancer efficacy of the CPT-FUDR nanoparticles including improved cell apoptosis, varied cell cycle arrest, as well as effective inhibition of cancer cell proliferation.
研究领域:
药学
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肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
·
2020
·
IF 5.065
Jiao Sha,Ruke Zhang,Yuanyuan Zun,Rui Zhao,Yameng Wan,Haixia He,Renren Sun,Gaoliang Jiang,Yu Li,Tao Li,Baozeng Ren
The solubility values of doxifluridine in three mixed solvents of (±)-2-ethyl-1-hexanol + (methanol, ethanol and acetone) ware determined within 278.15–328.15 K under 0.1 MPa using a laser monitoring technique. It can be seen from the solubility profiles that all the solubility of doxifluridine in the mixed solvents increases with the increasing mass fraction of the co-solvent (methanol, ethanol or acetone) and the experimental temperature. The minimum and maximum mole fraction solubility of doxifluridine was found in ethanol + (±)-2-ethyl-1-hexanol (4.981 × 10 −5 at w 1 = 0.1003, T = 278.15 K) and methanol + (±)-2-ethyl-1-hexanol (1.109 × 10 −1 at w 1 = 0.9001, T = 328.15 K), respectively. Through the application of Hansen solubility parameters, the solubility order and miscibility of doxifluridine in the three mixed solvents studied in this work was revealed, and the results showed that the dissolution behavior of doxifluridine was not only determined by a single factor, but also the result of the comprehensive action of various solubility parameters. In addition, three semi-empirical models (λh, Modified Apelblat, and MA) and one activity coefficient model (UNIQUAC) were applied to fit the solubility data of doxifluridine. The minimum average values of ARD (average relative deviation) and 10 4 RMSD (root-mean square deviation) were acquired from Modified Apelblat model, verifying that Modified Apelblat model provides maximum consistency among the four models. Furthermore, Van't Hoff model was used to calculate the apparent thermodynamic parameters (Δ sol G °, Δ sol H °, Δ sol S °) of the dissolution process of doxifluridine. The results demonstrated that the dissolution process of doxifluridine in all the three mixed solvents studied was an entropy-driven endothermic process.
研究领域:
药学
·
物理化学
✓ 已验证
产品关联
DOI
高影响因子
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