RSC Advances
·
2016
·Vol. 6
·期 80
·76905-76914
·
IF 3.289
Liujie Zhang,Ying Kuang,Jia Liu,Zhilan Liu,Shiwen Huang,Renxi Zhuo
In this paper, a receptor-mediated liposomal drug delivery system (DDS) was developed aiming to deliver cisplatin (cis-diaminedichloroplatinum(II); CDDP) targeting the liver. Acetyl glycyrrhetinic acid (AGA) was chosen as the hepatic targeting ligand and acetyl glycyrrhetinic acid-poly(ethylene glycol)-stearate (AGA-PEG-ST) was synthesized. Anionic 5-cholestene-3-beta-ol-3-hemisuccinate (CHO-HS) was also synthesized. The liposomal CDDPs were prepared by employing these functional moieties with phosphatidylcholine (PC) at various ratios. Meanwhile, methoxypolyethylene glycol-stearate (MPEG-ST) with an analogous structure but without AGA was also prepared as a control. The particle sizes of AGA modified liposomes ranged from 120 nm to 180 nm and the zeta potentials were located between −39.7 mV and −3.18 mV. The liposomes had encapsulation percentages of 51.5–61.7% and a loading capacity of 23.2–26.7% for CDDP. The transmission electron microscopy (TEM) observations showed that the liposomes had spherical morphologies with homogeneous distribution. In vitro cytotoxicity of CDDP-loaded liposomes against HepG2 human liver cancer cells and A549 human lung epithelial carcinoma cells were evaluated by MTT assays. The results demonstrated that the introduction of AGA could enhance the cytotoxicity of liposomal CDDP against HepG2 cells but showed less significant impact on A549 cells. CLSM observation and FCM measurement further confirmed that AGA modified liposomes had a stronger affinity to HepG2 cells than that of liposomes without AGA. The tissue distribution of calcein in mice indicated that AGA modified liposomes resulted in higher accumulation in the liver than that of liposomes without the AGA ligand. These results demonstrated the promise of AGA decorated anionic liposomes for hepatic targeted delivery of cisplatin.
研究领域:
药剂学
·
肿瘤学
·
纳米医学
·
药物递送系统
·
肝病学
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2014
·
IF 3.785
Ling-Ran Du,Xiao-Jing Lu,Hai-Tao Guan,Yong-Jie Yang,Meng-Jie Gu,Zhuo-Zhao Zheng,Tian-Shi Lv,Zi-Guang Yan,Li Song,Ying-Hua Zou,Nai-Qi Fu,Xian-Rong Qi,Tian-Yuan Fan
New type of liquid embolic agents based on a liquid crystalline material of glyceryl monooleate (GMO) was developed and evaluated in this study. Ternary phase diagram of GMO , water and ethanol was constructed and three isotropic liquids (ILs, GMO:ethanol:water = 49:21:30, 60:20:20 and 72:18:10 (w/w/w)) were selected as potential liquid embolic agents, which could spontaneously form viscous gel cast when contacting with water or physiological fluid. The ILs exhibited excellent microcatheter deliverability due to low viscosity, and were proved to successfully block the saline flow when performed in a device to simulate embolization in vitro . The ILs also showed good cytocompatibility on L929 mouse fibroblast cell line. The embolization of ILs to rabbit kidneys was performed successfully under monitoring of digital subtraction angiography (DSA), and embolic degree was affected by the initial formulation composition and used volume. At 5th week after embolization, DSA and computed tomography (CT) confirmed the renal arteries embolized with IL did not recanalize in follow-up period, and an obvious atrophy of the embolized kidney was observed. Therefore, the GMO-based liquid embolic agents showed feasible and effective to embolize, and potential use in clinical interventional embolization therapy.
研究领域:
生物材料学
·
介入放射学
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药剂学
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血管内治疗
·
转化医学
✓ 已验证
DOI
高影响因子
JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2018
·
IF 5.091
Xian-peng Zhang,Jian Luo,Da-xia Zhang,Tong-fang Jing,Bei-xing Li,Feng Liu
In this paper, porous microcapsules with tunable pore sizes were prepared using interfacial polymerization by employing a temperature-responsive cross-linking agent above its so-called cloud point temperature ( T scp ). The influences of porosity on the surface morphology , release profile and biological activity of the microcapsules were investigated. The results showed that both pore size and pore density could be controlled by regulating either the amount of cross-linking agent or the ratio of core material to shell material. Furthermore, the porosity of the microcapsules determined their release properties and further regulated the bioactivity of the microcapsules. In addition, the mechanism of pore formation was confirmed by investigating the morphology of microcapsules below the T scp . The microencapsulation methodology described here is convenient and versatile, which can be easily extended to encapsulate a broad range of lipophilic core materials.
研究领域:
药剂学
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生物材料
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纳米医学
·
药物递送
·
高分子科学
✓ 已验证
DOI
高影响因子
Journal of the Taiwan Institute of Chemical Engineers
·
2016
·
IF 2.848
Zhanjing Guo,Xiongmin Liu,Hongmiao Huang,Lingfeng Jiang
The strong acidic cationic exchange fiber (SACEF) was used to adsorb yohimbine from alcoholic solution. Batch experiments were performed to examine the effects of adsorbent dosage, solution pH and temperature in the adsorption process. The thermodynamics and kinetics of adsorption were also analyzed. The optimum yohimbine adsorption onto the SACEF was found at pH = 5 of solution and equilibrium could be attained within 20 min. The equilibrium adsorption data were preferably modeled with the Freundlich isotherm model and the thermodynamic parameters were calculated to be: 11.99 kJ/mol < Δ H < 13.72 kJ/mol, −21.17 kJ/mol < Δ G < −17.87 kJ/mol and 63.18 J/mol K < Δ S < 65.60 J/mol K. The results demonstrated that the adsorption was an endothermic, spontaneous and feasible process of physisorption . Meanwhile, yohimbine adsorption on SACEF fitted well to the pseudo-second-order kinetic model and the adsorption rate was limited by film diffusion. The activation energy Ea was calculated to be 14.39 kJ/mol. Furthermore, the surface morphologies of the SACEF before and after yohimbine adsorption were analyzed by SEM and the adsorption mechanism was discussed by FTIR analysis. SACEF could effectively adsorb yohimbine from alcoholic solution and could be used repeatedly for more than five cycles.
研究领域:
药物化学
·
药剂学
·
物理化学
·
分离科学
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吸附科学
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天然产物提取
·
药物代谢
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2018
·
IF 3.909
Yuanfeng Pan,Jingchun Wang,Pingxiong Cai,Huining Xiao
In this work, the stepwise synthesis of interpenetrating polymer network (IPN) strategy was developed in an attempt to fabricate novel hydrogels consisting of sugarcane bagasse cellulose (SBC), carboxymethylcellulose (CMC) and poly (N-isopropylacrylamide) (PNIPAm) as a dual-responsive drug carrier. The pretreated and dissolved SBC was pre-crosslinked using epichlorohydrin in the presence of CMC, followed by in-situ free-radical polymerization of NIPAm in the presence of N,N′-Methylene-bis(acrylamide) as a crosslinking agent. The carboxyl groups in CMC and PNIPAm chains rendered the resulting hydrogel pH and thermal responsive. The results from scanning electron microscopy, infrared spectroscopy , thermogravimetric analysis and mechanical property testing demonstrated the successful formation of the IPN with proper structure and mechanical strength . The swelling experiments at different temperatures and pH showed the dual–sensibility of the hydrogels. Moreover, bovine serum albumin (BSA) was used as a model drug and loaded in the hydrogel; and the drug release behavior was revealed in phosphate buffer solution (PBS) and simulated gastric fluid (SGF). The results indicated that the dual-responsive IPN hydrogel is of great potential for the controlled release of drug.
研究领域:
高分子材料
·
药物递送
·
生物医学工程
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智能响应材料
·
药剂学
✓ 已验证
DOI
高影响因子
JOURNAL OF APPLIED POLYMER SCIENCE
·
2015
·Vol. 133
·期 15
·
IF 1.768
Mi Zhou,Kaiyue Liu,Xin Qian
A series of pH-temperature dual stimuli-responsive random copolymers poly[ N,N -dimethylaminoethyl methacrylate- co -poly(poly(ethylene glycol) methyl ether methacrylate][poly(DMAEMA- co -MPEGMA)] were synthesized by free radical polymerization. The supramolecular hydrogel was formed by pseudopolyrotaxane, which was prepared with the host-guest interactions between α-cyclodextrin (α-CD) and poly(ethylene glycol) (PEG) side chains. Fourier transform infrared (FT-IR), nuclear magnetic resonance ( 1 H NMR), and X-ray diffraction (XRD) confirmed the structures of the hydrogels. The pH-temperature dual stimuli responsive properties of the hydrogels were characterized by rheometer. Finally, the controllable drug release behavior of the hydrogel, which was used 5-fluorouracil (5-Fu) as the model drug, was investigated at different temperatures and different pH values. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133 , 43279.
研究领域:
高分子材料科学
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药物递送系统
·
生物医学工程
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智能响应材料
·
药剂学
✓ 已验证
DOI
高影响因子
MATERIALS LETTERS
·
2018
·
IF 2.687
Huan Zhou,Ying Yang,Mengmeng Yang,Wenjie Wang,Yaping Bi
Mesoporous hydroxyapatite is widely applied in biomedical and environmental fields due to its high surface area and adsorption capacity. In current work a one-step hydrothermal method to synthesize mesoporous HA was developed with the assistance of a cost-effective template vitamin C. It was observed the pore size and morphology of hydrothermally synthesized HA were correlated to applied solution composition. A combination of calcium hydroxide, orthophosphate, and vitamin C can finally result in mesoporous rod-like HA nanoparticles with surface area of 88 m 2 .g −1 and pore size of 15.7 nm on average. The mesoporous HA exhibited enhanced adsorption of model drug doxorubicin in comparison to conventionally synthesized HA as expected. Consequently, this work provides new pathway to prepare mesoporous HA with advantages of economy and convenience.
研究领域:
生物材料学
·
纳米医学
·
药剂学
·
环境科学
·
生物无机化学
✓ 已验证
DOI
高影响因子
JOURNAL OF THE CHINESE CHEMICAL SOCIETY
·
2017
·Vol. 64
·期 2
·231-238
·
IF 0.935
Jie Wu,Zongmei Wu,Xuejiao Sun,Shichao Yuan,Ruling Zhang,Qingliang Lu,Yueqin Yu
Sodium alginate (SA) was combined with poly( N -isopropylacrylamide) (PNIPAAm) to prepare thermosensitive hydrogels through semi-interpenetrating polymer network (semi-IPN) and fully interpenetrating polymer network (full-IPN). The thermosensitive, swelling, mechanical, and thermal properties of pure PNIPAAm, SA/PNIPAAm semi-IPN, and Ca-alginate/PNIPAAm full-IPN hydrogels were investigated. The formation of semi-IPN and full-IPN significantly improved the hydrogels’ swelling capability and mechanical properties without altering their thermosensitivity. 5-Fluorouracil (5-Fu) was selected as a model drug to study the release behaviors of the hydrogels. It was found that in vitro controlled drug release from semi-IPN hydrogels showed an initial release burst, followed by a slower and sustained release, before reaching equilibrium. Full-IPN hydrogels showed slow and sustained release during the whole process. Temperature and pH were found to affect the rate of drug release. Ca-alginate/PNIPAAm full-IPN hydrogels have potential application as drug delivery matrices in controlled drug release.
研究领域:
生物材料
·
药剂学
·
高分子科学
·
组织工程
·
药物递送系统
✓ 已验证
DOI
高影响因子
MACROMOLECULAR CHEMISTRY AND PHYSICS
·
2012
·Vol. 213
·期 20
·2192-2200
·
IF 2.361
Xiao-Hui Dai,Chun-Yan Hong,Cai-Yuan Pan
A novel double-hydrophilic block copolymer P(MEO 2 MA- co -OEGMA)- b -PAMA has been successfully synthesized by two-step RAFT polymerization. Then, the amino groups of PAMA blocks in the copolymers react with 1-pyrenecarboxaldehyde via a “Schiff-base” reaction, and the resulting copolymers are self-assembled to form spherical micelles in aqueous solution. Because the “Schiff-base” linkage is pH sensitive, the release rate of pyrene depends upon the pH of solution. Complete release is achieved at pH 1, and the control release is much faster at pH 5.5 than that at pH 7.4. With progress of pyrene release, the micelles are disassembled gradually and disappeared completely at last. This double-hydrophilic copolymer is a promising candidate of drug carrier for the aldehyde- containing hydrophobic drugs.
研究领域:
高分子化学
·
药剂学
·
纳米医学
·
生物材料
·
药物递送系统
✓ 已验证
DOI
高影响因子
JOURNAL OF CHEMICAL THERMODYNAMICS
·
2016
·
IF 2.196
Rongrong Li,Jiaqi Weng,Cuihong Ye,Anguo Ying,Qizhong Zhou,Aiguo Zhong,Hao Chen,Jianguo Yang
The equilibrium solubility of sodium 2,4-diaminobenzene sulfonate in liquid mixtures (methanol + water, isopropanol + water, and 1,2-propanediol + water) were determined at temperatures ranging from (273.15 to 323.15) K. The solubility of sodium 2,4-diaminobenzene sulfonate increased with temperature increment but decreased with the concentrations of methanol, isopropanol or 1,2-propanediol in liquid mixtures. The obtained solubility data were correlated by Apelblat equation and Sun model. On the base of the measured solubility, the dissolution enthalpy ( Δ H sol o ) of the dissolution process were calculated.
研究领域:
药物化学
·
物理化学
·
药剂学
·
溶解行为研究
·
热力学
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2013
·
IF 3.458
Ziwei Zhang,Xiaole Qi,Xiangbo Li,Jiayu Xing,Xuehua Zhu,Zhenghong Wu
Multilayer-coating technology is the traditional method to achieve pulsatile drug release with the drawbacks of time consuming, more materials demanding and lack of efficiency. The purpose of this study was to design a novel pulsatile drug delivery system based on the physiochemical interaction between acrylic copolymer and organic acid with relatively simpler formulation and manufacturing process. The Enalapril Maleate (EM) pulsatile release pellets were prepared using extruding granulation, spheronization and fluid-bed coating technology. The ion-exchange experiment, hydration study and determination of glass transition temperature were conducted to explore the related drug release mechanism. Bioavailability experiment was carried out by administering the pulsatile release pellets to rats compared with marketed rapid release tablets Yisu ® . An obvious 4 h lag time period and rapid drug release was observed from in vitro dissolution profiles. The release mechanism was a combination of both disassociated and undisassociated forms of succinic acid physiochemically interacting with Eudragit ® RS. The AUC0-τ of the EM pulsatile pellets and the market tablets was 702.384 ± 96.891 h ng/mL and 810.817 ± 67.712 h ng/mL, while the relative bioavailability was 86.62%. These studies demonstrate this novel pulsatile release concept may be a promising strategy for oral pulsatile delivery system.
研究领域:
药剂学
·
药物递送
·
生物药剂学
·
药物代谢
·
制剂工程
·
药动学
✓ 已验证
DOI
高影响因子
JOURNAL OF CHEMICAL THERMODYNAMICS
·
2017
·
IF 2.726
Tianhua Huang,Dingqiang Lu,Xiuquan Ling,Xinxian Wang,Tongqi Liu,Fangfang Shen,Kefei He
In this paper, we focused on solubility and solution thermodynamics of istradefylline. Herein, we investigated the solubility and solution thermodynamics of istradefylline in binary solvent mixtures by gravimetric method. The solubility of istradefylline in (ethyl acetate + isopropanol), (ethyl acetate + tetrahydrofuran) and (ethyl acetate + acetone) was measured in the temperature range of 278.15 K–333.15 K under atmospheric pressure. In order to correlate the solubility of istradefylline, we employed the modified Apelblat equation, general cosolvency model and Jouyban-Acree model. Computational results showed that the modified Apelblat equation and general cosolvency model have low mean deviation. As calculated by van’t Hoff equation, the values of thermodynamic properties such as Gibbs energy, enthalpy, and entropy proved that the dissolution process is endothermic.
研究领域:
药物化学
·
药剂学
·
物理化学
·
药物热力学
·
分子溶解行为
·
药物结晶
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）