The goal of this study was to improve the solubility and oral bioavailability of tamibarotene by complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The inclusion complex of tamibarotene with hydroxypropyl-β-c...The goal of this study was to improve the solubility and oral bioavailability of tamibarotene by complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The inclusion complex of tamibarotene with hydroxypropyl-β-cyclodextrin(Am80-HP-β-CD)was prepared through a freeze-drying method at the mole ratio of 1:1(Am80:HP-β-CD).Fourier transform infrared spectroscopy(FT-IR)and differential scanning calorimetry(DSC)indicated the formation of Am80-HP-β-CD.In vitro dissolution studies showed that the solubility and dissolution percentage of Am80-HP-β-CD was improved substantially compared to Am80.An improved dissolution with approximately 97%drug release in 3 min was observed,in comparison with Am80 with approximately 60% release in 45 min.In vivo studies indicated that the AUC0-∞ has increased 2.79 times and the Cmax 4.37 times after the formation of inclusion complex.The decrease of tmaxindicated the Am80-HP-β-CD inclusion complex can be absorbed into blood faster.In short,the solubility and bio-availability of Am80 has notably increased with the complexation of HP-β-CD.Therefore,using the inclusion technique is a promising method to improve the solubility of insoluble drugs.展开更多
In order to set up a simple and effective method for resolution of optical isomers, hydroxypropyl-β-cyclodextrin was bonded to silica-gel, which can be used for preparation of thin-layer chromatography plates. Resolu...In order to set up a simple and effective method for resolution of optical isomers, hydroxypropyl-β-cyclodextrin was bonded to silica-gel, which can be used for preparation of thin-layer chromatography plates. Resolution of clenbuterol and propranolol were investigated on these thin-layer chromatography plates using different combinations of solvent systems at ambient temperature. The best simultaneous resolution was achieved in solvent system of acetonitrilen-butanol (50:50, v/v). Rst values of resolution of clenbuterol hydrochloride and propranolol hydrochloride are 3.6 and 4.3, respectively. The spots of different enantiomers are separated clearly. The results showed that hydroxypropyl-β-cyclodextrin bonded silica-gel could be successful in resolution of chiral adrenergic drugs. The study offers a direct, rapid and reliable method for separation of this kind of optically active compounds.展开更多
Novel insulin-loaded nanoparticles based on hydroxypropyl-β-cyclodextrin modified carboxymethyl chitosan(CMC-HP-β-CD) were prepared to improve the oral bioavailability of insulin. The CMC-HP-β-CD was characterize...Novel insulin-loaded nanoparticles based on hydroxypropyl-β-cyclodextrin modified carboxymethyl chitosan(CMC-HP-β-CD) were prepared to improve the oral bioavailability of insulin. The CMC-HP-β-CD was characterized by FT-IR spectroscopy and 1H-NMR spectra. The insulin-loaded nanoparticles were prepared through crosslinking with calcium ions, and the morphology and size of the prepared nanoparticles were characterized by transmission electron microscopy(TEM) and dynamic light scattering(DLS). Cumulative release in vitro study was performed respectively in simulated gastric medium fluid(SGF, p H=1.2), simulated intestinal fluid(SIF, p H=6.8) and simulated colonic fluid(SCF, p H=7.4). The encapsulation efficiency of insulin was up to 87.14 ± 4.32% through high-performance liquid chromatography(HPLC). Statistics indicated that only 15% of the encapsulated insulin was released from the CMC-HP-β-CD nanoparticles in 36 h in SGF, and about 50% of the insulin could be released from the nanoparticles in SIF, whereas more than 80% was released in SCF. In addition, the solution containing insulin nanoparticles could effectively reduce the blood glucose level of diabetic mice. The cytotoxicity test showed that the samples had no cytotoxicity. CMC-HP-β-CD nanoparticles are promising candidates as potential carriers in oral insulin delivery systems.展开更多
To overcome the chemical instability of forsythiaside,the forsythiaside-hydroxypropyl-β-cyclodextrin inclusion complex was prepared by triturating. The inclusion complex was found having a varied UV spectrum and melt...To overcome the chemical instability of forsythiaside,the forsythiaside-hydroxypropyl-β-cyclodextrin inclusion complex was prepared by triturating. The inclusion complex was found having a varied UV spectrum and melt temperature point. Inclusion complex has a higher stability to UV light and temperature over forythiaside itself. Pharmacological evidence showed that inclusion complex has little effect on pharmacokinetics by chicken intravenous injection. This study is favorable for developing preparations for forsythiaside and its clinical application.展开更多
Bakuchiol isolated from Psoralea corylifolia is a naturally occurring prenylated phenolic monoterpene with a variety of bioactivities.The aim of this study was to improve the water solubility and thermal stability of ...Bakuchiol isolated from Psoralea corylifolia is a naturally occurring prenylated phenolic monoterpene with a variety of bioactivities.The aim of this study was to improve the water solubility and thermal stability of bakuchiol through complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The bakuchiol/HP-β-CD inclusion complex's behavior and characterization were investigated by ultraviolet-visible(UV-vis)spectroscopy,Fourier transform infrared spectroscopy(FT-IR),thermogravimetric analysis(TGA),X-ray diffraction(XRD),1H nuclear magnetic resonance(NMR),and two-dimensional(2D)NMR.The obtained results indicated the formation of 1∶1 inclusion complex for bakuchiol with HP-β-CD.Water solubility of bakuchiol was significantly improved by complexation with HP-β-CD as demonstrated by phase solubility studies.The encapsulation of bakuchiol was confirmed by UV-vis,FT-IR,and XRD.The thermal stability was effectively enhanced by TGA and derivative thermogravimetry(DTG)analysis.In vitro antioxidant activity showed that bakuchiol/HP-β-CD inclusion complex had a little higher antioxidant ability than free bakuchiol.Moreover,we got the possible inclusion mode for the bakuchiol/HP-β-CD inclusion complex through NMR analysis.These results suggest that the inclusion complex can be a potentially useful approach in the design of novel formulations of bakuchiol for medical applications.展开更多
Domperidone Maleate (DOM), an antiemetic drug, has been used in treatment of adults and children. It has low aqueous solubility and hence low bioavailability. In present study, an attempt has been made to enhance the ...Domperidone Maleate (DOM), an antiemetic drug, has been used in treatment of adults and children. It has low aqueous solubility and hence low bioavailability. In present study, an attempt has been made to enhance the solubility of DOM by inclusion complexation with Hydroxypropyl-β-Cyclodextrin (HP-β-CD) using kneading technique and formulation of fast disintegrating tablets by using Sodium Starch Glycolate as superdisintegrant. Solubility analysis of DOM in different concentrations of HP-β-CD was carried out. Design of experiment (DOE) is done by using MINITAB 15.1 software to find out the variable for dissolution and disintegration time. HP-β-CD and SSG were identified as the variable for disintegration time and dissolution. For optimization of the concentration of HP-β-CD and SSG, two factors at two levels design through central composite design (CCD) were used which gave 13 formulations. All formulations are evaluated for characteristics such as weight variation, hardness, friability, disintegration time and dissolution of drug. Solubility of DOM increases linearly with increase in concentration of HP-β-CD. The optimum concentration of HP-β-CD is found to be in 1:2 molar ratios and SSG of 7%. The In-Vitro dissolution studies of optimized formulation and market sample were carried out in USP type II apparatus at different time intervals of 5, 10, 15 and 30 minutes at 50 rpm in 0.1 N HCl. The dissolution and disintegration time of optimized formulation is found better than market sample.展开更多
The inclusion of atrazine with 2-hydroxypropyl-β-cyclodextrin(HPCD) was synthesized by ultrasonic method, and it was characterized by UV, XRD and 1H NMR. The solubility in water and the bioactivity of the inclusion w...The inclusion of atrazine with 2-hydroxypropyl-β-cyclodextrin(HPCD) was synthesized by ultrasonic method, and it was characterized by UV, XRD and 1H NMR. The solubility in water and the bioactivity of the inclusion were also studied here. The results indicated that the UV maximum absorption wavelength of the inclusion remained at 223 nm, while its intensity decreased. The XRD peaks of atrazine disappeared, weakened and shifted in the inclusion, and the chemical shift of H-3 and H-5 of cyclodextrin inner cavity led to the upfield. The characterization data showed that the atrazine-HPCD inclusion had already formed. At the same time, the solubility of the atrazineHPCD inclusion in water became 20.08 times as that of atrazine. Moreover, the atrazine-HPCD inclusion had better herbicidal activity. When the concentration of the inclusion was 6.5 mg/mL, the inhibition ratios of the inclusion to taproot length, taproot fresh weight, sprout length and sprout fresh weight of barnyard grass were 66.96%, 57.22%, 70% and 57.53%, respectively, which were all higher than those of atrazine.展开更多
Difenoconazole(DIF)is a representative variety of broad-spectrum triazole fungicides and liposoluble pesticides.However,the water solubility of DIF is so poor that its application is limited in plant protection.In add...Difenoconazole(DIF)is a representative variety of broad-spectrum triazole fungicides and liposoluble pesticides.However,the water solubility of DIF is so poor that its application is limited in plant protection.In addition,the conventional formulations of DIF always contain abundant organic solvents,which may cause pollution of the environment.In this study,two DIF/cyclodextrins(CDs)inclusion complexes(ICs)were successfully prepared,which were DIF/β-CD IC and DIF/hydroxypropyl-β-CD IC(DIF/HP-β-CD IC).The effect of cyclodextrins on the water solubility and the antifungal effect of liposoluble DIF pesticide were investigated.According to the phase solubility test,the molar ratio and apparent stability constant of ICs were obtained.Fourier transform infrared spectroscopy,thermal gravity analysis,X-ray diffraction and scanning electron microscopy were used systematically to characterize the formation and characteristics of ICs.The results noted that DIF successfully entered the cavities of two CDs.In addition,the antifungal effect test proved the better performance of DIF/HP-β-CD IC,which exceeded that of DIF emulsifiable concentrate.Therefore,our study provides informative direction for the intelligent use of liposoluble pesticides with cyclodextrins to develop water-based environmentally friendly formulations.展开更多
The consequence of polycyclic aromatic hydrocarbons(PAHs)in the environment is of great concern.The hydrophobic properties of PAHs significantly impact phase distribution causing limited bioavailability.Enhanced biode...The consequence of polycyclic aromatic hydrocarbons(PAHs)in the environment is of great concern.The hydrophobic properties of PAHs significantly impact phase distribution causing limited bioavailability.Enhanced biodegradation has been extensively carried out by surfactants and the redeployment effect was recognized.However,the quantitative relationship concerning the impact of solids was rarely reported.A batch of biphasic tests were carried out by introducing Mycobacterium vanbaalenii PYR-1 and hydroxypropyl-β-cyclodextrin(HPCD)into a mixture of phenanthrene solution and various glass beads(GB37-63,GB105-125,and GB350-500).The comparative results demonstrated that HPCD had little effect on microbial growth and was not degradable by bacterium.A model was proposed to describe the biodegradation process.The regression results indicated that the partition coefficient kd(1.234,0.726 and 0.448 L·g–1)and the degradation rate k(0 mmol·L^(–1):0.055,0.094,and 0.112;20 mmol·L^(–1):0.126,0.141,and 0.156;40 mmol·L^(–1):0.141,0.156 and 0.184 d^(–1))were positively and negatively correlated with the calculated total surface area(TSA)of solids,respectively.Degradation enhanced in the presence of HPCD,and the enhancing factor f was calculated(20 mmol·L^(–1):15.16,40.01,and 145.5;40 mmol·L^(–1):13.29,37.97,and 138.4),indicating that the impact of solids was significant for the enhancement of biodegradation.展开更多
A method of cross-linking multi-walled carbon nanotubes by a nucleophilic substitution of brominated multi-walled carbon nanotubes using hydroxypropyl-β-cyclodextrin anions was studied. The modified multi-walled carb...A method of cross-linking multi-walled carbon nanotubes by a nucleophilic substitution of brominated multi-walled carbon nanotubes using hydroxypropyl-β-cyclodextrin anions was studied. The modified multi-walled carbon nanotube samples were characterized using thermogravimetric analysis, energy-dispersive X-ray spectroscopy, transmission electron microscopy, scanning electron microscopy, Raman spectroscopy and Fourier transform infrared spectroscopy. The hydroxypropyl-β-cyclodextrin modified multi-walled carbon nanotubes were used as a chiral stationary phase additive for thin-layer chromatography to separate clenbuterol enantiomers, and the chiral separation factor was increased.展开更多
Objective To increase the solubility and relieve the mucous irritation of cantharidin (CA) by preparing cantharidin-hydroxypropyl-β-cyclodextrin (CA/HP-β-CD) inclusion complex. Methods The inclusion complex was prep...Objective To increase the solubility and relieve the mucous irritation of cantharidin (CA) by preparing cantharidin-hydroxypropyl-β-cyclodextrin (CA/HP-β-CD) inclusion complex. Methods The inclusion complex was prepared by co-evaporation method and characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD), and nuclear magnetic resonance (NMR). Results The disappearance of CA as well as the shift of exothermic peaks shown in DSC results indicated the complexation phenomenon. XRD results showed that the crystalline CA pattern had disappeared, and in NMR results, H-5 shifted from δ 3.731 to 3.695 after complexation and H-2 shifted from δ 3.626 to 3.598, which suggested that part of the drug had entered the HP-β-CD cavity to form an inclusion complex. The solubility increased 10.3 times after complexation and the mucous irritation of CA was relieved remarkably. Conclusion Through complexation with HP-β-CD, the solubility and dissolution rate of CA are improved significantly, and the irritation of musous is relieved.展开更多
The purpose of the present study was to investigate the interaction of Cinnarizine(CIN)with Hydroxypropyl-β-Cyclodextrin(HPβCD)in the presence of Hydroxy Acids(HA).Various binary and ternary systems of CIN with HPβ...The purpose of the present study was to investigate the interaction of Cinnarizine(CIN)with Hydroxypropyl-β-Cyclodextrin(HPβCD)in the presence of Hydroxy Acids(HA).Various binary and ternary systems of CIN with HPβCD and HA were prepared by kneading and coevaporation methods.For the ternary systems,HA were tried in three different concentrations.The interaction in solution phase was studied in detail by the phase solubility method,and the solid phase interactions were characterized by Fourier Transform Infrared(FTIR)spectroscopy,Differential Scanning Calorimetry(DSC),X-Ray Diffractometry(XRD),Scanning Electron Microscopy(SEM)and Proton Nuclear Magnetic Resonance(^1H-NMR).Phase solubility revealed the positive effect of HA on the complexation of CIN with HPβCD.Solid phase characterization confirmed the formation of inclusion complex in the ternary systems.Solubility and dissolution studies illustrated that out of three different concentrations tried,HA were most effective at the 1 M concentration level.Ternary systems were very effective in improving the solubility as well as dissolution profile of CIN than the CIN–HPβCD binary systems.FTIR,^1H-NMR and Molecular docking studies gave some insight at molecular level that actually which part of CIN was interacting with the HPβCD.Molecular docking and free energy calculation even enlighten the role of tartaric acid in increasing solubility of CIN in the ternary system.展开更多
Centella asiatica (Linn.) belongs to the family of Apiaceae(Umbeliferae). It has been widely used for traditional medicine, especially for wound healing, anti-inflammatory,antipsoriatic, antiulcer, antibacterial and a...Centella asiatica (Linn.) belongs to the family of Apiaceae(Umbeliferae). It has been widely used for traditional medicine, especially for wound healing, anti-inflammatory,antipsoriatic, antiulcer, antibacterial and antifungal. The biologically active ingredients of Centella asiatica are believed to be triterpenes, particularly asiatic acid, madecassic acid,asiaticoside and madecassoside (Fig. 1).展开更多
Post-traumatic stress disorder(PTSD)is a psychiatric disease that seriously affects brain function.Currently,selective serotonin reuptake inhibitors(SSRIs)are used to treat PTSD clinically but have decreased efficienc...Post-traumatic stress disorder(PTSD)is a psychiatric disease that seriously affects brain function.Currently,selective serotonin reuptake inhibitors(SSRIs)are used to treat PTSD clinically but have decreased efficiency and increased side effects.In this study,nasal cannabidiol inclusion complex temperature-sensitive hydrogels(CBD TSGs)were prepared and evaluated to treat PTSD.Mice model of PTSD was established with conditional fear box.CBD TSGs could significantly improve the spontaneous behavior,exploratory spirit and alleviate tension in open field box,relieve anxiety and tension in elevated plus maze,and reduce the freezing time.Hematoxylin and eosin and c-FOS immunohistochemistry slides showed that the main injured brain areas in PTSD were the prefrontal cortex,amygdala,and hippocampus CA1.CBD TSGs could reduce the level of tumor necrosis factor-a caused by PTSD.Western blot analysis showed that CBD TSGs increased the expression of the 5-HT1 A receptor.Intranasal administration of CBD TSGs was more efficient and had more obvious brain targeting effects than oral administration,as evidenced by the pharmacokinetics and brain tissue distribution of CBD TSGs.Overall,nasal CBD TSGs are safe and effective and have controlled release.There are a novel promising option for the clinical treatment of PTSD.展开更多
文摘The goal of this study was to improve the solubility and oral bioavailability of tamibarotene by complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The inclusion complex of tamibarotene with hydroxypropyl-β-cyclodextrin(Am80-HP-β-CD)was prepared through a freeze-drying method at the mole ratio of 1:1(Am80:HP-β-CD).Fourier transform infrared spectroscopy(FT-IR)and differential scanning calorimetry(DSC)indicated the formation of Am80-HP-β-CD.In vitro dissolution studies showed that the solubility and dissolution percentage of Am80-HP-β-CD was improved substantially compared to Am80.An improved dissolution with approximately 97%drug release in 3 min was observed,in comparison with Am80 with approximately 60% release in 45 min.In vivo studies indicated that the AUC0-∞ has increased 2.79 times and the Cmax 4.37 times after the formation of inclusion complex.The decrease of tmaxindicated the Am80-HP-β-CD inclusion complex can be absorbed into blood faster.In short,the solubility and bio-availability of Am80 has notably increased with the complexation of HP-β-CD.Therefore,using the inclusion technique is a promising method to improve the solubility of insoluble drugs.
基金the National Natural Science Foundation of China(No.20376085,No.20576142)for its financial support.
文摘In order to set up a simple and effective method for resolution of optical isomers, hydroxypropyl-β-cyclodextrin was bonded to silica-gel, which can be used for preparation of thin-layer chromatography plates. Resolution of clenbuterol and propranolol were investigated on these thin-layer chromatography plates using different combinations of solvent systems at ambient temperature. The best simultaneous resolution was achieved in solvent system of acetonitrilen-butanol (50:50, v/v). Rst values of resolution of clenbuterol hydrochloride and propranolol hydrochloride are 3.6 and 4.3, respectively. The spots of different enantiomers are separated clearly. The results showed that hydroxypropyl-β-cyclodextrin bonded silica-gel could be successful in resolution of chiral adrenergic drugs. The study offers a direct, rapid and reliable method for separation of this kind of optically active compounds.
基金Funded by the National Nature Science Foundation of China(No.51273156)the Open Foundation of Hubei key laboratory of Purification and Application of Plant Anti-cancer Active Ingredients(No.HLPAI2014005)
文摘Novel insulin-loaded nanoparticles based on hydroxypropyl-β-cyclodextrin modified carboxymethyl chitosan(CMC-HP-β-CD) were prepared to improve the oral bioavailability of insulin. The CMC-HP-β-CD was characterized by FT-IR spectroscopy and 1H-NMR spectra. The insulin-loaded nanoparticles were prepared through crosslinking with calcium ions, and the morphology and size of the prepared nanoparticles were characterized by transmission electron microscopy(TEM) and dynamic light scattering(DLS). Cumulative release in vitro study was performed respectively in simulated gastric medium fluid(SGF, p H=1.2), simulated intestinal fluid(SIF, p H=6.8) and simulated colonic fluid(SCF, p H=7.4). The encapsulation efficiency of insulin was up to 87.14 ± 4.32% through high-performance liquid chromatography(HPLC). Statistics indicated that only 15% of the encapsulated insulin was released from the CMC-HP-β-CD nanoparticles in 36 h in SGF, and about 50% of the insulin could be released from the nanoparticles in SIF, whereas more than 80% was released in SCF. In addition, the solution containing insulin nanoparticles could effectively reduce the blood glucose level of diabetic mice. The cytotoxicity test showed that the samples had no cytotoxicity. CMC-HP-β-CD nanoparticles are promising candidates as potential carriers in oral insulin delivery systems.
基金Supported by National Science&Technology Pillar Program during the TwelfthFive-year Plan Period(2011BAD34B01)National Natural Science Foundation of China(31372485,31172362)the opening fund from Beijing Key Laboratory of TCVM(BUA-TCVM-200904)
文摘To overcome the chemical instability of forsythiaside,the forsythiaside-hydroxypropyl-β-cyclodextrin inclusion complex was prepared by triturating. The inclusion complex was found having a varied UV spectrum and melt temperature point. Inclusion complex has a higher stability to UV light and temperature over forythiaside itself. Pharmacological evidence showed that inclusion complex has little effect on pharmacokinetics by chicken intravenous injection. This study is favorable for developing preparations for forsythiaside and its clinical application.
基金Fundamental Research Funds for the Central Universities(No.2232018D3-40)National Natural Science Foundation of China(No.81671508)。
文摘Bakuchiol isolated from Psoralea corylifolia is a naturally occurring prenylated phenolic monoterpene with a variety of bioactivities.The aim of this study was to improve the water solubility and thermal stability of bakuchiol through complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The bakuchiol/HP-β-CD inclusion complex's behavior and characterization were investigated by ultraviolet-visible(UV-vis)spectroscopy,Fourier transform infrared spectroscopy(FT-IR),thermogravimetric analysis(TGA),X-ray diffraction(XRD),1H nuclear magnetic resonance(NMR),and two-dimensional(2D)NMR.The obtained results indicated the formation of 1∶1 inclusion complex for bakuchiol with HP-β-CD.Water solubility of bakuchiol was significantly improved by complexation with HP-β-CD as demonstrated by phase solubility studies.The encapsulation of bakuchiol was confirmed by UV-vis,FT-IR,and XRD.The thermal stability was effectively enhanced by TGA and derivative thermogravimetry(DTG)analysis.In vitro antioxidant activity showed that bakuchiol/HP-β-CD inclusion complex had a little higher antioxidant ability than free bakuchiol.Moreover,we got the possible inclusion mode for the bakuchiol/HP-β-CD inclusion complex through NMR analysis.These results suggest that the inclusion complex can be a potentially useful approach in the design of novel formulations of bakuchiol for medical applications.
文摘Domperidone Maleate (DOM), an antiemetic drug, has been used in treatment of adults and children. It has low aqueous solubility and hence low bioavailability. In present study, an attempt has been made to enhance the solubility of DOM by inclusion complexation with Hydroxypropyl-β-Cyclodextrin (HP-β-CD) using kneading technique and formulation of fast disintegrating tablets by using Sodium Starch Glycolate as superdisintegrant. Solubility analysis of DOM in different concentrations of HP-β-CD was carried out. Design of experiment (DOE) is done by using MINITAB 15.1 software to find out the variable for dissolution and disintegration time. HP-β-CD and SSG were identified as the variable for disintegration time and dissolution. For optimization of the concentration of HP-β-CD and SSG, two factors at two levels design through central composite design (CCD) were used which gave 13 formulations. All formulations are evaluated for characteristics such as weight variation, hardness, friability, disintegration time and dissolution of drug. Solubility of DOM increases linearly with increase in concentration of HP-β-CD. The optimum concentration of HP-β-CD is found to be in 1:2 molar ratios and SSG of 7%. The In-Vitro dissolution studies of optimized formulation and market sample were carried out in USP type II apparatus at different time intervals of 5, 10, 15 and 30 minutes at 50 rpm in 0.1 N HCl. The dissolution and disintegration time of optimized formulation is found better than market sample.
基金Supported by the National Natural Science Foundation of China(No.31370709)
文摘The inclusion of atrazine with 2-hydroxypropyl-β-cyclodextrin(HPCD) was synthesized by ultrasonic method, and it was characterized by UV, XRD and 1H NMR. The solubility in water and the bioactivity of the inclusion were also studied here. The results indicated that the UV maximum absorption wavelength of the inclusion remained at 223 nm, while its intensity decreased. The XRD peaks of atrazine disappeared, weakened and shifted in the inclusion, and the chemical shift of H-3 and H-5 of cyclodextrin inner cavity led to the upfield. The characterization data showed that the atrazine-HPCD inclusion had already formed. At the same time, the solubility of the atrazineHPCD inclusion in water became 20.08 times as that of atrazine. Moreover, the atrazine-HPCD inclusion had better herbicidal activity. When the concentration of the inclusion was 6.5 mg/mL, the inhibition ratios of the inclusion to taproot length, taproot fresh weight, sprout length and sprout fresh weight of barnyard grass were 66.96%, 57.22%, 70% and 57.53%, respectively, which were all higher than those of atrazine.
文摘Difenoconazole(DIF)is a representative variety of broad-spectrum triazole fungicides and liposoluble pesticides.However,the water solubility of DIF is so poor that its application is limited in plant protection.In addition,the conventional formulations of DIF always contain abundant organic solvents,which may cause pollution of the environment.In this study,two DIF/cyclodextrins(CDs)inclusion complexes(ICs)were successfully prepared,which were DIF/β-CD IC and DIF/hydroxypropyl-β-CD IC(DIF/HP-β-CD IC).The effect of cyclodextrins on the water solubility and the antifungal effect of liposoluble DIF pesticide were investigated.According to the phase solubility test,the molar ratio and apparent stability constant of ICs were obtained.Fourier transform infrared spectroscopy,thermal gravity analysis,X-ray diffraction and scanning electron microscopy were used systematically to characterize the formation and characteristics of ICs.The results noted that DIF successfully entered the cavities of two CDs.In addition,the antifungal effect test proved the better performance of DIF/HP-β-CD IC,which exceeded that of DIF emulsifiable concentrate.Therefore,our study provides informative direction for the intelligent use of liposoluble pesticides with cyclodextrins to develop water-based environmentally friendly formulations.
文摘The consequence of polycyclic aromatic hydrocarbons(PAHs)in the environment is of great concern.The hydrophobic properties of PAHs significantly impact phase distribution causing limited bioavailability.Enhanced biodegradation has been extensively carried out by surfactants and the redeployment effect was recognized.However,the quantitative relationship concerning the impact of solids was rarely reported.A batch of biphasic tests were carried out by introducing Mycobacterium vanbaalenii PYR-1 and hydroxypropyl-β-cyclodextrin(HPCD)into a mixture of phenanthrene solution and various glass beads(GB37-63,GB105-125,and GB350-500).The comparative results demonstrated that HPCD had little effect on microbial growth and was not degradable by bacterium.A model was proposed to describe the biodegradation process.The regression results indicated that the partition coefficient kd(1.234,0.726 and 0.448 L·g–1)and the degradation rate k(0 mmol·L^(–1):0.055,0.094,and 0.112;20 mmol·L^(–1):0.126,0.141,and 0.156;40 mmol·L^(–1):0.141,0.156 and 0.184 d^(–1))were positively and negatively correlated with the calculated total surface area(TSA)of solids,respectively.Degradation enhanced in the presence of HPCD,and the enhancing factor f was calculated(20 mmol·L^(–1):15.16,40.01,and 145.5;40 mmol·L^(–1):13.29,37.97,and 138.4),indicating that the impact of solids was significant for the enhancement of biodegradation.
基金Project supported by the National Natural Science Foundation of China (No. 50772133), the Central South University Science Development Foundation (No. 10SDF04), the Planned Science and Technology Project of Hunan Province (No. 2010GK3113) and the Fundamental Research Funds for the Central Universities (No. 201012200146).
文摘A method of cross-linking multi-walled carbon nanotubes by a nucleophilic substitution of brominated multi-walled carbon nanotubes using hydroxypropyl-β-cyclodextrin anions was studied. The modified multi-walled carbon nanotube samples were characterized using thermogravimetric analysis, energy-dispersive X-ray spectroscopy, transmission electron microscopy, scanning electron microscopy, Raman spectroscopy and Fourier transform infrared spectroscopy. The hydroxypropyl-β-cyclodextrin modified multi-walled carbon nanotubes were used as a chiral stationary phase additive for thin-layer chromatography to separate clenbuterol enantiomers, and the chiral separation factor was increased.
基金National S&T Major Special Project on Major New Drug Innovation (2009ZX09301-003&2008ZX09103-390)
文摘Objective To increase the solubility and relieve the mucous irritation of cantharidin (CA) by preparing cantharidin-hydroxypropyl-β-cyclodextrin (CA/HP-β-CD) inclusion complex. Methods The inclusion complex was prepared by co-evaporation method and characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD), and nuclear magnetic resonance (NMR). Results The disappearance of CA as well as the shift of exothermic peaks shown in DSC results indicated the complexation phenomenon. XRD results showed that the crystalline CA pattern had disappeared, and in NMR results, H-5 shifted from δ 3.731 to 3.695 after complexation and H-2 shifted from δ 3.626 to 3.598, which suggested that part of the drug had entered the HP-β-CD cavity to form an inclusion complex. The solubility increased 10.3 times after complexation and the mucous irritation of CA was relieved remarkably. Conclusion Through complexation with HP-β-CD, the solubility and dissolution rate of CA are improved significantly, and the irritation of musous is relieved.
文摘The purpose of the present study was to investigate the interaction of Cinnarizine(CIN)with Hydroxypropyl-β-Cyclodextrin(HPβCD)in the presence of Hydroxy Acids(HA).Various binary and ternary systems of CIN with HPβCD and HA were prepared by kneading and coevaporation methods.For the ternary systems,HA were tried in three different concentrations.The interaction in solution phase was studied in detail by the phase solubility method,and the solid phase interactions were characterized by Fourier Transform Infrared(FTIR)spectroscopy,Differential Scanning Calorimetry(DSC),X-Ray Diffractometry(XRD),Scanning Electron Microscopy(SEM)and Proton Nuclear Magnetic Resonance(^1H-NMR).Phase solubility revealed the positive effect of HA on the complexation of CIN with HPβCD.Solid phase characterization confirmed the formation of inclusion complex in the ternary systems.Solubility and dissolution studies illustrated that out of three different concentrations tried,HA were most effective at the 1 M concentration level.Ternary systems were very effective in improving the solubility as well as dissolution profile of CIN than the CIN–HPβCD binary systems.FTIR,^1H-NMR and Molecular docking studies gave some insight at molecular level that actually which part of CIN was interacting with the HPβCD.Molecular docking and free energy calculation even enlighten the role of tartaric acid in increasing solubility of CIN in the ternary system.
文摘Centella asiatica (Linn.) belongs to the family of Apiaceae(Umbeliferae). It has been widely used for traditional medicine, especially for wound healing, anti-inflammatory,antipsoriatic, antiulcer, antibacterial and antifungal. The biologically active ingredients of Centella asiatica are believed to be triterpenes, particularly asiatic acid, madecassic acid,asiaticoside and madecassoside (Fig. 1).
基金funded by the Beijing Municipal Natural Science Foundation,China(7202147 and 7172072,China)
文摘Post-traumatic stress disorder(PTSD)is a psychiatric disease that seriously affects brain function.Currently,selective serotonin reuptake inhibitors(SSRIs)are used to treat PTSD clinically but have decreased efficiency and increased side effects.In this study,nasal cannabidiol inclusion complex temperature-sensitive hydrogels(CBD TSGs)were prepared and evaluated to treat PTSD.Mice model of PTSD was established with conditional fear box.CBD TSGs could significantly improve the spontaneous behavior,exploratory spirit and alleviate tension in open field box,relieve anxiety and tension in elevated plus maze,and reduce the freezing time.Hematoxylin and eosin and c-FOS immunohistochemistry slides showed that the main injured brain areas in PTSD were the prefrontal cortex,amygdala,and hippocampus CA1.CBD TSGs could reduce the level of tumor necrosis factor-a caused by PTSD.Western blot analysis showed that CBD TSGs increased the expression of the 5-HT1 A receptor.Intranasal administration of CBD TSGs was more efficient and had more obvious brain targeting effects than oral administration,as evidenced by the pharmacokinetics and brain tissue distribution of CBD TSGs.Overall,nasal CBD TSGs are safe and effective and have controlled release.There are a novel promising option for the clinical treatment of PTSD.