The effect of various concentrations of 2-hydroxypropyl-β-cyclodextrin （HP-β-CD） on the solubility of dihydroartemisinin （DHA） in aqueous solution at different pHs was investigated. The influence of different co...The effect of various concentrations of 2-hydroxypropyl-β-cyclodextrin （HP-β-CD） on the solubility of dihydroartemisinin （DHA） in aqueous solution at different pHs was investigated. The influence of different concentrations of 2-hydroxypropyl-β- eyclodextrin on the stability of dihydroartemisinin at 50, 60, 70 and 80 ℃ was also studied. Inclusion complex of dihydroartemisinin with 2-hydroxypropyl-β-cyclodextrin was prepared and characterized by X-ray diffraction and differential scanning calorimetry. The 2-hydroxypropyl-β-cyclodextrin effectively inhibited the hydrolysis of dihydroartemisinin and greatly increased its solubility. Furthermore, we showed that the higher concentrations of 2-hydroxypropyl-β-cyclodextrin, the better stability and solubility of dihydroartemisinin. When the temperature was increased, the stability of dihydroartemisinin decreased. Our results indicated that 2-hydroxypropyl-β-cyclodextrin can be used as a stabilizer and solubilizer of dihydroartemisinin.展开更多
In our previous study,a novel organic selenium compound Eb was synthesized and found to have significant antitumor activity with much less toxicity compared with the leading compound Ebselen.Unfortunately,Eb was pract...In our previous study,a novel organic selenium compound Eb was synthesized and found to have significant antitumor activity with much less toxicity compared with the leading compound Ebselen.Unfortunately,Eb was practically insoluble in water （2.57 μg/mL） and had very low oral bioavailability,thus its clinical application was greatly limited.In the present study,the inclusion complex of Eb with 2-hydroxypropyl-β-cyclodextrin （HP-βCD） was prepared and pharmacokinetics of Eb and the inclusion complex were investigated.The water solubility of Eb was dramatically enhanced by inclusion with HP-βCD,which reached 8.4 mg/mL.The pharmacokinetic study showed that the elimination half-life （t 1/2β） of Eb was between 22 h and 30 h and the distribution half-life （t 1/2α） of Eb was 1 h.The results indicated that Eb was rapidly distributed to tissues but slowly eliminated in rats.The absolute bioavailability of Eb/HP-βCD inclusion complex solution through the oral route was 28.3%,and it was 1552% that of Eb in its pure form.In summary,the absorption of Eb in the Eb/HP-βCD inclusion complex was better and faster than that of Eb in its pure form.展开更多
Polycyclic aromatic hydrocarbons（PAHs）/heavy metals/fluorine（F） mixed-contaminated sites caused by abandoned metallurgic plants are receiving wide attention. To address the associated environmental problems,this s...Polycyclic aromatic hydrocarbons（PAHs）/heavy metals/fluorine（F） mixed-contaminated sites caused by abandoned metallurgic plants are receiving wide attention. To address the associated environmental problems,this study was initiated to investigate the feasibility of using carboxymethyl-β-cyclodextrin（CMCD） and carboxymethyl chitosan（CMC） solution to enhance ex situ soil washing for extracting mixed contaminants. Further,Tenax extraction method was combined with a first-three-compartment model to evaluate the environmental risk of residual PAHs in washed soil. In addition,the redistribution of heavy metals/F after decontamination was also estimated using a sequential extraction procedure. Three successive washing cycles using50 g/L CMCD and 5 g/L CMC solution were effective to remove 94.3% of total PAHs,93.2% of Pb,85.8% of Cd,93.4% of Cr,83.2% of Ni and 97.3% of F simultaneously. After the 3rd washing,the residual PAHs mainly existed as very slowly desorbing fractions,which were in the form of well-aged,well-sequestered compounds; while the remaining Pb,Cd,Cr,Ni and F mainly existed as Fe–Mn oxide and residual fractions,which were always present in stable mineral forms or bound to non-labile soil fractions. Therefore,this combined cleanup strategy proved to be effective and environmentally friendly.展开更多
The contamination of soils by polycyclic aromatic hydrocarbons （PAHs） is a widespread environmental problem and the remediation of PAHs from these areas has been a major concern. The effectiveness of many in situ bi...The contamination of soils by polycyclic aromatic hydrocarbons （PAHs） is a widespread environmental problem and the remediation of PAHs from these areas has been a major concern. The effectiveness of many in situ bioremediation systems may be constrained by low contaminant bioavailability due to limited aqueous solubility or a large magnitude of sorption. The objective of this research was to evaluate the effect of methyl-β-cyclodextrin （MCD） on bioaugmentation by Paracoccus sp. strain HPD-2 of an aged PAH-contaminated soil. When 10% （W/W） MCD amendment was combined with bioaugmentation by the PAH-degrading bacterium Paracoccus sp. strain HPD-2, the percentage degradation of total PAHs was significantly enhanced up to 34.8%. Higher counts of culturable PAH- degrading bacteria and higher soil dehydrogenase and soil polyphenol oxidase activities were observed in 10% （W/W） MCD-assisted bioaugmentation soil. This MCD-assisted bioaugmentation strategy showed significant increases （p 〈 0.05） in the average well color development （AWCD） obtained by the BIOLOG Eco plate assay, Shannon-Weaver index （H） and Simpson index （λ） compared with the controls, implying that this strategy at least partially restored the microbiological functioning of the PAH-contaminated soil. The results suggest that MCD-aided bioaugmentation by Paracoccus sp. strain HPD-2 may be a promising practical bioremediation strategy for aged PAH-contaminated soils.展开更多
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
Enantioseparation of aminoglutethimide was performed by high-speed counter-current chromatography with a two-phase system composed of ethyl acetate： methanol： water = 10： 1： 9. The lower phase contained 20 mmol/L ...Enantioseparation of aminoglutethimide was performed by high-speed counter-current chromatography with a two-phase system composed of ethyl acetate： methanol： water = 10： 1： 9. The lower phase contained 20 mmol/L of carboxymethly-β-cyclodextrin as chiral selector. The enantiomers were separated in 1.2 h and identified by chiral HPLC. This method was very efficient for the chiral preparative separation.展开更多
used－silical capillary columns containing heptakis（2、3、6－tri－o－pentyl）-β-cyclodextrinand dibenzo-18-crown-6 were prepared．By studying the selectivity of mixed stationary phases forsome solute pairs.as well a...used－silical capillary columns containing heptakis（2、3、6－tri－o－pentyl）-β-cyclodextrinand dibenzo-18-crown-6 were prepared．By studying the selectivity of mixed stationary phases forsome solute pairs.as well as comparing with the heptakis（2．3、6-tri-O-pentyl）-β-cyclodextrin and thedibenzo-18-crown-6 used as individual stationary phase、the synergistic effects were observed.These effects were affected by the column temperature．mixed ratio and linear velocity of carrier gas．展开更多
A cationic cyclodextrin derivative 6-O-（hydroxypropyltrimethylammonia）-β-cyclodextrin （GTA-β-CD） with low degree of substitution was prepared through a convenient method in solid phase. The product could be used...A cationic cyclodextrin derivative 6-O-（hydroxypropyltrimethylammonia）-β-cyclodextrin （GTA-β-CD） with low degree of substitution was prepared through a convenient method in solid phase. The product could be used as a valuable chiral selector in the capillary electrophoresis （CE） separation of some acidic drug enantiomers such as naproxen, ofloxacin, ibuprofen and warfarin.展开更多
Sulfobutylether－β－cyclodextrin（SBE－β－CD）was used as a chiral selector tor separatingten chlral drugs with resolution 1．2 by capillary zone electrophoresls（CZE）， The backgroundelectrolylc solution compris...Sulfobutylether－β－cyclodextrin（SBE－β－CD）was used as a chiral selector tor separatingten chlral drugs with resolution 1．2 by capillary zone electrophoresls（CZE）， The backgroundelectrolylc solution comprised of 120 mmol／L Britton－Robinson buffer（BRB） containing1 ～10mmol／L SBE－β－CD with the pH value adjusted from 5．0－6．8． Five of the drugs were better resolvedthan those previously reported with neutral CDs．展开更多
The inclusion interaction between three types of methylated-β-cyclodextrins （Me-β-CDs） and albendazole （ABZ） was studied by spectrofluorimetry. The result showed that Me-β-CDs reacted with ABZ to form an inclus...The inclusion interaction between three types of methylated-β-cyclodextrins （Me-β-CDs） and albendazole （ABZ） was studied by spectrofluorimetry. The result showed that Me-β-CDs reacted with ABZ to form an inclusion complex, 1： 1 stoichiometry for Me- β-CDs-ABZ complex was established and its association constant have been determined from fluorescence data by Benesi- Hildebrand＇s method （double reciprocal plots）. It was noted that 2,6-DM-β-CD exhibited stronger binding ability than other Me-β- CDs. Based on the significant enhancement of fluorescence intensity of inclusion complex, a simple and highly sensitive fluorimetric method is proposed for the determination of ABZ in the presence of 2,6-DM-β-CD. The proposed method was successfully applied to the determination of ABZ in tablets and human urine.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
A chiral stationary phase （CSP） was prepared by chemically bonding carboxymethyl-β-cyclodextrin （CM- β-CD） onto 3-aminopropyl silica gel through amidation reaction in water solution and was characterized by Four...A chiral stationary phase （CSP） was prepared by chemically bonding carboxymethyl-β-cyclodextrin （CM- β-CD） onto 3-aminopropyl silica gel through amidation reaction in water solution and was characterized by Fourier transform infrared spectroscopy （FT-IR）, element analysis （EA） and thermal gravimetry analysis （TGA）. The chromatographic performance was evaluated with 24 racemates under reversedphase conditions, The effect of salt, organic modifier, mobile phase pH and structures of analytes were discussed. In comparison with native β-CD bonded column, CYCLOBOND 12000, CM-β-CD CSP exhibited enhanced enantioseparation.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
Stimuli-responsive drug delivery systems based on polymeric micelles can achieve controlled drug release to improve the therapeutic outcome and reduce unwanted systematic toxicity and side effects of the cytotoxic dru...Stimuli-responsive drug delivery systems based on polymeric micelles can achieve controlled drug release to improve the therapeutic outcome and reduce unwanted systematic toxicity and side effects of the cytotoxic drug in chemotherapy but often face challenging synthesis and purification of functionalized biocompatible polymer materials and low drug loading efficiency. In the present study, we reported a novel redox-responsive self-assembly polymeric micelle system, mPEG-β-CD/Ad-SS-CPT, to achieve high loading efficiency and selective delivery of camptothecin(CPT) in a reductive environment inside cancer cells. The host-vip supramolecular micelles utilized a simple β-CD modified PEG, mPEG-β-cyclodextrin(mPEG-β-CD), as the polymeric host with the ease of synthesis and purification. The vip prodrug Ad-SS-CPT contained the disulfide bond as the redox sensitivity group. The selective cleavage of disulfide bond and subsequent drug release in a reductive environment could potentially reduce system toxicity and improve the therapeutic outcome of CPT. In vitro studies showed that the micelles exhibited excellent cytotoxicity against He La cells comparable to the free drug. The host-vip polymeric micelles also showed great potentials for multi-drug co-delivery. Collectively, our current findings provided a general and convenient approach to design drug delivery systems based on stimuli-responsive polymeric micelles for disease treatment.展开更多
Capillary column preparation using perpentylated (2,3,6-tri-O-pentyl)-β-cyclodextrin asstationary phase by sol-gel technology with simplicity and rapidity is described. Multiplepreparation steps in conventional colum...Capillary column preparation using perpentylated (2,3,6-tri-O-pentyl)-β-cyclodextrin asstationary phase by sol-gel technology with simplicity and rapidity is described. Multiplepreparation steps in conventional column technology were avoided. The prepared columns exhibitsatisfactory chromatographic performances and pronounced selectivity for a wide range of testsolutes, and have been successfully used for the separation of nitrotoluene, dimethoxybenzene,alcohols, alkanes, dimethylphenol and cresol isomers.展开更多
Heptakis(2, 3, 6-tri-O-octyl)-β-cyclodextrin was coated onto the fused silica capillary by sol-gel technology. Column efficiency and column selectivity were studied. The results indicated that high ability of separat...Heptakis(2, 3, 6-tri-O-octyl)-β-cyclodextrin was coated onto the fused silica capillary by sol-gel technology. Column efficiency and column selectivity were studied. The results indicated that high ability of separation was acquired . Positional isomers of aromatic compounds were well separated.展开更多
Heptakis(2.6-di-O-pentyl-3-O-ally)-β-cyclodextrin as an excellent gas chromatographic stationary phase separating phenol and cresol isomers is described.
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
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
Four basic drugs were separated by capillary electrophoresis (CE) usingcarboxymethyl-β-yclodextrin (CM-0-CD) as chiral selector. The effects of CM-β-CDconmptration, applied voltage. operation temperature were invest...Four basic drugs were separated by capillary electrophoresis (CE) usingcarboxymethyl-β-yclodextrin (CM-0-CD) as chiral selector. The effects of CM-β-CDconmptration, applied voltage. operation temperature were investigated. Under the selectedconditions. norephedrine. ofloxacin. terbutaline and chlorpheniramine were enantiomerallybaieline-separated using H3PO4-triethanolamine buffer at PH 3 containing 10, 5.5, 2. 2mmol/LCM-β-CD respectively.展开更多
文摘The effect of various concentrations of 2-hydroxypropyl-β-cyclodextrin （HP-β-CD） on the solubility of dihydroartemisinin （DHA） in aqueous solution at different pHs was investigated. The influence of different concentrations of 2-hydroxypropyl-β- eyclodextrin on the stability of dihydroartemisinin at 50, 60, 70 and 80 ℃ was also studied. Inclusion complex of dihydroartemisinin with 2-hydroxypropyl-β-cyclodextrin was prepared and characterized by X-ray diffraction and differential scanning calorimetry. The 2-hydroxypropyl-β-cyclodextrin effectively inhibited the hydrolysis of dihydroartemisinin and greatly increased its solubility. Furthermore, we showed that the higher concentrations of 2-hydroxypropyl-β-cyclodextrin, the better stability and solubility of dihydroartemisinin. When the temperature was increased, the stability of dihydroartemisinin decreased. Our results indicated that 2-hydroxypropyl-β-cyclodextrin can be used as a stabilizer and solubilizer of dihydroartemisinin.
基金Natural Science Foundation of Beijing (Grant No. 7021001)the Foundation for the Special Program of the Following Novel Candidate Drug by Beijing S&T Committee (Grant No. H20220060190)National Natural Science Foundation (Grant No.30472036)
文摘In our previous study,a novel organic selenium compound Eb was synthesized and found to have significant antitumor activity with much less toxicity compared with the leading compound Ebselen.Unfortunately,Eb was practically insoluble in water （2.57 μg/mL） and had very low oral bioavailability,thus its clinical application was greatly limited.In the present study,the inclusion complex of Eb with 2-hydroxypropyl-β-cyclodextrin （HP-βCD） was prepared and pharmacokinetics of Eb and the inclusion complex were investigated.The water solubility of Eb was dramatically enhanced by inclusion with HP-βCD,which reached 8.4 mg/mL.The pharmacokinetic study showed that the elimination half-life （t 1/2β） of Eb was between 22 h and 30 h and the distribution half-life （t 1/2α） of Eb was 1 h.The results indicated that Eb was rapidly distributed to tissues but slowly eliminated in rats.The absolute bioavailability of Eb/HP-βCD inclusion complex solution through the oral route was 28.3%,and it was 1552% that of Eb in its pure form.In summary,the absorption of Eb in the Eb/HP-βCD inclusion complex was better and faster than that of Eb in its pure form.
基金supported by the National Natural Science Foundation of China (Nos.41030531,41001335G,21377138 and 41271464b)
文摘Polycyclic aromatic hydrocarbons（PAHs）/heavy metals/fluorine（F） mixed-contaminated sites caused by abandoned metallurgic plants are receiving wide attention. To address the associated environmental problems,this study was initiated to investigate the feasibility of using carboxymethyl-β-cyclodextrin（CMCD） and carboxymethyl chitosan（CMC） solution to enhance ex situ soil washing for extracting mixed contaminants. Further,Tenax extraction method was combined with a first-three-compartment model to evaluate the environmental risk of residual PAHs in washed soil. In addition,the redistribution of heavy metals/F after decontamination was also estimated using a sequential extraction procedure. Three successive washing cycles using50 g/L CMCD and 5 g/L CMC solution were effective to remove 94.3% of total PAHs,93.2% of Pb,85.8% of Cd,93.4% of Cr,83.2% of Ni and 97.3% of F simultaneously. After the 3rd washing,the residual PAHs mainly existed as very slowly desorbing fractions,which were in the form of well-aged,well-sequestered compounds; while the remaining Pb,Cd,Cr,Ni and F mainly existed as Fe–Mn oxide and residual fractions,which were always present in stable mineral forms or bound to non-labile soil fractions. Therefore,this combined cleanup strategy proved to be effective and environmentally friendly.
基金supported by the Natural Science Foundation of Jiangsu Province (No. BK2009016)the Chinese National Environmental Protection Special Funds for Scientific Research on Public Causes (No. 2010467016)the National High Technology Research and Development Program (863) of China (No. 2007AA061101)
文摘The contamination of soils by polycyclic aromatic hydrocarbons （PAHs） is a widespread environmental problem and the remediation of PAHs from these areas has been a major concern. The effectiveness of many in situ bioremediation systems may be constrained by low contaminant bioavailability due to limited aqueous solubility or a large magnitude of sorption. The objective of this research was to evaluate the effect of methyl-β-cyclodextrin （MCD） on bioaugmentation by Paracoccus sp. strain HPD-2 of an aged PAH-contaminated soil. When 10% （W/W） MCD amendment was combined with bioaugmentation by the PAH-degrading bacterium Paracoccus sp. strain HPD-2, the percentage degradation of total PAHs was significantly enhanced up to 34.8%. Higher counts of culturable PAH- degrading bacteria and higher soil dehydrogenase and soil polyphenol oxidase activities were observed in 10% （W/W） MCD-assisted bioaugmentation soil. This MCD-assisted bioaugmentation strategy showed significant increases （p 〈 0.05） in the average well color development （AWCD） obtained by the BIOLOG Eco plate assay, Shannon-Weaver index （H） and Simpson index （λ） compared with the controls, implying that this strategy at least partially restored the microbiological functioning of the PAH-contaminated soil. The results suggest that MCD-aided bioaugmentation by Paracoccus sp. strain HPD-2 may be a promising practical bioremediation strategy for aged PAH-contaminated soils.
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 work is supported by National Natural Science Foundation of China （No. 30160092） TRAP0YT and Yunnan Province＇s Natural Science Foundation.
文摘Enantioseparation of aminoglutethimide was performed by high-speed counter-current chromatography with a two-phase system composed of ethyl acetate： methanol： water = 10： 1： 9. The lower phase contained 20 mmol/L of carboxymethly-β-cyclodextrin as chiral selector. The enantiomers were separated in 1.2 h and identified by chiral HPLC. This method was very efficient for the chiral preparative separation.
文摘used－silical capillary columns containing heptakis（2、3、6－tri－o－pentyl）-β-cyclodextrinand dibenzo-18-crown-6 were prepared．By studying the selectivity of mixed stationary phases forsome solute pairs.as well as comparing with the heptakis（2．3、6-tri-O-pentyl）-β-cyclodextrin and thedibenzo-18-crown-6 used as individual stationary phase、the synergistic effects were observed.These effects were affected by the column temperature．mixed ratio and linear velocity of carrier gas．
文摘A cationic cyclodextrin derivative 6-O-（hydroxypropyltrimethylammonia）-β-cyclodextrin （GTA-β-CD） with low degree of substitution was prepared through a convenient method in solid phase. The product could be used as a valuable chiral selector in the capillary electrophoresis （CE） separation of some acidic drug enantiomers such as naproxen, ofloxacin, ibuprofen and warfarin.
文摘Sulfobutylether－β－cyclodextrin（SBE－β－CD）was used as a chiral selector tor separatingten chlral drugs with resolution 1．2 by capillary zone electrophoresls（CZE）， The backgroundelectrolylc solution comprised of 120 mmol／L Britton－Robinson buffer（BRB） containing1 ～10mmol／L SBE－β－CD with the pH value adjusted from 5．0－6．8． Five of the drugs were better resolvedthan those previously reported with neutral CDs．
基金the Natural Science Foundation of Shanxi(No.2007011027)
文摘The inclusion interaction between three types of methylated-β-cyclodextrins （Me-β-CDs） and albendazole （ABZ） was studied by spectrofluorimetry. The result showed that Me-β-CDs reacted with ABZ to form an inclusion complex, 1： 1 stoichiometry for Me- β-CDs-ABZ complex was established and its association constant have been determined from fluorescence data by Benesi- Hildebrand＇s method （double reciprocal plots）. It was noted that 2,6-DM-β-CD exhibited stronger binding ability than other Me-β- CDs. Based on the significant enhancement of fluorescence intensity of inclusion complex, a simple and highly sensitive fluorimetric method is proposed for the determination of ABZ in the presence of 2,6-DM-β-CD. The proposed method was successfully applied to the determination of ABZ in tablets and human urine.
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.
文摘A chiral stationary phase （CSP） was prepared by chemically bonding carboxymethyl-β-cyclodextrin （CM- β-CD） onto 3-aminopropyl silica gel through amidation reaction in water solution and was characterized by Fourier transform infrared spectroscopy （FT-IR）, element analysis （EA） and thermal gravimetry analysis （TGA）. The chromatographic performance was evaluated with 24 racemates under reversedphase conditions, The effect of salt, organic modifier, mobile phase pH and structures of analytes were discussed. In comparison with native β-CD bonded column, CYCLOBOND 12000, CM-β-CD CSP exhibited enhanced enantioseparation.
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National Key Research and Development Program of China (Grant No. 2019YFA0904800)Science and Technology Commission of Shanghai Municipality (Grant No. 11DZ2260600 and 10DZ2220500)Shanghai Natural Science Fund (Grant No. 20ZR1414700)。
文摘Stimuli-responsive drug delivery systems based on polymeric micelles can achieve controlled drug release to improve the therapeutic outcome and reduce unwanted systematic toxicity and side effects of the cytotoxic drug in chemotherapy but often face challenging synthesis and purification of functionalized biocompatible polymer materials and low drug loading efficiency. In the present study, we reported a novel redox-responsive self-assembly polymeric micelle system, mPEG-β-CD/Ad-SS-CPT, to achieve high loading efficiency and selective delivery of camptothecin(CPT) in a reductive environment inside cancer cells. The host-vip supramolecular micelles utilized a simple β-CD modified PEG, mPEG-β-cyclodextrin(mPEG-β-CD), as the polymeric host with the ease of synthesis and purification. The vip prodrug Ad-SS-CPT contained the disulfide bond as the redox sensitivity group. The selective cleavage of disulfide bond and subsequent drug release in a reductive environment could potentially reduce system toxicity and improve the therapeutic outcome of CPT. In vitro studies showed that the micelles exhibited excellent cytotoxicity against He La cells comparable to the free drug. The host-vip polymeric micelles also showed great potentials for multi-drug co-delivery. Collectively, our current findings provided a general and convenient approach to design drug delivery systems based on stimuli-responsive polymeric micelles for disease treatment.
文摘Capillary column preparation using perpentylated (2,3,6-tri-O-pentyl)-β-cyclodextrin asstationary phase by sol-gel technology with simplicity and rapidity is described. Multiplepreparation steps in conventional column technology were avoided. The prepared columns exhibitsatisfactory chromatographic performances and pronounced selectivity for a wide range of testsolutes, and have been successfully used for the separation of nitrotoluene, dimethoxybenzene,alcohols, alkanes, dimethylphenol and cresol isomers.
文摘Heptakis(2, 3, 6-tri-O-octyl)-β-cyclodextrin was coated onto the fused silica capillary by sol-gel technology. Column efficiency and column selectivity were studied. The results indicated that high ability of separation was acquired . Positional isomers of aromatic compounds were well separated.
文摘Heptakis(2.6-di-O-pentyl-3-O-ally)-β-cyclodextrin as an excellent gas chromatographic stationary phase separating phenol and cresol isomers is described.
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.
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.
文摘Four basic drugs were separated by capillary electrophoresis (CE) usingcarboxymethyl-β-yclodextrin (CM-0-CD) as chiral selector. The effects of CM-β-CDconmptration, applied voltage. operation temperature were investigated. Under the selectedconditions. norephedrine. ofloxacin. terbutaline and chlorpheniramine were enantiomerallybaieline-separated using H3PO4-triethanolamine buffer at PH 3 containing 10, 5.5, 2. 2mmol/LCM-β-CD respectively.
