The purpose of this study was to investigate the effect of ionization of drug on drug solubilization in SMEDDS(self-microemulsifying drug delivery system) prepared using Capmul MCM and caprylic acid. Solubilization ca...The purpose of this study was to investigate the effect of ionization of drug on drug solubilization in SMEDDS(self-microemulsifying drug delivery system) prepared using Capmul MCM and caprylic acid. Solubilization capacity of blank SMEDDS dispersions for danazol,indomethacin and haloperidol as model drugs was determined. Based on the outcomes of solubilization capacity study, drug-loaded SMEDDS formulations were prepared and subjected to dispersion/precipitation study and droplet size analysis. Blank SMEDDS dispersions exhibited the highest solubilization capacity for haloperidol followed by indomethacin and danazol. Furthermore, the solubilization of the three drugs in blank SMEDDS dispersions was explained by a modified mathematical model. Dispersion/precipitation studies indicate that drug-loaded SMEDDS formulations exhibited superiority in solubilizing the drugs in comparison to their respective drug powder. In addition, indomethacin and haloperidol were found to reduce the droplet size of the microemulsions while danazol did not affect droplet size formation for drug-loaded SMEDDS formulations. These findings suggest that ionization of drug affects drug solubilization, droplet size formation, drug loading and drug dispersion/precipitation profiles for the SMEDDS formulations.展开更多
Objective This study aimed to investigate the effects of caprylic acid(C8:0)on lipid metabolism and inflammation,and examine the mechanisms underlying these effects in mice and cells.Methods Fifty-six 6-week-old male ...Objective This study aimed to investigate the effects of caprylic acid(C8:0)on lipid metabolism and inflammation,and examine the mechanisms underlying these effects in mice and cells.Methods Fifty-six 6-week-old male C57BL/6J mice were randomly allocated to four groups fed a highfat diet(HFD)without or with 2%C8:0,palmitic acid(C16:0)or eicosapentaenoic acid(EPA).RAW246.7 cells were randomly divided into five groups:normal,lipopolysaccharide(LPS),LPS+C8:0,LPS+EPA and LPS+cAMP.The serum lipid profiles,inflammatory biomolecules,and ABCA1 and JAK2/STAT3 mRNA and protein expression were measured.Results C8:0 decreased TC and LDL-C,and increased the HDL-C/LDL-C ratio after injection of LPS.Without LPS,it decreased TC in mice(P<0.05).Moreover,C8:0 decreased the inflammatory response after LPS treatment in both mice and cells(P<0.05).Mechanistic investigations in C57BL/6J mouse aortas after injection of LPS indicated that C8:0 resulted in higher ABCA1 and JAK2/STAT3 expression than that with HFD,C16:0 and EPA,and resulted in lower TNF-α,NF-κB mRNA expression than that with HFD(P<0.05).In RAW 264.7 cells,C8:0 resulted in lower expression of pNF-κBP65 than that in the LPS group,and higher protein expression of ABCA1,p-JAK2 and p-STAT3 than that in the LPS and LPS+cAMP groups(P<0.05).Conclusion Our studies demonstrated that C8:0 may play an important role in lipid metabolism and the inflammatory response,and the mechanism may be associated with ABCA1 and the p-JAK2/p-STAT3 signaling pathway.展开更多
Photoluminescent semiconductor nanocrystals or quantum dots(QDs)are usually produced using expensive ligands and solvents at high temperature above 280◦C to ensure high-quality optical properties,particularly the phot...Photoluminescent semiconductor nanocrystals or quantum dots(QDs)are usually produced using expensive ligands and solvents at high temperature above 280◦C to ensure high-quality optical properties,particularly the photoluminescence of QDs.The reproducibility of highly stable photoluminescence in QD preparation,in most cases,varies depending on many effects,such as the ligand used and temperature.Here a facile preparation of photoluminescent semiconductor CdTe nanocrystals or quantum dots(QDs)is conducted in the presence of caprylic acid at moderate temperatures between 80–140◦C,which are much lower than the high temperatures used in conventional organic-phase preparation of CdTe QDs.The results show that the optical properties of CdTe QDs depend considerably on the reaction time,temperature and ligand used.展开更多
目的比较6种脂肪酸对高胆固醇血症小鼠体质量和血脂的影响。方法建立C57BL/6J小鼠高胆固醇血症模型,分别用含2%的辛酸(C8∶0)、癸酸(C10∶0)、油酸(C18∶1)、α-亚麻酸(C18∶3)、棕榈酸(C16∶0)和硬脂酸(C18∶0)高胆固醇饲料喂养12周,1...目的比较6种脂肪酸对高胆固醇血症小鼠体质量和血脂的影响。方法建立C57BL/6J小鼠高胆固醇血症模型,分别用含2%的辛酸(C8∶0)、癸酸(C10∶0)、油酸(C18∶1)、α-亚麻酸(C18∶3)、棕榈酸(C16∶0)和硬脂酸(C18∶0)高胆固醇饲料喂养12周,12周时检测血脂及脂蛋白相关指标。结果研究12周后各组小鼠体质量均显著增加,辛酸(C8∶0)、癸酸(C10∶0)、油酸(C18∶1)对控制体质量增加的作用较棕榈酸(C16∶0)和硬脂酸(C18∶0)差异显著(P<0.05);6种脂肪酸均显示出不同程度血总胆固醇(total cholesterol,TC)和低密度脂蛋白胆固醇(low density lipoprotein cholesterol,LDL-C)降低,高密度脂蛋白胆固醇(high density lipoprotein cholesterol,HDL-C)与低密度脂蛋白胆固醇比值(HDL-C/LDL-C)增加的作用。辛酸(C8∶0)、癸酸(C10∶0)和α-亚麻酸(C18∶3)降低TC和LDL-C及升高HDL-C/LDL-C比值的作用比油酸、棕榈酸和硬脂酸显著(P<0.05)。结论中链的饱和脂肪酸(saturated fatty acid,SFA)较长链的SFA降低小鼠体质量和血脂的作用显著。展开更多
基金St. John’s University for providing financial assistance
文摘The purpose of this study was to investigate the effect of ionization of drug on drug solubilization in SMEDDS(self-microemulsifying drug delivery system) prepared using Capmul MCM and caprylic acid. Solubilization capacity of blank SMEDDS dispersions for danazol,indomethacin and haloperidol as model drugs was determined. Based on the outcomes of solubilization capacity study, drug-loaded SMEDDS formulations were prepared and subjected to dispersion/precipitation study and droplet size analysis. Blank SMEDDS dispersions exhibited the highest solubilization capacity for haloperidol followed by indomethacin and danazol. Furthermore, the solubilization of the three drugs in blank SMEDDS dispersions was explained by a modified mathematical model. Dispersion/precipitation studies indicate that drug-loaded SMEDDS formulations exhibited superiority in solubilizing the drugs in comparison to their respective drug powder. In addition, indomethacin and haloperidol were found to reduce the droplet size of the microemulsions while danazol did not affect droplet size formation for drug-loaded SMEDDS formulations. These findings suggest that ionization of drug affects drug solubilization, droplet size formation, drug loading and drug dispersion/precipitation profiles for the SMEDDS formulations.
基金supported by the National Natural Science Fund of China[no.81703204].
文摘Objective This study aimed to investigate the effects of caprylic acid(C8:0)on lipid metabolism and inflammation,and examine the mechanisms underlying these effects in mice and cells.Methods Fifty-six 6-week-old male C57BL/6J mice were randomly allocated to four groups fed a highfat diet(HFD)without or with 2%C8:0,palmitic acid(C16:0)or eicosapentaenoic acid(EPA).RAW246.7 cells were randomly divided into five groups:normal,lipopolysaccharide(LPS),LPS+C8:0,LPS+EPA and LPS+cAMP.The serum lipid profiles,inflammatory biomolecules,and ABCA1 and JAK2/STAT3 mRNA and protein expression were measured.Results C8:0 decreased TC and LDL-C,and increased the HDL-C/LDL-C ratio after injection of LPS.Without LPS,it decreased TC in mice(P<0.05).Moreover,C8:0 decreased the inflammatory response after LPS treatment in both mice and cells(P<0.05).Mechanistic investigations in C57BL/6J mouse aortas after injection of LPS indicated that C8:0 resulted in higher ABCA1 and JAK2/STAT3 expression than that with HFD,C16:0 and EPA,and resulted in lower TNF-α,NF-κB mRNA expression than that with HFD(P<0.05).In RAW 264.7 cells,C8:0 resulted in lower expression of pNF-κBP65 than that in the LPS group,and higher protein expression of ABCA1,p-JAK2 and p-STAT3 than that in the LPS and LPS+cAMP groups(P<0.05).Conclusion Our studies demonstrated that C8:0 may play an important role in lipid metabolism and the inflammatory response,and the mechanism may be associated with ABCA1 and the p-JAK2/p-STAT3 signaling pathway.
基金supported by the initiating grant of HUST,the NSFC(20874025)the Fundamental Research Funds for the Central Universities,(HUST-2010MS101).
文摘Photoluminescent semiconductor nanocrystals or quantum dots(QDs)are usually produced using expensive ligands and solvents at high temperature above 280◦C to ensure high-quality optical properties,particularly the photoluminescence of QDs.The reproducibility of highly stable photoluminescence in QD preparation,in most cases,varies depending on many effects,such as the ligand used and temperature.Here a facile preparation of photoluminescent semiconductor CdTe nanocrystals or quantum dots(QDs)is conducted in the presence of caprylic acid at moderate temperatures between 80–140◦C,which are much lower than the high temperatures used in conventional organic-phase preparation of CdTe QDs.The results show that the optical properties of CdTe QDs depend considerably on the reaction time,temperature and ligand used.
文摘目的比较6种脂肪酸对高胆固醇血症小鼠体质量和血脂的影响。方法建立C57BL/6J小鼠高胆固醇血症模型,分别用含2%的辛酸(C8∶0)、癸酸(C10∶0)、油酸(C18∶1)、α-亚麻酸(C18∶3)、棕榈酸(C16∶0)和硬脂酸(C18∶0)高胆固醇饲料喂养12周,12周时检测血脂及脂蛋白相关指标。结果研究12周后各组小鼠体质量均显著增加,辛酸(C8∶0)、癸酸(C10∶0)、油酸(C18∶1)对控制体质量增加的作用较棕榈酸(C16∶0)和硬脂酸(C18∶0)差异显著(P<0.05);6种脂肪酸均显示出不同程度血总胆固醇(total cholesterol,TC)和低密度脂蛋白胆固醇(low density lipoprotein cholesterol,LDL-C)降低,高密度脂蛋白胆固醇(high density lipoprotein cholesterol,HDL-C)与低密度脂蛋白胆固醇比值(HDL-C/LDL-C)增加的作用。辛酸(C8∶0)、癸酸(C10∶0)和α-亚麻酸(C18∶3)降低TC和LDL-C及升高HDL-C/LDL-C比值的作用比油酸、棕榈酸和硬脂酸显著(P<0.05)。结论中链的饱和脂肪酸(saturated fatty acid,SFA)较长链的SFA降低小鼠体质量和血脂的作用显著。
