Hydroxypropyl chitosan(HP-chitosan) has been shown to have promising applications in a wide range of areas due to its biocompatibility, biodegradability and various biological activities, especially in the biomedical ...Hydroxypropyl chitosan(HP-chitosan) has been shown to have promising applications in a wide range of areas due to its biocompatibility, biodegradability and various biological activities, especially in the biomedical and pharmaceutical fields. However, it is not yet known about its pharmacokinetics and biodegradation performance, which are crucial for its clinical applications. In order to lay a foundation for its further applications and exploitations, here we carried out fluorescence intensity and GPC analyses to determine the pharmacokinetics mode of fluorescein isothiocyanate-labeled HP-chitosan(FITC-HP-chitosan) and its biodegradability. The results showed that after intraperitoneal administration at a dose of 10 mg per rat, FITC-HP-chitosan could be absorbed rapidly and distributed to liver, kidney and spleen through blood. It was indicated that FITC-HP-chitosan could be utilized effectively, and 88.47% of the FITC-HP-chitosan could be excreted by urine within 11 days with a molecular weight less than 10 k Da. Moreover, our data indicated that there was an obvious degradation process occurred in liver(< 10 k Da at 24 h). In summary, HP-chitosan has excellent bioavailability and biodegradability, suggesting the potential applications of hydroxypropyl-modified chitosan as materials in drug delivery, tissue engineering and biomedical area.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
采用壳聚糖(CS)、羟丙基甲基纤维素(HPMC)为原料制备了温敏性水凝胶,分析了CS含量、HPMC含量、HPMC黏度和甘油添加量对CS/HPMC的低临界溶解温度的影响。最优条件为CS含量为1%(m/V),HPMC的黏度为6 m Pa·s,HPMC的含量为7%(m/V),甘油...采用壳聚糖(CS)、羟丙基甲基纤维素(HPMC)为原料制备了温敏性水凝胶,分析了CS含量、HPMC含量、HPMC黏度和甘油添加量对CS/HPMC的低临界溶解温度的影响。最优条件为CS含量为1%(m/V),HPMC的黏度为6 m Pa·s,HPMC的含量为7%(m/V),甘油含量为32%(m/V),得到体系的低临界溶解温度为32℃,体系的黏度为1407 m Pa·s。红外光谱测试表明CS、HPMC与甘油之间没有化学作用,流变性测试显示体系可以在36℃下凝胶化。MTT测试结果表明CS/HPMC/Gyl无毒副作用,具有良好的生物相容性。研究结果表明该体系是一种良好的可注射型温敏水凝胶。展开更多
提出以醇洗酮沉脱碱法纯化羟丙基壳聚糖(HPCS),并用FT-IR、1 H NMR谱图和元素分析法的数据与常用的酸中和法相比较。结果表明:该法简便、高效,明显优于酸中和法。由于酸中和法的中和终点较难把握,所得HPCS中极易含有极微量的残留酸而生...提出以醇洗酮沉脱碱法纯化羟丙基壳聚糖(HPCS),并用FT-IR、1 H NMR谱图和元素分析法的数据与常用的酸中和法相比较。结果表明:该法简便、高效,明显优于酸中和法。由于酸中和法的中和终点较难把握,所得HPCS中极易含有极微量的残留酸而生成—NH+3,从而造成HPCS吸水性的大幅度提高。该结构变化可明显体现在FT-IR谱图中,而对1 H NMR谱图和元素分析结果无影响,仍可用后两种方法测定其取代度。展开更多
基金financially supported by National High Technology Research and Development Program of China(863 Program,Grant No.2007AA091603)
文摘Hydroxypropyl chitosan(HP-chitosan) has been shown to have promising applications in a wide range of areas due to its biocompatibility, biodegradability and various biological activities, especially in the biomedical and pharmaceutical fields. However, it is not yet known about its pharmacokinetics and biodegradation performance, which are crucial for its clinical applications. In order to lay a foundation for its further applications and exploitations, here we carried out fluorescence intensity and GPC analyses to determine the pharmacokinetics mode of fluorescein isothiocyanate-labeled HP-chitosan(FITC-HP-chitosan) and its biodegradability. The results showed that after intraperitoneal administration at a dose of 10 mg per rat, FITC-HP-chitosan could be absorbed rapidly and distributed to liver, kidney and spleen through blood. It was indicated that FITC-HP-chitosan could be utilized effectively, and 88.47% of the FITC-HP-chitosan could be excreted by urine within 11 days with a molecular weight less than 10 k Da. Moreover, our data indicated that there was an obvious degradation process occurred in liver(< 10 k Da at 24 h). In summary, HP-chitosan has excellent bioavailability and biodegradability, suggesting the potential applications of hydroxypropyl-modified chitosan as materials in drug delivery, tissue engineering and biomedical area.
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.
文摘采用壳聚糖(CS)、羟丙基甲基纤维素(HPMC)为原料制备了温敏性水凝胶,分析了CS含量、HPMC含量、HPMC黏度和甘油添加量对CS/HPMC的低临界溶解温度的影响。最优条件为CS含量为1%(m/V),HPMC的黏度为6 m Pa·s,HPMC的含量为7%(m/V),甘油含量为32%(m/V),得到体系的低临界溶解温度为32℃,体系的黏度为1407 m Pa·s。红外光谱测试表明CS、HPMC与甘油之间没有化学作用,流变性测试显示体系可以在36℃下凝胶化。MTT测试结果表明CS/HPMC/Gyl无毒副作用,具有良好的生物相容性。研究结果表明该体系是一种良好的可注射型温敏水凝胶。
文摘提出以醇洗酮沉脱碱法纯化羟丙基壳聚糖(HPCS),并用FT-IR、1 H NMR谱图和元素分析法的数据与常用的酸中和法相比较。结果表明:该法简便、高效,明显优于酸中和法。由于酸中和法的中和终点较难把握,所得HPCS中极易含有极微量的残留酸而生成—NH+3,从而造成HPCS吸水性的大幅度提高。该结构变化可明显体现在FT-IR谱图中,而对1 H NMR谱图和元素分析结果无影响,仍可用后两种方法测定其取代度。
