1.Analysis of the characteristics of pulse pressure index in elderly men with hypertension
Yanran LI ; Yajie ZHAO ; Cuiyan JIN
Chinese Journal of Geriatric Heart Brain and Vessel Diseases 2009;11(8):578-580
Objective To analyze the characteristics of pulse pressure index(PPI) and its value in predicting the risk for cerebral and cardiac vascular events in old males with hypertension. Meth-ods The 24-hours ambulatory blood pressure monitoring was performed in a total of 265 elderly men with essential hypertension(EH). The patients were classified into 3 groups based on the lev-el of PPI.PPI≤0.400(103) ,0. 401-0. 500(124) ,and≥0.501(38). Results There was significant difference in PP between day-time and night-time in hypertensive patients. The change of PPI was less than that of PP. With the increase in PPI, SBP(24 h, day-time, night-time), PP(24 h, day-time, night-time), the load of SBP(night-time), systolic blood pressure variation(BPV, 24 h, day-time) were raised significantly (P<0.01); while DBP(24 h, day-time, night-time), nocturnal de-cline in BP and the load of DBP(day-time) declined with the decrease in PPI (P<0.01). High PPI would increase the incidence of cardiac-cerebral vascular events (P < 0.01). Conclusion PPI is a useful parameter in clinical evaluation of arteriosclerosis. It may also have prognostic value for cardiac-cerebral vascular events in elderly men with EH.
2.Preparation of Salinomycin Nanostructured Lipid Carriers and Formulation Optimization
Cuiyan HAN ; Shanshan JIN ; Xiaoli WANG ; Baiyu JIAN ; Xiaoyu SUI ; Lixin CAO
China Pharmacy 2018;29(3):317-321
OBJECTIVE: To prepare Salinomycin nanostructured lipid carriers (Sal-NLCs) and optimize its formulation. METHODS: Sal-NLCs was prepared by emulsion evaporation-low temperature solidification method. Using particle size, Zeta potential, encapsulation efficiency and drug loading as evaluation indexes, central composite design-response surface methodology was used to optimize the amount of Sal, the ratio of solid lipid glyceryl bisstearate to liquid lipid glyceryl octanoate in oil phase, ratio of surface active agent polyoxyethylene 35 castor oil (EL) to polyethylene glycol-15-hydroxy stearate (HS 15), the amount of polyoxyethylene (40) stearate (P40). The morphology, particle size, polydispersity index (PDI), Zeta potential, encapsulation efficiency, drug loading and in vitro release mechanism of Sal-NLCs were investigated. RESULTS: The optimal prescription was as follows as Sal 0. 86 mg, glyceryl bisstearate 40.70 mg, glyceryl octanoate 11.30 mg, EL 44.05 mg, HS15 7.95 mg, P40 3.8 mg. Prepared Sal-NLCs was round-like and dispersed evenly. The particle size, PDI, Zeta potential, encapsulation efficiency and drug loading of prepared Sal-NLCs were(81.81 ± 2.60) nm, 0.183 ± 0.042, (-24.9 ± 3.4) mV,(94.35 ± 1.50)% and (1.47 ±0.04)% (n=5), respectively.24 h accumulative release rate was (99.81 ± 3.90)% (n=3).Drug release behavior was in line with Higuchi model, and relative error of particle size, Zeta-potential, encapsulation efficiency and drug loading to predicted value of model were all lower than 4%. CONCLUSIONS: Sal-NLCs with sustained-release effect is prepared successfully according to optimized formulation, and its quality meets the expected standard.
3.Preparation of Small Peptide AEYLR Modified Paclitaxel Nanostructured Lipid Carriers and Evaluation of Its Anti-tumor Effects
Cuiyan HAN ; Jianwen ZHOU ; Chang LIU ; Xiaoxing MA ; Cheng YUAN ; Yan DONG ; Shanshan JIN
China Pharmacy 2019;30(6):770-775
OBJECTIVE: To prepare Paclitaxel(PTX)nanostructured lipid carriers (NLC) modified by small peptide alanine-glutamic acid-tyrosine-leucine-arginine (AEYLR), and to evaluate its anti-tumor effect in vitro and in vivo. METHODS: NLC, PTX-NLC (P-NLC) and AEYLR modified P-NLC (A-P-NLC) were prepared by emulsion evaporation-low temperature solidification curing method. Its appearance, particle size, multi-dispersion index(PDI) and Zeta potential were characterized,encapsulation rate,drug loading and in vitro drug release were detected respectively. Using NCI-H1299 and S180 cells as objects, CCK-8 method was adopted to investigate inhibitory effects of free PTX, P-NLC and A-P-NLC (0.44-44.00 μg/mL, by PTX) to those cells. The half inhibition concentration (IC50) was calculated. Using S180 tumor-bearing mice as model animal, anti-tumor effects of free PTX, P-NLC and A-P-NLC (5 mg/kg, by PTX) were evaluated. RESULTS: P-NLC and A-P-NLC were round-like and dispersed evenly. The particle size, PDI and Zeta potential of A-P-NLC were (43.92±0.76) nm, 0.203±0.034 and (-19.77±1.16) mV, which were all increased to certain extent, compared with P-NLC. The encapsulation efficiency and drug loading of A-P-NLC were (95.71±0.68)% and(1.97±0.25)%, which were both decreased to certain extent, compared with P-NLC. The cumulative release rate of A-P-NLC was(35.17±2.08)% within 48 h, showing significant sustained-release effect compared with free PTX; the release of A-P-NLC was slower than P-NLC. Compared with free PTX and P-NLC, inhibitory rates of same concentration of A-P-NLC to NCI-H1299 cells and S180 cells were almost increased significantly, while IC50 values were all decreased significantly. There was no death in S180 tumor-bearing mice treated with A-P-NLC and the general condition was good; the volume of tumors was significantly reduced, the mass of tumors was significantly reduced, and the inhibition rate of tumors was significantly increased (P<0.05 or P<0.01). CONCLUSIONS: A-P-NLC has significantly sustained-release effects; its inhibitory rate to NCI-H1299 cells and S180 cells in vitro, and its inhibitory effects on S180 solid tumor in mice are all better than free PTX and P-NLC, while the toxicity is decreased to certain extent.