Vinflunine tartrate-loaded liposomes (VT-L) with two drug-to-lipid ratios were prepared by pH gradient method. Vesicle size and zeta potential were determined by the Zetasizer Nano ZS. Entrapment efficiency was evaluated by cation exchange resin centrifugalization method. The toxicity and tumor inhibition to nude mouse administrated by VT-L with different drug-to-lipid ratios were investigated and compared with the vinflunine tartrate injection (VT-I). The results showed that the mean particle size, zeta potential and entrapment efficiency of the VT-L with drug-to-lipid ratios of 1 : 5 and 1 : 10 were 124.6 nm and 128.3 nm, -25.3 mV and -22.8 mV, 94.46% and 97.31%, respectively. The VT-L with two different drug-to-lipid ratios has significantly higher anti-tumor effect to nude mouse transplanted human non-small cell lung carcinoma A549 and lower toxicity than VT-I. While there were no significant differences in anti-tumor effect and toxicity between VT-L with two different drug-to-lipid ratios.

For the purpose of preparing the ondansetron hydrochloride sustained-release tablets and studying the influencing factors, we prepared the ondansetron hydrochloride sustained-release tablets, using hydroxypropylmethylcellose (HPMC) as the matrix material. Then we investigated the effects of the viscosity and amount of HPMC,the sort of fillers, the preparation methods, the alcohol content in adhesives, and the pH of the dissolving solution on the release of ondansetron hydrochloride from sustained-release tablets. On the basis of pharmaceutical preformulation studies,the best formulation and preparation methods were screened out according to orthogonal experiment design method. The release behavior of the tablets followed the Higuchi equation. The viscosity of HPMC,the sort of fillers and the rotation speed had no significant effects on the release of ondansetron hydrochloride sustained-release tablets,while the preparation methods, the alcohol content in adhesives and the pH of the dissolving solution influcenced the release of ondansetron hydrochloride sustained-release tablets significantly. Ondansetron hydrochloride sustained-release tablets had good drug relase behavior for in 12 h in vitro.
Delayed-Action Preparations ; Lactose ; analogs & derivatives ; chemistry ; Methylcellulose ; analogs & derivatives ; chemistry ; Models, Chemical ; Ondansetron ; administration & dosage ; chemistry ; Pharmaceutical Preparations ; chemistry ; Tablets ; Viscosity

Objective To investigate the expression of hypoxia-inducible factor-1α(HIF-1α),matrix metalloprotein-ase(MMP)-1 and MMP-2 in the serum of patients with diabetic retinopathy(DR),and to analyze their relationship with the stage of DR and angiogenesis.Methods A total of 280 patients with type 2 diabetes mellitus(T2DM)and no DR who were hospitalized in our hospital from December 2020 to December 2021 were selected as the T2DM group;276 DR patients who were hospitalized in the ophthalmology department of our hospital during the same period were selected as the DR group;another 282 healthy subjects who underwent physical examination in our hospital were selected as the normal group.There were no significant differences in gender and age distribution among the normal group,T2DM group and DR group(both P＞0.05).According to the results of fundus examination and fluorescein angiography,the patients in the DR group were divided into non-proliferative diabetic retinopathy(NPDR)group(129 patients)and proliferative diabetic reti-nopathy(PDR)group(147 patients).The fasting plasma glucose(FPG),glycosylated hemoglobin(HbA1c)and serum HIF-1 α,MMP-1,MMP-2 levels of subjects in the normal group,T2DM group and DR group,as well as NPDR group and PDR group were compared.The serum basic fibroblast growth factor(bFGF),angiopoietin-1(Ang-1)and vascular endo-thelial growth factor(VEGF)levels of subjects in the normal group,T2DM group and DR group,as well as NPDR group and PDR group were compared.Pearson correlation analysis was used to analyze the correlation between serum HIF-1α,MMP-1,MMP-2 and bFGF,Ang-1,VEGF levels in DR patients.Results The FPG,HbA1c and serum HIF-1α,MMP-1,MMP-2 levels of the T2DM group and DR group were higher than those of the normal group,and the differences were statis-tically significant(all P＜0.05).The serum HIF-1α,MMP-1 and MMP-2 levels of the DR group were significantly higher than those of the T2DM group(all P＜0.05);there were no significant differences in FPG and HbA1 c between the two groups(both P＞0.05).The serum HIF-1α,MMP-1 and MMP-2 levels of the PDR group were significantly higher than those of the NPDR group(all P＜0.05);there were no significant differences in FPG and HbA1c between the two groups(both P＞0.05).The serum bFGF,Ang-1 and VEGF levels of the T2DM group and DR group were higher than those of the normal group,and the differences were statistically significant(all P＜0.05).The serum bFGF,Ang-1 and VEGF levels of the DR group were significantly higher than those of the T2DM group(all P＜0.05).The serum bFGF,Ang-1 and VEGF levels of the PDR group were significantly higher than those of the NPDR group(all P＜0.05).Pearson correlation analysis showed that HIF-1α,MMP-1 and MMP-2 were positively correlated with bFGF,Ang-1 and VEGF levels in DR patients(all P＜0.05).Conclusion The serum HIF-1α,MMP-1 and MMP-2 levels of DR patients are abnormally elevated,and are closely related to the progression of DR and angiogenesis.These parameters can be used to predict the disease development trend and guide clinical intervention.