OBJECTIVE:To optimize the formulation and preparation technology of podophyllotoxin derivative(5-FPE) liposomes.METHODS:A thin film-ultrasonic dispersion method was used to prepare the 5-FPE liposomes.Orthogonal experiment was performed to optimize its best formulation and preparation technology with entrapment efficiency as the evaluation index;meanwhile,the entrapment efficiency,drug-loading amount,morphology,particle size distribution,Zeta electric potential and stabilities of the liposomes within 10 days' storing at 25 ℃ or 4 ℃ were investigated.RESULTS:The optimal formulation and prepariton technology of the liposomes has been established in our study.3 batches of liposomes prepared in the optimal conditions had a mean entrapment efficiency of 66.45%,a mean drug-loading amount of 7.97%,mean particle size of 284.7 nm and mean Zeta electric potential of-22.15 mV.The entrapment efficiency of the liposomes decreased more after storing for 10 days at 25 ℃ than at 4 ℃.CONCLUSION:The optimal formulation and preparation technology of 5-FPE liposomes are feasible and which serve as a basis for the further study of 5-FPE preparations.

With the development of drug discovery, more and more candidate compounds need to be studied. Methods that can screen compound rapidly received significant attention. Parallel artificial membrane permeability assay (PAMPA) as a powerful tool has been applied to drug studies. It uses an artificial lipid membrane to mimic the barrier for drug permeability studies. This article introduces the establishment and characteristics of PAMPA, as well as its applications in screening compounds. It can be used as models (e.g. predicting the ability of compound in gastro-intestinal absorption, blood-brain barrier transportation and skin penetration) by changing the component of artificial lipid membrane. PAMPA has advantages in high throughput selection of valuable compound with low cost, versatile, low dose, and good reproducibility.

Objective To evaluate the physical dependence of Zhixieling capsule.Methods The physical dependence of Zhixieling capsule was observed by mouse jump test,rat precipitation test and rat natural withdrawal test.Results Zhixieling capsule showed no obvious withdrawal symptoms.Conclusion Zhixieling capsule has no physical dependence.

The purpose of this study is to investigate the intracellular transporters effect and the cytotoxicity of carboxyl nanodiamond (CND) - podophyllotoxin (PPT). Nanodiamond (ND) was treated with mixed carboxylic acid and finally got 64 nm CND by centrifugation, and then it was reacted with PPT to form CND-PPT. UV spectrophotometry was used to calculate the content of PPT in CND-PPT, the particle size distribution and zeta potential were measured by Dynamic laser scattering instrument. CND, PPT, CND-PPT and CND + PPT (physical mixture of CND and PPT) were characterized by Fourier transform infrared spectroscopy, at the same time, thermal analysis and element analysis were used to estimate the content of the PPT in CND-PPT. The affect of CND, PPT, CND-PPT on HeLa cell was measured with MTT assay. The results showed that content of PPT combined with CND accounted for about 10%. MTT assay showed that CND has low cytotoxicity and CND-PPT can increase the water soluble of PPT. As a conclusion, CND as a hydrophilic pharmaceutical carrier combined with PPT is able to increase the water solubility of PPT, at low concentration, CND-PPT can enhance the antitumor activity in comparison with PPT, so CND can be used as a potential anticancer drug carrier.

Alpha-glucosidase inhibitor can reduce the postprandial hyperglycemia and have good effect on preventing and treating the diabetes and diabetic complication. Along with the application of acarbose which is a kind of alpha-glucosidase inhibitor, many research groups pay attention to the crude alpha-glucosidase inhibitor screened from the medicinal herbs in order to find new, safe, and effective medicine. The development of alpha-glucosidase inhibitor screened from the medicinal herbs and its evaluation in vivo and vitro as well as the varieties of the medicinal herbs that contain alpha-glucosidase inhibitor in recent 30 years were summarized in this paper.
Cell Line ; Drug Evaluation, Preclinical ; Enzyme Inhibitors ; isolation & purification ; pharmacology ; Glycoside Hydrolase Inhibitors ; Humans ; Plant Extracts ; isolation & purification ; pharmacology ; Plants, Medicinal ; chemistry