[Objective] To investigate the possibility of [poly(lactic-co-glycolic acid) ,PLGA] nanoparticles (NP) as a new kind of protein drug carrier for nasal administration. [Method] CNT-PLGA-NP was prepared by double emulsification solvent evaporation. Its morphology was examined by transmission electronmicroscope (TEM). In the use of photon correlation spectroscopy(PCS) and laser Doppler anemometry(LDA),its Zeta potential and mean particle size were estimated .Also, the entrapment efficiency of CNT-PLGA-NP and its pharmacokinetics in rats through nasal administration were studied. [Result] The Zeta potential, mean particle size, entrapment efficiency of CNT-PLGA-NP were-13.4mV, 320.20nm and 45% respectively .Its vitro CNT release from CNT-PLGA-NP appeared to consisting of two components with initial rapid release followed by a exponential stage.The AUC and t1/2(?) of CNT, CNT-PLGA-Np and CNT-PLGA-NP(B+T)were 1.14, 8.37, 7.12?g?h/mL and 20.06, 44.14, 34.82h respectively. [Conclusion]PLGA-NP might be a potential new drug carrier for CNT.Polysorbate 80 and borneol might be good absorption enhancers.

Objective To investigate the current situation of pharmaceutial research and influencing factors in primary hospitals located in Hangzhou Fuyang county.Methods A designed questionnaire was used collecting information from the pharmacists of six Fuyang city medical institutes.Results Among 156 valid questionnaires 54 (34.62％) pharmacists showed their interest in pharmaceutial research,however only 4 of them had the opportunity to participate or host such project.The top reason of interesting in research was that it would help in their job promotion and enhance their own value.We found that most of pharmacists thought that it is very difficulties to conduct research and it is not necessary to do so.The educational background was found to related with research interest with a statistical significance (P＜0.001);and the difference in accomplishment was statistically significant among pharmacists (P＜0.05).Conclusions Current status of research in primary hospital pharmacists is worrysome.The hospital administrators need to pay great attention to medical research,make efforts to develop and provide the excellent policy and technological platform to enhance the research activities of pharmacists.

[Objective] To prepare adriamycin self-assembled nanoparticles, and study the in vivo anti-tumor activity. [Methods]The self-assembled adri-amycin loaded cholesterol-modified pul ulan nanoparticles were prepared by dialysis and were characterized by morphology for particle size,Zeta potential, entrapment efficiency,drug loading content.They were incubated with U251 cel s to assess the inhibition ability of the self-assembled adriamycin-loaded cholesterol-modified pul ulan nanoparticles. [Results]The morphology of self-assembled adriamycin loaded cholesterol-modified pul ulan nanoparticles was spherical. The mean particle size, Zeta potential, entrapment efficiency and drug loading were (112.8 ±1.02)nm,(-27.2±0.246)mV,(67.14±1.21)% and (7.65±0.58)%, respectively.The profiles of release were expressed wel by Higuchi equation. When the dosages were 25μg·mL-1 plus, the inhibiton ability against U251 was stronger than adriamycin solution( P<0.01).[Conclusion]The self-assembled adriamycin loaded cholesterol-modified pul ulan nanoparticles exhibited more cycitoxic activity against U251 than adriamycin solution.

Aim To prepare NT-Ⅰ loaded nanoparticles with different diameters modified by Methylated-polyethyleneglycol (Me-PEG) and evaluate their brain pharmacokinetics after administered nasally in rats. Methods NT-Ⅰ-NP was prepared by emulsion/solvent evaporation method and MePEG-PLA was used as the carrier material. Microdialysis technique and fluorospectrophotometry were used to determine NT-Ⅰ concentration after nasal administration in the brain of rats. Results The appearance of all NT-Ⅰ-NP groups was round or similar. The AUC(0-t) of below 100 nm NT-Ⅰ-NP was 1.22 fold as that of 100~200 nm NT-Ⅰ-NP,1.34 fold as that of 200~300 nm and 1.60 fold as that of exceed 300 nm NT-Ⅰ-NP(P

AIM:To establish the quality standard for Shengxue Micro Capsules(melanteritum,Cortex Cinnamo-(mi,) Endoconcha Sepiae,Colla Corii asini,Placenta Hominis). METHODS: The melanteritum,Endoconcha sepiae was identified by physic-chemical analysis. Cortex Cinnamomi was identified by TLC.UV was employed for the assay of FeSO_4.GC was used to determine Cinnamaldehyde of Shengxue Micro Capsules. RESULTS: Green vitriol,Endoconcha sepiae could be identified by physico-chemical analysis.Cortex Cinnamomi could be identified by TLC.The linear range of FeSO_4 was within 0～20 mg,r = 0.999 8;The average recovery of assay was(96.7%.) The linear range of cinnamaldehyde was within 0.157 5～0.551 4 ?g,r = 0.999 8;The average(recovery) of assay was 101.52%. CONCLUSION: The method is simple, reproducible.It could be used for(quality) control of Shengxue Micro Capsules.

Objective To prepare the supersaturation self-emulsifying drug delivery system(S-SEDDS) containing silymarin and to evaluate its basic properties.Methods With the time of self-emulsifying,the consequence of color visual examination and particle size as parameters,the optimum formulations of silymarin SSEDDS were screened by solubility test,compatibility tests and pseudo ternary phase diagrams.The silymarin concentration was determined by HPLC.The in vitro dissolution characteristics of silymarin S-SEDDS were investigated with silymarin SEDDS as control.Results The optimum silymarin S-SEDDS was composed of medium chain triglycerides(MCT) 40%,Cremophor RH40(ethoxylated hydrogenatedcastor oil) 48%,Labrasol 12%.The time of self-emulsifying was less than 3 min,the average particle diameter was 49.6 nm,the adding amount of hydroxypropyl methylcellulose(HPMC) was 50 mg/g,and the average content of silymarin was 39.3 mg/g.The in vitro dissolution test of silymarin S-SEDDS showed that the presence of a small amount of cellulosic polymer effectively sustained a metastable supersaturated state by retarding precipitation kinetics.Conclusion The designed formulation of silymarin S-SEDDS is reasonable and provides a strong foundation for further development of new preparations.

Objective To prepare ligustrazine-chitosan microspheres and to investigate the drug release behavior in vitro. Methods Microspheres were prepared using the spray drying method.The encapsulation efficiency was used to evaluate the influence of different formulation and preparation factors,the formulation was optimized by L9(34) orthogonal design.Results The optimal formulation and preparation factors were as follows: chitosan concentration(0.01 g/mL),ratio of chitosan to ligustrazine(1∶4),inlet temperature(120 ℃),air flow rate(500 L/h).The optimized microspheres had a spherical shape,the loading capacity was(18.60?0.15)%,entrapment efficiency was(93.01?0.76)%,the average diameter was(10.69?0.64) ?m.The drug release profile in vitro could be described by Higuchi equation Q=19.798 t1/2+25.209(r=0.997) at 1-15 h,which showed the prepared microspheres obviously had the sustained release effect.Conclusion The encapsulation efficiency of ligustrazine-chitosan microspheres is higher,the preparation method is simple,and the process is stable.It will provide the basis for realizing the industrialization in Chinese materia medica microspheres.

Objective Fluctuation of glucose levels is more likely to cause oxidative stress which contributes to the development of insulin resistance through activating c-Jun N-terminal kinase (JNK).Such antio xidants as vitamin C or vitamin E do not appear very helpful.Radix Astragali (RA) is an herbal medicine with antioxidative ability.The study was to explore whether RA would lower the risk of insulin resistance in diabetic rats.Methods Diabetic rats received RA,insulin or both RA and insulin after diabetes were induced in male Wistar rats.Serum levels of interleukin 6 (IL-6) and tumor necrosis factor α (TNFα),advanced glycation endproducts(AGEs) levels in kidney,the expression of insulin receptor (IR),insulin receptor substrate 1 (IRS-1),p38 mitogen-activated protein kinase (MAPK),p-p38 MAPK,p-JNK,p-IRS-1 Ser307,and p-IRS-1 Tyr612 in skeletal muscles were determined.Results Compared to diabetic rats treated with insulin,the diabetic rats treated with both insulin and RA demonstrated significantly lower levels of IL-6,TNF-α and AGEs (P ＜ 0.05),significantly lower activation of p-p38 MAPK and JNK (P ＜0.05),significantly higher expressions of IRS-1 (P ＜0.05),p-IRS-1 Tyr612,and significantly lower expression of p-IRS-1 Ser307 (P ＜ 0.05).Conclusions RA can lower the risk of insulin resistance through fighting oxidative stress in diabetic rats.

This study was aimed at the transport across blood-brain barrier (BBB) of polysorbate-80 modified neurotoxin loaded polybutylcyanoacrylate nanoparticle (P-80-NT-NP) and its cytotoxicity. An in vitro model of BBB using rat brain microvascular endothelial cells (rBMECs) was established. The cytotoxicity of P-80-NT-NP was measured by the MTT assays, where neurotoxin (NT), nanoparticle (NP), neurotoxin nanoparticle (NT-NP) as control, and the permeability of P-80-NT-NP was determined by using of Millicell insert coculture with rBMECs and fluorescence spectrophotometry. MTT results showed that NT, NP, NT-NP and P-80-NT-NP were avirulent to rBMECs when the concentration of NT was lower than 200 ng x mL(-1). But the cytotoxicity of NP, NT-NP and P-80-NT-NP would be augmented accordingly as concentration increased (P < 0.01), causing obvious reductions of cell survival rate, with no significant difference between them (P > 0.05). When the concentration of NT was 150 ng x mL(-1), the permeability on rBMECs of P-80-NT-NP and NT-NP were both significantly higher than that of NT (P < 0.01), and the permeability of P-80-NT-NP was greater than that of NT-NP (P < 0.05). In conclusion, polysorbate-80 modified neurotoxin nanoparticles can transport across the BBB, while concentration of NT is greater than 200 ng x mL(-1), P-80-NT-NP has a little cytotoxicity against rBMECs.

A novel targeting drug carrier (FA-BO-PAMAM) based on the PAMAM G5 dendrimer modified with borneol (BO) and folic acid (FA) molecules on the periphery and doxorubicin (DOX) loaded in the interior was designed and prepared to achieve the purposes of enhancing the blood-brain barrier (BBB) transportation and improving the drug accumulation in the glioma cells. 1H NMR was used to confirm the synthesis of FA-BO-PAMAM; its morphology and mean size were analyzed by dynamic light scattering (DLS) and transmission electron microscope (TEM). Based on the HBMEC and C6 cells, cytotoxicity assay, transport across the BBB, cellular uptake and anti-tumor activity in vitro were investigated to evaluate the properties of nanocarriers in vitro. The results showed that the nanocarrier of FA-BO-PAMAM was successfully synthesized, which was spherical in morphology with the average size of (22.28 ± 0.42) nm, and zeta potential of (7.6 ± 0.89) mV. Cytotoxicity and transport across the BBB assay showed that BO-modified conjugates decreased the cytotoxicity of PAMAM against both HBMEC and C6 cells and exhibited higher BBB transportation ability than BO-unmodified conjugates; moreover, modification with FA increased the total uptake of DOX by C6 cells and enhanced the cytotoxicity of DOX-polymer against C6 cells. Therefore, FA-BO-PAMAM is a promising nanodrug delivery system in employing PAMAM as a drug carrier and treatment for brain glioma.