Formulation Optimization and Quality Evaluation of Ferulic Acid Ligustrazine Solid Lipid Nanoparticles / 中国药房

OBJECTIVE:To optimize the formulation of ferulic acid ligustrazine (FATM) solid lipid nanoparticles (FATM-SLN),and conduct the quality evaluation. METHODS:Emulsification ultrasonic method was used to prepare FATM-SLN. Using particle size and entrapment efficiency as indexes,amount of glyceryl monostearate,egg yolk lecithin (PC),poloxamer 188 (P188),and sodium stearate as factors,single factor test and orthogonal test were used to optimize the formulation;and verifica-tion test was conducted. The appearance morphology,distribution of particle size,Zeta potential,stability and in vitro release de-gree of prepared FATM-SLN were investigated. RESULTS:The optimal formulation was as follows as FATM of 10 mg,glyceryl monostearate of 300 mg,PC of 200 mg,P188 of 200 mg,sodium stearate of 10 mg,and purified water of 20 mL. The prepared FATM-SLN showed spherical solid particles,appearance morphology was round,distribution of particle size was 40-800 nm,parti-cle size was 106.23 nm,polydispersity index was 0.254,Zeta potential was -34.8 mV,entrapment efficiency was 73.32%,drug loading was 1.20%;the appearance had no obvious changes within 10 d in 4 ℃(RSD<2%). The drug-release in 0.5-1 h was the fastest,the cumulative release degree reached to 60.47%;it tended to be stable after 8 h,the cumulative release degree reached to 93.46%,and drugs were basically released completely. CONCLUSIONS:FATM-SLN formulation is successfully optimized,and the prepared FATM-SLN has small particle size,high entrapment efficiency and good stability.

Carboxyl nanodiamond as intracellular transporters of anticancer drug--podophyllotoxin / 药学学报

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.

Biodistribution of co-exposure to multi-walled carbon nanotubes and nanodiamonds in mice.

In this work, technetium-99 (99mTc) was used as the radiolabeling isotope to study the biodistribution of oxidized multi-walled carbon nanotubes (oMWCNTs) and/or nanodiamonds (NDs) in mice after intravenous administration. The histological impact of non-radiolabeled oMWCNTs or NDs was investigated in comparison to the co-exposure groups. 99mTc-labeled nanomaterials had high stability in vivo and fast clearance from blood. After a single injection of oMWCNTs, the highest distribution was found in the lungs, with lower uptake in the liver/spleen. As for NDs injected alone, high distribution in the liver, spleen, and lungs was observed right after. However, uptake in the lungs was decreased obviously after 24 h, while high accumulation in the liver or spleen continued. After co-injection of oMWCNTs and NDs, oMWCNTs significantly affected the distribution pattern of NDs in vivo. Meanwhile, the increasing dose of oMWCNTs decreased the hepatic and splenic accumulation of NDs and gradually increased lung retention. On the contrary, the NDs had no significant effects on the distribution of oMWCNTs in mice. Histological photographs showed that oMWCNTs were mainly captured by lung macrophages, and NDs were located in the bronchi and alveoli after co-administration. oMWCNTs and NDs had different modes of micro-cells. In conclusion, the behavior and fate of NDs in mice depended strongly on oMWCNTs, but NDs had a small influence on the biodistribution and excretion pattern of oMWCNTs.