Application Advantages of Nanoemulsion in Field of Traditional Chinese Medicine Preparation：A Review / 中国实验方剂学杂志

As a new technology with unique drug delivery advantages， nanoemulsion has been widely used in the field of traditional Chinese medicine （TCM） preparations. By searching， classifying and sorting out the literature reports at home and abroad in recent years， this paper systematically expounded the application advantages and production mechanism of nanoemulsion in delivering effective components of TCM from three aspects of improving oral bioavailability， enhancing targeting effect and delaying drug release. The current formulation optimization strategies， preparation processes and quality evaluation indicators commonly used in TCM nanoemulsion were summarized. Based on the research status of TCM nanoemulsion with different active components， the common problems and possible solutions in the development of TCM nanoemulsion were discussed， and the future research hotspots and directions of TCM nanoemulsion were prospected. This article clarifies the feasibility of nanoemulsion for enriching the selection of TCM dosage forms， which can provide reference for the subsequent rational design and improvement of TCM preparations. At the same time， it is revealed that the research focus of TCM nanoemulsion in the future lies in the integrated research of TCM compounds， and shows a trend of multi-disciplinary joint and targeted research.

Pharmacokinetic study on five components in phthalide target areas of Chaxiong and its β-CD inclusion compounds based on UPLC-MS/MS / 中国中药杂志

This study aims to establish a method for the determination of the concentration of five main components of phthalide target areas of Chaxiong(CPTA) and its inclusion of β-CD in the plasma of rats, and determine the pharmacokinetic parameters, absolute bioavailability and relative bioavailability of CPTA/β-CD inclusion compound in vivo. The plasma concentrations of senkyunolide A, N-butylphthalide, new osthol lactone, Z-ligustilide and butenyl phthalide were determined with UPLC-MS/MS. The content determination was conducted at the chromatographic conditions as follows: Shim-pack GIST C_(18)-AQ HP column(2.1 mm×100 mm, 3 μm), mobile phase of 0.1% formic acid solution(A)-acetonitrile(B), gradient elution, flow rate of 0.3 mL·min~(-1), column temperature of 35 ℃ and injection volume of 2 μL. The mass spectra were obtained with electrospray ion source(ESI), positive ion mode and multi reaction monitoring. CPTA/β-CD inclusion compound was prepared by grinding method, DAS 2.0 software was used to model the data, and the absolute bioavailability of CPTA and relative bioavailability of inclusion compound were calculated. Finally, the methods for the determination of five components of senkyunolide A, N-butylphthalide, new osthol lactone, Z-ligustilide and butenyl phthalide in CPTA, were successfully established. The linear relationship among the five components was good within their respective ranges, r>0.99. The absolute bioavailability of the five components in rats was 22.30%, 16.32%, 21.90%, 10.16% and 12.43%, respectively. After CPTA/β-CD inclusion was prepared, the relative bioavailability of the five components was 138.69%, 198.39%, 218.01%, 224.54% and 363.55%, respectively, significantly improved. This method is rapid, accurate and sensitive, so it is suitable for the pharmacokinetic study of extracts in traditional Chinese medicine and their preparations.

Progress in regulation effect of aromatic refreshing traditional Chinese medicine on BBB permeability and its mechanism / 中国中药杂志

The blood-brain barrier (BBB) protects the brain against unwanted substances, while, at the same time, limits the transport of many drugs into the brain. Aromatic refreshing traditional Chinese medicine (TCM) can induce resuscitation and modify the permeability of BBB, promoting other drugs entering into the brain with brain protection effect. This paper mainly reviews the research progress in regulation effects and mechanism of usual aromatic refreshing TCM, such as borneol, moschus, styrax, benzoinum and Tatarinow Sweetflag Rhizome, on BBB permeability. To broaden the application of these drugs in modern pharmaceutics in the future, the relatively research should emphasis on combining aromatic refreshing TCM with new formulations and technologies in pharmaceutics, providing novel promising strategies for brain diseases therapy.

Studies on preparation of sinomenine hydrochloride-loaded bovine serum albumin microspheres / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare Sinomenine hydrochloride-loaded bovine serum albumin microspheres (SM-BSA-MS).</p><p><b>METHOD</b>SM-BSA-MS was prepared by spray drying technique. The morphology, drug-loading and release in vitro of SM-BSA-MS was studied.</p><p><b>RESULT</b>The diameters of SM-BSA-MS were in the range of 1-3 m. The drug loading of microspheres, formulated with different drug/albumin ratios as 1, 2, 1:1, 2:1, were 31.6%, 47.7% and 67.9% , respectively. And the drug entrapment efficiencies of different drug/albumin ratios were higher than 94%. The results of in vitro release experiments showed that the drug loaded microspheres have the properties of sustained-release compared with the Sinomenine hydrochloride injection. Different release characteristics could be obtained by adjusting the prescription composition and the thermal denaturation condition.</p><p><b>CONCLUSION</b>Spray drying technique is a simple and feasible method for preparing SM-BSA-MS. The drug loaded microspheres had high drug-loading and sustained-release effect.</p>

Optimization preparation of chansu-loaded solid lipid nanoparticles by central composite design and response surface method / 中国中药杂志

<p><b>OBJECTIVE</b>To optimize the formulation of chansu-loaded solid lipid nanoparticles (Cs-SLN).</p><p><b>METHOD</b>Cs-SLN was prepared by cold homogenization technique. The effects of influence factors such as the weight of compritol 888 ATO, soybean lecithin and poloxamer 188, on mean diameter, entrapment efficiency, drug loading and overall desirability were investigated by using central composite design and response surface method. The data were imitated using multi-linear equation and second-order polynomial equation.</p><p><b>RESULT</b>The latter was prior to the former considering from multiple correlation coefficients. Under the optimal conditions, the mean diameter, entrapment efficiency, drug loading of the Cs-SLN were 71.5 nm, 92.45% and 5.26%.</p><p><b>CONCLUSION</b>The optimized preparation technique for Cs-SLN is stable, feasible and high inclusion rate. It can be used for production of Cs-SLN.</p>

Effect of particle size on oral absorption of silymarin-loaded solid lipid nanoparticles / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate effect of particle size on oral absorption of silymarin-loaded solid lipid nanoparuicles.</p><p><b>METHOD</b>Solid lipid nanoparticles (SLN) of various sizes (150 nm, 500 nm and 1000 nm) using Compritol 888 ATO as the material and silymarin (SM) as a model drug were prepared. Silybinin concentration in plasma of rats were determined by RP-HPLC with UV detector. The main pharmacokinetic parameters were calculated by 3p97.</p><p><b>RESULT</b>Results showed that the AUC of 150 nm SLN was 2.08 fold that of 500 nm SLN and 2.54 fold of 1000 nm SLN treated orally to rats (P < 0.05). The oral bioavailability of 150 nm SLN was remarkably higher than the other two size SLN.</p><p><b>CONCLUSION</b>This has important implications in designing of SM-SLN as a new oral drug delivery system.</p>

Freeze-drying of silymarin-loaded solid lipid nanoparticles (SM-SLN) / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate lyophilization of SM-SLN.</p><p><b>METHOD</b>The parameters of lyophilization process was optimized. In addition, the protective effect of various types and concentrations of cryoprotectants were tested by shape, colour and disparity.</p><p><b>RESULT</b>The mixture of 2% lactose and 2% glucose could better prevent nanoparticles from aggregating, the optimal lyophilization process was followed: precooled at -45 degrees C for 10 hr; primary drying at -25 degrees C for 5 hr; secondary drying at 10 degrees C for 3 hr; finally drying at 30 degrees C for 6 hr.</p><p><b>CONCLUSION</b>Changes in particle size distribution during lyophilization could be minimized by optimizing the parameters of the lyophilization process and adding supporting agent.</p>