Freeze-drying of oleanolic acid-loaded nanosuspensions / 中国中药杂志

<p><b>OBJECTIVE</b>Several cryoprotectants were employed to study the protective effect on the freeze-drying process of the oleanolic acid-loaded nanosuspensions (OLA-LS) in order to select the optimum formulation.</p><p><b>METHOD</b>The protective effect was evaluated by measuring the mean particle size of samples before and after freeze-drying process.</p><p><b>RESULT</b>Sucrose with the concentration of 10% was selected as the optimum cryoprotectant. The average size of excellent sample was 236.3 nm (versus 211.2 nm of fresh one), and a much higher polydispersity index of 0.242 (versus 0.180).</p><p><b>CONCLUSION</b>The optimum lyophilized powder could be obtained with suitable type of cryoprotectant with appropriate concentration and proper freeze-drying conditions.</p>

Microstructure of novel solid lipid nanoparticle loaded triptolide / 药学学报

Novel solid lipid nanoparticle (SLN) system is prepared with Compritol ATO 888 and tricaprylic glyceride. DSC, XRD, SAXS and NMR are employed to study the novel carrier property and microstructure. When the peak melting point decreased from 70.8 degrees C to 61.4 degrees C, the enthalpy sharply decreased. It could be concluded that the regular crystal lattices in the novel carriers are broken out for the oil joined in them. Melting behavior is occurred at -17.7 degrees C while novel SLN is composed of oil and solid lipid mixture from the DSC measurement. Most alpha phase and least beta' phase are in the nano carrier system whether drug loading or not from the XRD investigation. There is only 0.1 nm change of long space among the novel SLN made of mixture and the lipid matrix and traditional SLN; therefore, it is impossible of the oil molecular insert into the solid glyceride structure. Since the different melting behavior (DSC measurements) and molecular move state (NMR investigations), two lipid matrix are still in two state of liquid and solid lipid in the novel SLN carrier. Presume the microstructure of the novel SLN prepared by our experiment would be that liquid oil has formed superfine nano accommodation encapsulated with solid lipid, but the whole particle is still in nano size range.

Study on separation and purification of total flavones from Smilax china by macroporous absorption resin / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the technological parameters of the purification process of total flavones from Smilax china with macroporous absorption resin.</p><p><b>METHOD</b>The technical process for purification of total flavones with the optimum macroporous absorption resin was screened by yield of total flavones product.</p><p><b>RESULT</b>The D140 macroporous absorption resin had the best separating efficiency when the flavones content in the liquid was 0.5 g x mL(-1) equivalent to raw material, the volume of drug 18 BV (resin bad volume) with the adsorption-power 2 BV x h(-1), and the volume of 60% (mL x mL(-1)) ethanol as eluant 5-10 BV (resin bad volume) with desorption-power 1 BV x h(-1). The obtained flavones product has total flavones recovery rate of 84.72%.</p><p><b>CONCLUSION</b>The treatment of regenerated resin is easy, this method is advisable.</p>

Preparation and permeation studies of soybean lecithin-based vesicles / 中国医学科学院学报

<p><b>OBJECTIVE</b>To investigate various methods for constructing soybean lecithin (SL)-based vesicles and evaluate the permeation-enhancing effect of SL-based vesicles on the penetration of insulin through buccal mucosa.</p><p><b>METHODS</b>The ultrasonic method, high speed shear method and high pressure homogenization method were respectively used to prepare the SL-based vesicles, and the particle size of the vesicles was measured with photon correlation spectrometry (PCS). The penetration rate of insulin through porcine buccal mucosa was investigated with the Valia-Chien diffusion cells.</p><p><b>RESULTS</b>The average particle sizes of 3 formulations of SL-based vesicles were 97.39, 85.60, and 100.60 nm when prepared by ultrasonic method, and were 58.7, 88.7, and 91.9 nm when prepared by high pressure homogenization method. Both vesicles presented good stability. However, the SL-based vesicles prepared by high speed shear method had larger average diameters and were found to be unstable. Transmission electron microscopy showed that SL-based vesicles had a spherical shape and the result accorded with PCS. The permeation flux of insulin of formulation 1 and control solution were 0.0024 and 0.0008 IU x ml(-1) x min(-1), respectively. The accumulative amount of formulation 1 at 180 min was (0.436 +/- 0.010 ) IU x ml(-1), which was 1.46 times higher than the control solution.</p><p><b>CONCLUSIONS</b>The SL-based vesicles obtained using high pressure homogenization method are characterized by small particle size, narrow distribution, good stability, and powerful permeation-enhancing effect, which enables them to be good carriers for the buccal delivery of insulin.</p>

The anti-inflammation effects of Smilax china ethylacetate extract in rats and mice / 中国中药杂志

<p><b>OBJECTIVE</b>To study the anti-inflammations of the ethyl acetate extract of S. china on acute and chronic inflammations.</p><p><b>METHOD</b>The rat paw edema induced by egg-albumin, the ear edema and the foot edema of mice induced by xylene and formaldehyde, the increased vascular permeability of capillary induced by intraperitoneal injection of 0.7% acetic acid in mice were used to study on the acute, early inflammations and chronic inflammation for the ethyl acetate extract of S. china.</p><p><b>RESULT</b>The extract (50-100 g x kg(-1)) could significantly decrease the rat paw edema, and inhibit the ear edema, the increased vascular permeability and the foot edema of mice.</p><p><b>CONCLUSION</b>The ethyl acetate extract of S. china possesses remarkable anti-inflammatory effects on acute inflammation, and also displays anti-inflammatory effects on the chronic inflammation at a certain extent.</p>

Design and manufacture of microneedles array for transdermal drug delivery / 中国医疗器械杂志

It is very important to disrupt the stratum corneum structure and to create pathways allowing transport of macromolecules, as the traditional transdermal drug delivery has been severely limited by the skin barrier. With the development of the Micro Electro-Mechanical System (MEMS), it becomes possible for microneedles array to strengthen the transdermal drug delivery. In addition to the increase of the skin permeability, it can also be used to deliver drugs into skin, such as insulin and vaccine, providing a new direction for drug delivery systems. In this paper, we review the development and applications in transdermal drug delivery of microneedles' array. The commercial prospects and recommendations for the future research work are also represented.

Isopropyl myristate molecular gels and drug-loaded transdermal capability / 药学学报

<p><b>AIM</b>To prepare of isopropyl myristate (IPM) molecular gels and investigate of its transdermal capability.</p><p><b>METHODS</b>Microstructure of IPM gels was studied by scanning electron microscope (SEM) and optical microscope (OM). The rheology and thixotropy of IPM gels were investigated by viscosity. Triptolide was used as model drug to investigate its transdermal capability.</p><p><b>RESULTS</b>The microstructure of IPM gels was a three-dimension network formed by the aggregation of Span 60 in IPM, which was rod-like tubular aggregate. It has good rheology and thixotropy. There was a good linear correlation between the accumulative permeated amount per unit area and the time for triptolide-loaded IPM gels. The permeation process agreed with zero order pharmacokinetics. The average permeability through rat skin for triptolide was 19.26 ng x cm(-2) x h(-1), which was 2.92 times of triptolide unguents obtained commercially available.</p><p><b>CONCLUSION</b>Isopropyl myristate molercular gel can be formed by span 60 assemblies. Transdermal capability drug-loaded IPM gels was better than that of triptolide unguents.</p>

Optimization of purification conditions for with macroporous adsorption resin total saponins from smilax china / 中国中药杂志

<p><b>OBJECTIVE</b>To develop a with high efficiency and practicality for separating and purifying total steroidal saponins lax china.</p><p><b>METHOD</b>Using adsorption capacity and desorption rate of total steroidal saponins as the primary screening index, surveyed, and the optimized conditions of adsorption and desorption of total steroidal saponins were studied.</p><p><b>RESULT</b>The adsorption and desorption rate of total steroidal saponins reached 16 mg x mL(-1) and 90% respectively for macroporous resin HPD100 chosen. Macroporous resin HPD100 could be well used in separating and purifying total steroidal saponins from S. china.</p>

Progress in research on triptolide / 中国中药杂志

To further understand triptolide, this paper has introduced the pharmacology, pharmacokinetics, toxicity, the clinic application and semi-synthesis of triptolide on basis of importance and significant contents of reference which have been consulted in the past twenty years. Presently triptolide and Tripterygium wilfordii have been a hot spot of modernization of Chinese traditional medicine. It is very important to develop a new dosage form of high effect and low toxicity by making use of advanced technology according to its characteristics.

Enhanced absorption of breviscapine photosomes in small intestine of rats / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate whether the absorption of breviscapine can be enhanced by using breviscapine photosomes.</p><p><b>METHOD</b>Testing the uptake and intestinal permeability of breviscapine powder and breviscapine photosomes by using intestine perfusion technique and reverted gut sac method.</p><p><b>RESULT</b>The uptake and permeability coefficient of breviscapine were increased in photosomes. The absorption process obeyed the Fick's law in the range of 0-100 microg x mL(-1).</p><p><b>CONCLUSION</b>The absorption breviscapine photosomes is enhanced by increasing the permeability through a passive mechanism.</p>

Characterization of Me. PEG-PLA copolymer nanoparticles prepared by modified spontaneous emulsion-solvent evaporation / 药学学报

<p><b>AIM</b>Characterization of poly (D, L-lactic acid)/monomethylether terminated/polyethylene glycol (Me. PEG-PLA) block copolymers nanoparticles.</p><p><b>METHODS</b>Me. PEG-PLA block copolymers were prepared by bulk polymerization. A series of nanoparticles were made from Me. PEG-PLA block copolymer by modified spontaneous emulsion-solvent evaporation technique.</p><p><b>RESULTS AND CONCLUSION</b>The structure of copolymer was performed by means of 1HNMR and FT-IR. The morphological examination of nanoparticles was performed by means of atomic force microscope (AFM). Results indicated that nanoparticles exhibited a smooth spherulite and core-shell structure. The hydrophilic shell is consisted of PEG segments and hydrophobic core is consisted of PLA segments. Zeta potential of nanoparticles was zero and further indicated core-shell structure. The particle size and size distribution of nanoparticles were measured by laser light scattering technique. The effective particle size range was from 70 to 160 nm and showed a normal distribution.</p>

Preparation and toxicity of triptolide-loaded poly (D,L-lactic acid) nanoparticles / 药学学报

<p><b>AIM</b>Investigations on reducing the toxicity of triptolide through poly(D, L-lactic acid) nanoparticles as a drug carrier by oral administration to Wistar rats.</p><p><b>METHODS</b>Triptolide-loaded poly (D, L-lactic acid) nanoparticles (TP-PLA-NPs) were prepared by modified spontaneous emulsification solvent diffusion (modified-SESD). The shape of nanoparticles was observed by transmission electron microscope (TEM). The size distribution and mean diameter were measured by laser light scattering technique. The entrapment efficiency and contents of drug loading were determined by RP-HPLC. The physical state of drug loaded in nanopartiles were primarily investigated by X-ray powder diffractometry. TP-PLA-NPs release behavior in vitro was carried out. After oral administration of the nanoparticles to Wistar rats in 15d, the toxicity for liver and kidney were studied by determining aspartate transaminase (AST), alanine transaminase (ALT) and blood urea nitrogen in serum and concentration of protein in urine.</p><p><b>RESULTS</b>The preparation process adapted to the formulation was as follows: the volume ratio of the aqueous and organic phases was 40/15; the surfactant concentration was 1%; the drug concentration was 0.3%; triptolide-PLA was 1:15 (w/w). The mean diameter was 149.7 nm and the polydispersity index was 0. 088 for the nanoparticles prepared by above conditions. The entrapment efficiency and content of drug loading were 74.27% and 1.36%, respectively. The release behavior of drug in vitro showed an initial burst effect, subsequently a slower rate stage. The results indicated that the liver toxicity (P < 0.01) and kidney toxicity (P < 0.05) caused by triptolide could be decreased significantly by nanoparticles carrier.</p><p><b>CONCLUSION</b>PLA-NPs might be used as a new oral carrier for triptolide.</p>