Effect of Electroporation on Percutaneous Permeation of Sinomenine Hydrochloride / 中国实验方剂学杂志

Objective:To investigate the percutaneous permeability of sinomenine hydrochloride （SNH） and optimize the parameters of electroporation to achieve the best permeation enhancing effect on SNH. Method:The percutaneous permeability of SNH and the enhancement effect of electroporation were studied by <italic>in vitro</italic> diffusion cell method， and the enhancement effect of electroporation was further evaluated by <italic>in vivo</italic> study in mice. Result:Under steady-state condition， the permeation rates of SNH in stripped skin and intact skin of hairless mice were （385.81±12.88）， （0.88±0.20） μg·cm^-2·h^-1， respectively. The permeation rate in stripped skin was 438 times higher than that in intact skin. The results of percutaneous permeation kinetics analysis showed that the solubility and diffusion coefficient of SNH in stratum corneum were relatively low， which were （70.82±9.63）×10³ g·m^-3 and （3.07±1.52）×10^-14 cm²·s^-1， respectively. Under the optimized electroporation conditions （voltage of 72 V， time of 60 min）， the 24 h cumulative permeation amount of SNH through skin of mice was （10 008.39±1 961.57） μg·cm^-2， and the steady-state permeation rate was （456.01±51.26） μg·cm^-2·h^-1， which were 5.4 times and 5.1 times higher than those of blank group， respectively. <italic>In vivo</italic> studies in mice showed that the contents of SNH in skin and muscle of electroporation group were 2.0 times and 1.5 times higher than those of blank group. Conclusion:The low solubility and low diffusion coefficient of SNH in the stratum corneum are the main factors hindering the percutaneous permeation of SNH. Electroporation can significantly increase the percutaneous permeation of SNH and its retention in skin and muscle of mice.

Enhancement of transdermal absorption of puerarin by microneedle-assisted microemulsion / 中草药

Objective: To enhance the percutaneous absorption of puerarin, a water insoluble drug, using microneedle-assisted microemulsion. Methods: With puerarin microemulsion as control, in vivo and in vitro experiments were conducted to evaluate permeation amount of puerarin, which was increased by 12.4 times using microneedle-assisted microemulsion. In rat skin microdialysis experiments in vivo, the peak concentration (Cmax) of puerarin in reception medium was (713.51 ± 72.23) ng/mL for microneedle-assisted microemulsion group and (108.56 ± 5.72) ng/mL for microemulsion group; The areas under concentration-time curves (AUCs) of puerarin were (5 021.45 ± 547.09) ng∙h/L for microneedle-assisted microemulsion group and (622.36 ± 41.21) ng∙h/L for microemulsion group, respectively. Compared with microemulsion, the Cmax and AUC of puerarin in rat skin microdialysis experiments in vivo were increased by 5.57 times and 7.07 times, respectively, when microneedle-assisted microemulsion was used. In pharmacokinetic experiments in rats, the Cmax and AUC of puerarin in rat plasma were (234.35 ± 25.02) ng/mL and (3 047.13 ± 486.51) ng∙h/L for the microneedle-assisted microemulsion group. The puerarin concentration in rat plasma for the microemulsion group were lower than the limit of detection. Conclusion: The transdermal absorption of puerarin could be enhanced obviously using microneedle-assisted microemulsion. By conducting this research, a preliminary foundation is laid for the development of novel delivery systems for puerarin.

Transdermal Permeation of Compound Film Forming Gel in vitro / 中国药师

Objective:To study the preparation and in vitro release and transdermal absorption of compound film forming gel. Methods:The compound film forming gel was made from new types of film-forming materials. The in vitro release rate was determined by Franz diffusion cells. Results:The in vitro release rate of mupirocin and dyclonine from the compound film forming gel was 81.34% and 88.46%,the transdermal cumulative release amount was(192.73 ± 0.45) μg·cm-2and(103.58 ± 0.66) μg·cm-2,and the skin retention was (419.81 ± 1.48) μg·cm-2and (212.07 ± 1.81) μg·cm-2, respectively. Conclusion: The release of drug is nearly complete. The transdermal absorption test shows that about 30.26% mupirocin and 32.53% dyclonine can pass through skin, and about 65.91% mupirocin and 66.59% dyclonine are stored in skin. The preparation not only plays the role of bacteriostasis,but also promotes wound healing and analgesia.

Preparation of baicalin nasal gel and its permeation through nasal mucosa / 中草药

Objective: To prepare the nasal gel of baicalin and to evaluate its permeation in vitro. Methods: The orthogonal design was carried out using Cabopol-936 as gel matrix, glycerine as solubilizer, and triethanolamine as pH value and viscosity adjuster. The permeating rate of baicalin from nasal gel was determined through pig nasal mucosa in vitro by transdermal diffusion method. Results: The optimum nasal gel was made by 0.5% Carbomer-936, 30% glycerine, and 2% baicalin, with pH value 6.85-7.00, and the average viscosity was 1850-2350 Pa·s. The permeation of baicalin through nasal mucosa was fitted with first-order kinetics, the regression equation was Y=0.2806 X+0.5643, r=0.997, and the permeating rate was 0.2806 μg/(mm2·h). Conclusion: The preparation of baicalin nasal gel is simple. Baicalin is almost permeated through nasal mucosa by simple diffusion.