ABSTRACT
In order to increase the stability and solubility of essential oil in Jieyu Anshen Formula, this study was to prepare the essential oil into liposomes. In this experiment, the method for the determination of encapsulation efficiency of liposomes was established by ultraviolet spectrophotometer and dextran gel column. The encapsulation efficiency and particle size of liposomes were used as evaluation indexes for single factor investigation and Box-Behnken design-response surface method was used to optimize the design. Then the optimal formulation of volatile oil liposome was characterized using methyleugenol, elemin, β-asarone and α-asarone as index components. Finally, the in vitro transdermal properties of liposomes were studied by modified Franz diffusion cell. The results showed that the concentration of lecithin, the mass ratio of lecithin to volatile oil, and the stirring speed were the three most significant factors affecting the liposome preparation. The optimum formulation of volatile oil liposome was as follows: the concentration of lecithin was 7 g·L~(-1); mass ratio of lecithin to volatile oil was 5∶1; and the stirring speed was 330 r·min~(-1). Under such conditions, the prepared liposomes had blue emulsion light, good fluidity, half translucent, with particle size of(102.6±0.35) nm, Zeta potential of(-17.8±0.306) mV, permeability of(1.67±1.01)%, and stable property if liposome was stored at 4 ℃. 24 h after percutaneous administration, the cumulative osmotic capacity per unit time was(30.485 2±1.238 9),(34.794 8±0.928 3),(26.677 1±1.171 7),(3.066 2±0.175 3) μg·cm~(-2)respectively for methyleugenol, elemin, β-asarone and α-asarone. In vitro transdermal behaviors of methyleugenol, elemin, β-asarone and α-asarone in liposomes were all consistent with Higuchi equation. The prepared volatile oil liposomes met the relevant quality requirements, providing a reference for further research on preparation of multi-component Chinese medicine essential oil liposomes.
Subject(s)
Administration, Cutaneous , Drugs, Chinese Herbal , Liposomes , Oils, Volatile , Particle Size , SolubilityABSTRACT
Objective In order to optimize the preparation technology of triptolide and ferulic acid ethosomes and evaluate its characteristics of the in vitro transdermal penetration and the preparations performance using ethosome as carrier. Methods The compatibility ratio between triptolide and ferulic acid was determined by MTT. The triptolide and ferulic acid ethosomes were prepared with injection method based on the results of single factor experiments, Box-Behnken design was used to optimize the particle size, electric potential, and encapsulation efficiency (EE) of the ethosomes, and the in vitro release behavior prepared by the optimal formulation were studied. The in vitro transdermal absorption experiment was carried out in optimized Franz diffusion cells. Results The ratio of triptolide to ferulic acid was 1:100. The optimized prescription of the ethosomes was 20% ethanol, 2.2% phospholipid, 90 s ultrasonic time. The results showed that the appearance of the triptolide and ferulic acid ethosomes was clear liquid with blue opalescence in an average diameter of (46.75 ± 2.39) nm at potential of (-46.32 ± 3.76) mV, and the EE was (67.72 ± 1.10)%. The in vitro transdermal behaviors of ferulic acid and triptolide in the ethosomes were in line with the Higuchi equation. Conclusion The ethosomes has the advantages of small particle size, uniform distribution, good stability, and good transdermal absorption property, so as to provide the basis for the development of the transdermal preparation of the effective components of Tripterygium wilfordii.
ABSTRACT
Objective: To prepare the ethosomes-based gel of demethylzeylasteral (DMZ) and to investigate its properties and transdermal absorption behavior. Methods: The infusion method was used to prepare DMZ ethosomes. The particle size, entrapment efficiency (EE), analysis methodology, and in vitro release behavior were examined, respectively. The in vitro transdermal absorption of ethosomes-based gel of DMZ was evaluated by Franz diffusion cells. Results: The DMZ ethosomes was yellowish emulsion. The average particle size of the ethosomes was (365.2 ± 14.4) nm and the EE was (72.30 ± 2.31)%. The cumulative permeation curve of DMZ in ethosomes-based gel was consistent with Higuchi equation (Q=80.198 t1/2-71.641, r=0.986 8). Compared with common gel, the ethosomes-based gel had 3.94 times higher cumulative permeation amount in 24 h. Conclusion: The prepared ethosomes- based gel of DMZ could enhance the transdermal permeation, which provides evidence for the development of transdermal drug delivery system of DMZ.
ABSTRACT
Objective: To study the releasing rule of Artesunate TDD s (ASTDDs). Methods: To prepare the ASTDDS and determine the content of artesunate, the transdermal experiments are used to study the relation between accumulative releasing ratio or releasing speed and releasing time. Results: The content of artesunate is about 45mg/10cm 2 and the accumulative releasing ratio increases with releasing time, but releasing speed is constant when the releasing speed reached some value. Conclusion: The releasing rule of ASTDDs conforms to Higuchi equation. The ASTDDs can come to durable effect.