Preparation and quality evaluation of Acori Tatarinowii Rhizoma-volatile oil microemulsion / 中草药

Objective: Taking the volatile oil of Acori Tatarinowii Rhizoma with the effect of anti-senile dementia as model drug to prepare Acori Tatarinowii Rhizoma-volatile oil microemulsion (AO-ME). Methods: The composition of microemulsion was preliminarily determined according to the solubility of volatile oil from Acori Tatarinowii Rhizoma in various solvents. By drawing pseudo-ternary phase diagram, the optimal microemulsion formulation was selected according to the size of particles and microemulsion region, stability of preparations and drug loading. Results: The optimal microemulsion formulation was that volatile oil of Acori Tatarinowii Rhizoma-Cremophor EL-glycerol-water was 6.25:20.83:10.42:62.5. The average particle size of AO-ME was (30.5 ± 0.2) nm with a polydispersity index of 0.150 ± 0.002. The viscosity value of AO-ME was (2.80 ± 0.21) mPa∙s. In vitro transdermal rate of AO-ME was (1 288.76 ± 16.20) μg/(cm2∙h), measured in β-asarone. Compared with ordinary emulsion, the transdermal rate of AO-ME was increased 14 times. The ciliary toxicity test of toad showed that the preparation had no significant toxicity. Conclusion: The preparation of AO-ME was prepared with stable physicochemical properties, good transdermal properties, and low toxicity to nasal mucosa cilia.

Preparation and In Vitro Evaluation of Sinomenine Liquid Crystal Gel / 中国药学杂志

OBJECTIVE: To prepare and characterize sinomenine liquid crystal gel, study the rheological properties and in vitro transdermal properties and compare with sinomenine ointment and sinomenine hydrophilic gel. METHODS: Sinomenine liquid crystal gel was prepared by using phytanetriol-water system and then characterized by polarized light microscope(PLM)and small angle X-ray diffraction(SAXS). Using DHR-2 rheometer, the rheological properties of sinomenine liquid crystal gel were investigated and compared with those of sinomenine ointment and sinomenine hydrophilic gel. Modified Franz diffusion cell was used for in vitro transdermal experiment and the in vitro transdermal properties were compared with sinomenine hydrogels and ointments. RESULTS: The appearance of sinomenine liquid crystal gel was colorless, clear and transparent, and showed dark field under PLM. SAXS showed cubic phase. The rheological parameters were good. The steady-state infiltration rates of sinomenine liquid crystal gel, ointment and hydrophilic gel were 153.93, 119.99, and 106.89 μg·cm-2·h-1, and their 48 h cumulative permeation amounts(%)were 93.76%, 91.55%, and 87.60%, respectively. CONCLUSION: PLM and SAXS can be used to characterize the liquid crystal gel.The prepared sinomenine liquid crystal gel has good appearance and suitable rheology, and its infiltration rate and 48 h cumulative permeation amount are superior to those of ointment and hydrophilic gel, which provides theoretical reference for sinomenine percutaneous administration.

In vitro and in vivo Transdermal Penetration of Testosterone Undecanoate Binary Ethosomes Gel / 中国药师

Objective:To study the in vitro and in vivo transdermal penetration of testosterone undecanoate ( TU) binary ethosomes gel. Methods:TU binary ethosomes were prepared by an ethanol injection method, and using carbopol 941 as the gel base, TU binary ethosomes gel was prepared. Using mouse skin as the barrier, Franz cells were applied to explore the in vitro transdermal penetration of TU binary ethosomes and the gel. Rats were used as the animals, and TU binary ethosomes and the gel was respectively administrated on the back skin. At the predetermined time points, plasma samples were withdrawn to detect the concentration of TU, and the main pharmacokinetics parameters were calculated. Results: The in vitro transdermal penetration of TU binary ethosomes and the gel was both fitted first-order equation:Q=8. 68t+6. 78(r=0. 998 2) and Q=6. 09t+3. 09(r=0. 999 3), and the stable penetration rate was 8. 68 μg·cm-2 ·h-1 and 6. 09μg·cm-2 ·h-1 , respectively. After the 24-hour penetration, the residual amount in skin of TU binary ethosomes and the gel was (208. 80 ± 55. 26)μg·g-1 and (225. 60 ± 38. 90)μg·g-1 , respectively. The main pharmacokinet-ics parameters of TU binary ethosomes and the gel were Cmax of(18.50 ±2.75)mg·L-1 and(20.80 ±2.42)mg·L-1, tmax of(6.20 ± 0. 14)h and(9. 54 ± 0. 52)h, and AUC0-48h of(336. 74 ± 2. 05)h and(486. 30 ± 1. 68)h. Conclusion:TU binary ethosomes and the gel both exhibit promising in vitro transdermal penetration, and the gel shows better sustained release property.

Study on preparation and in vitro transdermal penetration of betulinic acid ethosomes modified by sodium deoxycholate / 中草药

Objective: To prepare and optimize the prescription of betulinic acid (BA) ethosomes modified by sodium deoxycholate (SDC) and then to investigate its transdermal penetration as carrier of BA. Methods: The BA ethosomes modified by SDC were prepared by the ethanol injection method. The encapsulation efficiency (EE) was considered as the evaluation index to optimize the prescription of the ethosomes by orthogonal design, and the shape and particle size of the optimized ethosomes were analyzed. The in vitro transdermal absorption of BA was evaluated using Franz diffusion cells. The accumulated permeation amounts and permeation rate of liposomes, ethosomes, and BA ethosomes modified by SDC were compared. Results: The best formulation consisted of soybean lecithin-SDC-BC (18:1:1) and 35% ethanol. The average EE and the particle size were (93.8 ± 1.6)% and (102.3 ± 3.6) nm, respectively. The accumulated permeation amount of BA ethosomes modified by SDC in 12 h was (99.62 ± 9.44) μg/cm2, which was 1.67, 3.85, and 8.33 times of ethosomes, liposomes, and satuated solution containing 10% isopropanol, respectively. Conclusion: The BA ethosomes, modified by SDC with high EE, obviously enhance the percutaneous absorption of BA and might be one of the most perspective percutaneous preparations.

Preparation of perillyl alcohol ointment and investigaion on its in vitro transdermal penetration / 中草药

Objective: To prepare perillyl alcohol ointment (PAO) and to investigate its properties and transdermal absorption behavior. Methods: The emulsion method was used to prepare PAO. The morphology, stability, and in vitro release were examined, respectively. The transdermal absorption of PAO was evaluated using Franz diffusion cells and the perillyl alcohol content was determined by HPLC. Results: The optimal prescription of PAO was perillyl alcohol, stearic acid, glyceryl monostearate, white vaseline, lanolin, liquid paraffin, triethanolamine, glycerine, and ethylparaben. The product was a pale yellow semi-solid oil-in-water emulsion with a uniform appearance. The content of perillyl alcohol in ointment was (2.89 ± 0.17)%, the release accumulation in vitro achieved 61.25% in 12 h, and the percutaneous penetration rate was 9.42 μg/(cm2·h). The ointment was not stratified after the centrifugation at 3500 r/min for 30 min, and the product was fairly stable under the condition of storing at 0 and 40°C for 30 d. Conclusion: The prepared PAO with increased skin retention amount could be developed into a novel preparation of perillyl alcohol for focal administration.