ABSTRACT
Objective: To optimize the preparation process of gambogic acid (GA) liposomes and study the in vitro and in vivo release. Methods: The detection method of GA was established, using the Box-Behnken experiment design to optimize liposomes formula, GA liposomes were obtained with the highest encapsulation efficiency; Using scanning electron micrographs (SEM) to observe liposome surface morphology, using the dialysis method to study the liposome release in vitro, we also measured the stability of liposome in 15 d; Male Wistar rats were injected with GA or GA liposomes (1 mg/mL) via tail vein, UPLC-MS/MS method was used to determine the drug concentration, and differences in pharmacokinetic parameters of the two drugs were compared. Results: After Box-Behnken optimization, the encapsulation efficiency of liposomes was 92.3%, and the optimized liposomes formula is cholesterol of 440 mg, egg phosphatidylcholine of 1823 mg,,and istearoyl phosphoethanolamine-PEG 2000 of 705 mg, liposomes had uniform particle size and smooth surface; In vitro release results showed that the liposomes could be gentle and slowly release and had a long- term effect. The liposomes were stable keeping in 4 ℃ within 15 d; In in vivo study, the half-life of GA liposome was 9.97 h, 4.43 times of GA; AUC0-24 h of GA liposome was 22.55 μg∙h/mL, 4.73 times of GA. Conclusion: Compared with GA, GA liposome has the characteristics of long-circulating, high blood drug concentration, and could release smoothly.
ABSTRACT
Objective: To optimize the prescription of Baoxieling Hydrogel Patch (BHP) using Box-Behnken test design and to investigate its transdermal absorption properties in vitro. Methods: Taking the comprehensive scores of the early adhesion, uniformity, ductility, consistence, skin adhesive ability, repeated exposing paste, and residue as response values, Box-Behnken test design was used to optimize the amounts of sodium polyacrylate NP 800, aluminum glycinate, and fillers, and to validate the optimal formulation. The percutaneous permeation of cinnamaldehyde, eugenol, evodiamine, and rutaecarpine in the optimal formulation was studied by in vitro transdermal delivery experiment with Franz diffusion cells and their contents were determined by HPLC. Results: The optimal ratio of the prescription was as follows: sodium polyacrylate NP 800-aluminum glycinate-fillers (0.82:0.02:1.56). The foremost factors were fillers and aluminum glycinate. Its transdermal absorption met zero order dynamic process. Conclusion: The optimal prescription has uniform paste, suitable consistence, easy ductility, moderate adhesion, and perfect transdermal effect. It could provide the foundation for the development of new prescription of Baoxieling.