RESUMO
OBJECTIVE: To prepare docetaxel liposomes by freeze-drying of tert-butyl alcohol (TBA)/water cosolvent system and evaluate the in vitro and in vivo properties. METHODS: The formulation was optimized by single factor screening experiments. The effects of TBA/water ratio, lipid/drug ratio, sucrose/lipid ratio and mixing temperature on encapsulation efficiency were investigated. The in vitro release profiles were also investigated with docetaxel injection (Duopafei®) as control. RESULTS: The formulated liposomes had a mean size of 263 nm with entrapment efficiency of (845±1.63)% at TBA/water ratio 50:50, lipid/drug ratio 10:1, sucrose/lipid ratio 5:1 and mixing temperature 60℃. In vitro drug release from liposomes lasted for 48 h. CONCLUSION: Freeze-drying of TBA/water cosolvent system method may be feasible to prepare docetaxel liposomes.
RESUMO
Objective: To prepare the hyperoside solid nanocrystal (Hyp-SN) and to determine the in vitro release. Methods: The high pressure homogenization technology was applied to preparing Hyp nanosuspension, and then Hyp-NS was solidificated into Hyp-SN by freeze-drying. The fomulation and process of Hyp-SN were optimized by the single factor experiment. Dried powders were prepared under the optimal condition and characterized for crystallinity and particle size. In vitro dissolution of Hyp-SN was also determined. Results: The particle size of Hyp-SN protected by tert-butyl alcohol was (405.2 ± 14.6) nm, as well as the polydispersity index (PI) was 0.25 ± 0.08. The results of SEM showed that Hyp-SN powder was irregular rod and XRD showed Hyp was crystalline in both coarse powder and nanosuspensions. In the in vitro dissolution test, Hyp-SN showed an increased dissolution markedly. Conclusion: The method employed to prepare the Hyp-SN is simple and feasible. Hyp-SN could significantly improve the dissolution of Hyp. It has a broad application prospects.