Abstract:

BACKGROUND: How to improve the efficacy and stability of all-trans retinoic acid, as well as to reduce side effects are great issues in clinical treatment. In recent years, biodegradable polymers materials are prepared into particle dispersion system by using emulsifying and encapsulation technology, increasing studies investigate its role as a slow and controlled release agent.
OBJECTIVE: To prepare all-trans retinoic acid-polyanhydride (ATRA-PAD) long-term delayed release microspheres therapeutic agent, and to determine slow-release treatment agent ATRA release in vivo and in vitro by the changes of time.
METHODS: A long-acting sustained-release microsphere ATRA-PAD therapeutic agent was established with emulsion/solvent evaporation method, the appearance and microsphere size were detected by using scanning electron microscopy, high performance liquid chromatography was applied to detect the drug loading, encapsulation efficiency, release volume in vivo and in vitro.
RESULTS AND CONCLUSION: The therapeutic microspheres were smooth and had uniform size, the average particle size was (154.42±26.76) nm, drug loading was (16.52±1.45)%, encapsulation efficiency was (87.84±4.79)%; release in vitro experiments indicated that the ATRA sustainable release of the therapeutic agent microsphere was about 50 days, following intramuscular injection into rabbits, ATRA may be stably released for about 45 days. ATRA-PAD microsphere therapeutic agent exhibits high drug loading and encapsulation efficiency, in vivo and in vitro drug release are stable and has obvious long-term sustained action.