[An experirmental study on the preparation and drug sustained release characteristics of Pingyangmycin Albumin Microspheres].

OBJECTIVE

The aim of this study was to prepare Pingyangmycin Albumin Microspheres (PYM-AMS) for arteriovenous malformations treatment.

METHODS

PYM-AMS was prepared at 140 degrees C by the method of emulsification-heat solidification and its characteristics were evaluated, such as morphosis, particle size, drug loading (DL%), encapsulation efficiency (EE%), stability and drug sustained-releasing in vitro. After being packaged, PYM-AMS were sterilized with 13.7 kGy of 60Co. Small samples of PYM-AMS were packaged in small bottles and stored at 3 - 5 degrees C, 15 - 25 degrees C, 37 degrees C for 3 months, then checked the change of morphology, DL, EE and the release rate.

RESULTS

The surface of particles was smooth and integrated. The average diameter of PYM-AMS particles was 139.422 microm and 80% was in the range of 56 - 251 microm. The mean DL% and EE% were 26.47% and 84.3%, respectively. PYM released fast in 5 h, but then released slowly. 88.65% drugs were released in 24 h, and t50 was 1.5 h. There was no obvious change of the morphology, DL,EE and the release rate of PYM-AMS stored at 3 - 5 degrees C 15 - 25 degrees C, 37 degrees C for 3 months.

CONCLUSIONS

PYM-AMS prepared in this study had sustained-release effect, high drug loading and high stability. Albumin is a good carrier of PYM embolization agent.