[Preliminary study on preparation and pharmaceutic features of adrimycin-loaded human serum albumin microspheres].
OBJECTIVE
To prepare adrimycin-loaded human serum albumin microspheres(ADR-HSA-MS) and to study its pharmaceutic properties and in vitro cytotoxicity.


METHODS
ADR-HSA-MS, consisting of ADR and HSA, were prepared by emulsion heating solidification method and its morphology was observed by optical microscopy and scanning electron microscopy. Pepsin digestion method was used for determining drug loading of ADR-HSA-MS and membrane diffusion technique for detection of in vitro release of ADR from the microspheres. MTT colorimetric assay was used to determine cytotoxicity of ADR-HSA-MS for human hepatoma SMMC-7721 cell line.


RESULTS
ADR-HSA-MS looked like smooth red spheres with an average diameter of 1.2 microns and had an apparent drug-loading of 2.73% or an effective drug-loading of 1.69%. Its peak of the accumulated drug-releasing fraction was 65%, and 50% of ADR releasing from the MS would take five days, which suggested a slow release of ADR from the albumin microspheres. ADR-HSA-MS exerted remarkable cytotoxicity to human hepatoma SMMC-7721 cells with dose-dependence at a range of ADR concentration from 0.3 microgram/ml to 2.5 micrograms/ml when incubated with the target cells for four days. Its killing curve was similar to that of free ADR.


CONCLUSIONS
Emulsion heating solidification method could be used for preparation of adrimycin-loaded human serum albumin microspheres with sustained release property.
Immunology Department, West China School of Preclinical and Forensic Medicine, Sichuan University, Chengdu 610041, China.
Xiao-bo
XB
Liu
Mei-ying
MY
Cai
Yan
Y
Gong
Zhi-rong
ZR
Zhang
Da-peng
DP
Wei
Xia
X
Wang
Guang
G
Li
D000903:Antibiotics, Antineoplastic / Q000494:pharmacology; D006528:Carcinoma, Hepatocellular / Q000473:pathology*; D003602:Cytotoxicity, Immunologic; D003692:Delayed-Action Preparations; D004317:Doxorubicin / Q000494:pharmacology*; D004337:Drug Carriers; D006801:Humans; D008113:Liver Neoplasms / Q000473:pathology*; D008863:Microspheres; D004364:Pharmaceutical Preparations / Q000138:chemical synthesis; D012709:Serum Albumin; D014407:Tumor Cells, Cultured
D000903:Antibiotics, Antineoplastic; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004364:Pharmaceutical Preparations; D012709:Serum Albumin; D004317:Doxorubicin