[Studies on gelatin microspheres-in-oil emulsion of pingyangmycin].
As a drug for lymphosarcoma, pingyangmycin (A5) is not widely used because of its toxicities, short half-life and low affinity to lymph. For the purpose of delivering A5 to the lymph system to strengthen and sustain its effects and to lower its toxicities, its gelatin microspheres-in-oil emulsion (S/O) was studied in vitro and in vivo. By ultrasonication, gelatin microspheres with diameters of 1.67 +/- 0.69 microns were homogeneously dispersed in oil to form the S/O, which was a pseudoplastic flow and stable under 0 degrees C for at least 1 month. With the content of 14.03 +/- 0.15 mg.ml-1, A5 released from the emulsion in a zero order rate with t0.5 of 12.0 h. In vivo experiments showed that the S/O emulsion exhibited potent lymphotropicity, prolonged plasma concentration and a probably lower pulmonary toxicity.
Li
H S
HS
School of Pharmacy, Beijing Medical University.
Wei
S L
SL
Lu
W
W
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001761:Bleomycin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000031:analogs & derivatives; D016503:Drug Delivery Systems; D004655:Emulsions; D005780:Gelatin; D008863:Microspheres; D011817:Rabbits; D014018:Tissue Distribution
D000903:Antibiotics, Antineoplastic; D004655:Emulsions; D001761:Bleomycin; C021771:zhengguangmycin; D005780:Gelatin