Preparation and characteristics of erythromycin microspheres for lung targeting.
BACKGROUND
If erythromycin is micronized into microspheres with suitable particle size, it can improve pulmonary drug concentration to maximize its effectiveness and minimize the adverse side effects.


OBJECTIVE
In this study, erythromycin gelatin microspheres (EM-GMS) were prepared and some characteristics of EM-GMS were investigated. The drug-targeting index (DTI) of EM-GMS was evaluated to predict their potential as a targeted delivery system.


METHODS
Erythromycin was microencapsulated with gelatin by a double emulsion solvent evaporation method. Some characteristics of EM-GMS, including morphology, particle size, in vitro release, and safety were researched.


RESULTS
EM-GMS had a spherical shape and smooth surface morphology. The drug loading and encapsulation efficiency of EM-GMS were 13.56 +/- 0.25% and 55.82 +/- 2.23%, respectively. The release of erythromycin from EM-GMS showed an initial burst and following a sustained release, with an accumulate release of 80% at 4 hours. The EM-GMS was safe since there was no vein irritation and no hemolysis on the erythrocyte of rabbit at 3.5 mg/mL and a LD50 of 173.07 mg/kg. After administering EM-GMS to rabbits, the concentration of erythromycin in lung was 15.92 times higher than that in plasma and the DTI of EM-GMS in lung was 6.65 as compared with erythromycin lactobionate.


CONCLUSIONS
The preparation technology of EM-GMS for lung targeting was successful and the quality of microspheres was good.
Fan
Yang
Y
Department of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, PR China.
Shan-Guang
Wu
W
Yu-Fang
Pan
P
Feng-Lan
Song
S
Tao
Li
L
D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000633:toxicity; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D004917:Erythromycin / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000493:pharmacokinetics / Q000633:toxicity; D005260:Female; D005780:Gelatin; D008168:Lung / Q000378:metabolism*; D008297:Male; D051379:Mice; D008863:Microspheres; D010316:Particle Size; D011817:Rabbits; D013678:Technology, Pharmaceutical / Q000379:methods; D013997:Time Factors; D014018:Tissue Distribution
D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; C010948:erythromycin lactobionate; D004917:Erythromycin; D005780:Gelatin