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  • Title: Preparation and characteristics of erythromycin microspheres for lung targeting.
    Author: Fan Y, Shan-Guang W, Yu-Fang P, Feng-Lan S, Tao L.
    Journal: Drug Dev Ind Pharm; 2009 Jun; 35(6):639-45. PubMed ID: 19259878.
    Abstract:
    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. AIM: 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. METHOD: 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.
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