Abstract
Purpose: To optimize erythromycin microparticles by in vitro bioassay methods based on its antibacterial activity.
 Methods: The microparticles were produced by high shear homogenization. The effects of different lipid-to-surfactant ratios were studied. The hydrodynamic size of the different batches was evaluated using dynamic light scattering while bioactive drug load per batch was assessed in agar using bioassay methods. The antimicrobial activities of selected batches were tested ex vivo by determination of reduction in bacteraemia following administration of the microparticles to infected animals.
 Results: All batches had particles with hydrodynamic sizes < 8.5 microns. Batch 7 with a 2: 5: 2.5 (drug: surfactant: stearic acid) ratio, represents the optimized batch with a hydrodynamic size of 2281 nm, a bioactive drug loading capacity (BLC) of 4.67 ± 0.70 % and bioactive drug entrapment efficiency (BEE) of 10.51 %. The “microparticle MIC” against Staphylococcus aureus was 1.74 x 10-3 μg/ml. Despite containing lower amounts of erythromycin than the pure sample, the microparticles achieved comparable reduction in bacteraemia, with the optimized batch exhibiting lower variation in bacteraemia than the pure drug.
 Conclusion: Erythromycin microparticles have been successfully optimized with the aid of bioassay methods which has the advantage that only the bioactive drug concentration is factored in. This method eliminates problems posed by inadequate or non-discriminating chemical assay methods.
 Keywords: Microparticles, Erythromycin, Gastrointestinal, Bioavailability Antimicrobial, Bioactivity, Encapsulation
Highlights
Erythromycin is an insoluble drug used in many infectious disease conditions including atypical pneumonia [1,2,3]
Three endothermic peaks (Fig. 3) were observed in the thermogram of the erythromycin-loaded microparticles. These peaks represent the components of the microparticles including erythromycin and stearic acid
The appearance of the peak of erythromycin in the formulation thermogram shows that the erythromycin is dispersed in the stearic acid matrix and the microparticles exists more as solid suspensions since the peak of erythromycin was still very much pronounced in the microparticles thermogram
Summary
Erythromycin is an insoluble drug used in many infectious disease conditions including atypical pneumonia [1,2,3]. In addition to poor solubility, erythromycin is unstable, requiring storage at low temperatures. Being basic, it is protonated at low pH, which causes loss of activity. It is protonated at low pH, which causes loss of activity This instability has been associated with gastrointestinal side effects and hepatotoxicity [46]. It has an unpleasant taste, and a rather low half-life of 1.5 h [3].
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