Preparation and optimization of chlorophene-loaded nanospheres as controlled release antimicrobial delivery systems

Chlorophene-loaded nanospheres with various formulation parameters were evaluated. The optimal formulation was found at 0.1% w/v of poloxamer 407, 15 mL of ethyl acetate and 20% initial chlorophene loading that provided the suitable size (179 nm), the highest loading content (19.2%), encapsulation efficiency (88.0%) and yield (91.6%). Moreover, encapsulation of chlorophene in nanospheres was able to prolong and sustain drug release over one month. Chlorophene-loaded nanospheres were effective against Staphylococcus aureus (S. aureus) and Candida albicans (C. albicans), the main cause of hospital-acquired infections. Chlorophene-loaded nanospheres were effective against S. aureus (>46 µg/mL) and C. albicans (>184 µg/mL). These nanospheres appeared to have profound effect on the time-dependent hemolytic activity due to gradual release of chlorophene. At the concentration of 46 µg/mL, nearly no HRBC hemolysis in 24 h compared to 80% of hemolysis from free drug. In conclusion, polymeric nanospheres were successfully fabricated to encapsulate chlorophene which can eliminate inherent toxicity of drugs and have potential uses in prolonged release of antimicrobial.