作者: Gabriella Costabile , Kathrin I. Gasteyer , Venkatereddy Nadithe , Katherine Van Denburgh , Qian Lin
DOI: 10.1208/S12249-018-1187-9
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摘要: Due to the increasing incidents of antimicrobial-resistant pathogens, development new antibiotics and their efficient formulation for suitable administration is crucial. Currently, one group promising antimicrobial compounds are benzophenone tetra-amides which show good activity even against gram-positive, drug-resistant pathogens. These suffer from poor water solubility bioavailability. It therefore important develop dosage forms can address this disadvantage while also maintaining efficacy potentially generating long-term exposures minimize frequent dosing. Biodegradable nanoparticles provide solution, we describe here encapsulation experimental benzophenone-based antibiotic, SV7. Poly-lactic-co-glycolic-acid (PLGA) were optimized physicochemical properties, efficiency, sustained drug release as well activity. The contained particles smaller than 200 nm with a slightly negative zeta potential released 39% load over 30 days. This maintains antibacterial SV7 minimizing impact on mammalian cells.