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Costabile, Gabriella; Gasteyer, Kathrin I.; Nadithe, Venkatereddy; Denburgh, Katherine van; Lin, Qian; Sharma, Shiv; Reineke, Joshua J.; Firestine, Steven M.; Merkel, Olivia M. (2018): Physicochemical and In Vitro Evaluation of Drug Delivery of an Antibacterial Synthetic Benzophenone in Biodegradable PLGA Nanoparticles. In: Aaps Pharmscitech, Vol. 19, No. 8: pp. 3561-3570
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Abstract

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