Physicochemical and In Vitro Evaluation of Drug Delivery of an Antibacterial Synthetic Benzophenone in Biodegradable PLGA Nanoparticles.
Authors of this article are:
Costabile G Gasteyer KI Nadithe V Van Denburgh K Lin Q Sharma S Reineke JJ Firestine SM Merkel OM.
A summary of the article is shown below:
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 200 nm with a slightly negative zeta potential which released 39% of their drug load over 30 days. This formulation maintains the antibacterial activity of SV7 while minimizing the impact on mammalian cells.
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This article is a good source of information and a good way to become familiar with topics such as: PLGA nanoparticles;benzophenone antibiotics;poorly water-soluble drug;sustained release.
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