Trimethoprim-Loaded Microspheres Prepared from Low-Molecular-Weight PLGA as a Potential Drug Delivery System for the Treatment of Urinary Tract Infections

Bernhard Brauner; Caroline Schuster; Michael Wirth; Franz Gabor

doi:10.1021/acsomega.0c00981

Trimethoprim-Loaded Microspheres Prepared from Low-Molecular-Weight PLGA as a Potential Drug Delivery System for the Treatment of Urinary Tract Infections

ACS Omega. 2020 Apr 7;5(15):9013-9022. doi: 10.1021/acsomega.0c00981. eCollection 2020 Apr 21.

Authors

Bernhard Brauner¹, Caroline Schuster¹, Michael Wirth¹, Franz Gabor¹

Affiliation

¹ Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Althanstraße 14, 1090 Vienna, Austria.

Abstract

Commonly, therapy of urinary tract infections suffers from increasing resistance to antibiotics and the ability of uropathogenic Escherichia coli (UPEC) to invade bladder cells and cause recurring infections. As an alternative strategy for instillation into the bladder, trimethoprim-loaded microparticles with poly(d,l-lactic-co-glycolic acid) (PLGA) as a matrix were prepared. To reduce particle loss by washout, their surface was grafted with bioadhesive wheat germ agglutinin, providing biomimicry akin to UPEC. Since PLGA 503H has shown a slow drug release profile, the low-molecular-weight PLGA 2300 was studied. Whereas the drug loading of PLGA 503H particles amounted to 2.8%, the drug content of PLGA 2300 particles was twice as high. Although the drug release pattern started with an initial burst of 30% after 24 h for both PLGA types, half of the trimethoprim content was released after 4 days from PLGA 503H microparticles as opposed to 2 days in the case of PLGA 2300. Higher drug loading and accelerated release render PLGA 2300 a viable alternative to PLGA 503H.