PMID- 32081799 OWN - NLM STAT- MEDLINE DCOM- 20201229 LR - 20201229 IS - 1873-3476 (Electronic) IS - 0378-5173 (Linking) VI - 579 DP - 2020 Apr 15 TI - Micro vs. nano: PLGA particles loaded with trimethoprim for instillative treatment of urinary tract infections. PG - 119158 LID - S0378-5173(20)30142-3 [pii] LID - 10.1016/j.ijpharm.2020.119158 [doi] AB - Recurring infections and increasing resistances continue to complicate treatment of urinary tract infections. To investigate alternative treatment options, trimethoprim loaded micro- (D[4;3] of 1-9 microm) and nanoparticles (Z-Avg of 200-400 nm) were prepared from two types of poly(d,l-lactic-co-glycolic acid) (PLGA) for instillative therapy. While PLGA 503H microparticles could not be loaded with more than 2.6% trimethoprim, PLGA 2300 entrapped 22%. When preparing nanoparticles, both types displayed an even higher drug load of up to 29% using PLGA 2300, while PLGA 503H drug load stagnated at 10%. After eight hours, drug release from microparticles amounted to 55% (503H) and 35% (2300) whereas total drug release occurred after 8 (503H) and 9 days (2300). In case of nanoparticles, trimethoprim was liberated much faster with 60% after 2 h and a complete release after 24 h from both polymers. PLGA 2300 seems to be the better choice for entrapment of trimethoprim in microparticles considering the drug load. Both polymers, however, seem to be viable options for nanoparticles. Due to the higher overall drug load, nanoparticles seem to be advantageous over microparticles for instillative therapy, especially when prepared with PLGA 2300. CI - Copyright (c) 2020 Elsevier B.V. All rights reserved. FAU - Brauner, Bernhard AU - Brauner B AD - Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Althanstrasse 14, 1090 Vienna, Austria. FAU - Schwarz, Patrik AU - Schwarz P AD - Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Althanstrasse 14, 1090 Vienna, Austria. FAU - Wirth, Michael AU - Wirth M AD - Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Althanstrasse 14, 1090 Vienna, Austria. FAU - Gabor, Franz AU - Gabor F AD - Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Althanstrasse 14, 1090 Vienna, Austria. Electronic address: franz.gabor@univie.ac.at. LA - eng PT - Journal Article DEP - 20200217 PL - Netherlands TA - Int J Pharm JT - International journal of pharmaceutics JID - 7804127 RN - 0 (Drug Carriers) RN - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer) RN - AN164J8Y0X (Trimethoprim) SB - IM MH - Administration, Intravesical MH - Drug Carriers MH - Drug Liberation MH - Drug Stability MH - *Microspheres MH - Nanoparticles/administration & dosage/*chemistry/ultrastructure MH - Particle Size MH - Polylactic Acid-Polyglycolic Acid Copolymer/administration & dosage/*chemistry MH - Time Factors MH - Trimethoprim/administration & dosage/*chemistry MH - Urinary Tract Infections/drug therapy OTO - NOTNLM OT - Instillative therapy OT - Microparticles OT - Nanoparticles OT - PLGA OT - Trimethoprim OT - Urinary tract infection COIS- Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. EDAT- 2020/02/23 06:00 MHDA- 2020/12/30 06:00 CRDT- 2020/02/22 06:00 PHST- 2019/12/05 00:00 [received] PHST- 2020/02/11 00:00 [revised] PHST- 2020/02/16 00:00 [accepted] PHST- 2020/02/23 06:00 [pubmed] PHST- 2020/12/30 06:00 [medline] PHST- 2020/02/22 06:00 [entrez] AID - S0378-5173(20)30142-3 [pii] AID - 10.1016/j.ijpharm.2020.119158 [doi] PST - ppublish SO - Int J Pharm. 2020 Apr 15;579:119158. doi: 10.1016/j.ijpharm.2020.119158. Epub 2020 Feb 17.