Milena Koch, Dominika Stencel, Dorota Małgorzata Wrześniok

Potential formulations and routes of administration of tigecycline in the face of increasing bacterial resistance and off-label use

2025-09-12

Research Subject. Tigecycline is the first antimicrobial drug classified in the new generation of tetracycline antibiotics - glycylcyclines. It has improved antibacterial activity, especially against multidrug-resistant strains. It is approved to treat complicated skin and skin structure infections, complicated intra-abdominal infections, and community-acquired pneumonia. The only available route of its administration is through intravenous infusion, which sometimes leads to higher toxicity and lack of effectiveness of antibiotic therapy.

Research Object. The aim of this study was to present new possible formulations and routes of administration for tigecycline with potential advantages in light of growing bacterial resistance and off-label use.

Material and Methods. A literature review was made through Google Scholar and PubMed databases, based on the following keywords: “tigecycline”, “formulation”, “bacterial resistance”, and “off-label use”. The conducted review consists of scientific articles in the field of pharmacy and medicine, mainly from 2020–2025, and a few older papers to supplement the topic. The article also contains two websites.

Results. Tigecycline, apart from FDA indications, can be used off-label to treat various bacterial infections, such as urinary tract infections, infections caused by Clostridium difficile, intracranial infections, or bloodstream infections. Currently, there is no officially registered formulation of tigecycline that could be applied locally or provide targeted therapy. Latest studies show a potential new possibility to treat intracranial infections through tigecycline-based nanoparticles or their intraventricular or intracranial administration. Tigecycline also has the potential to be used as an inhalable dry powder in case of mycobacteriosis. Wound dressings made of tigecycline-chitosan composite are promising options to treat and prevent bacterial infections caused by Staphylococcus aureus. On the other hand, adding excipients can improve the stability and bioavailability of tigecycline.

Conclusions. Tigecycline is an important antibiotic in the treatment of infections caused by multi-drug resistant strains, due to its wide-spectrum antibacterial activity. Growing bacterial resistance and the need to increase the comfort of pharmacotherapy lead to the creation of the new formulations or routes of administration of tigecycline. Proposed new therapeutical options present promising antibacterial effectiveness, better bioavailability and biocompatibility, and better pharmacokinetic parameters. However, more in vivo studies are required to confirm the efficacy of the mentioned formulations in humans.

Keywords: tigecycline, excipients, off-label use, nanoparticles.

© Farm Pol, 2025, 81(1): 15–23