Work

Preservative-free electrospun nanofibrous inserts for sustained delivery of ceftazidime; design, characterization and pharmacokinetic investigation in rabbit's eye

Year: 2024

Type: article

Abstract: Ocular drug delivery presents significant challenges, attributed to the various anatomical and physiological barriers, as well as the limitations associated with conventional ocular formulations including low bioavailability, necessitating frequent dosing. The objective of the essay was to design sustained release nanofibrous inserts loaded with ceftazidime (CAZ), an antibiotic effective against gram-negative and gram-positive microorganisms, for the treatment of ocular infections. These nanofibers were fabricated using the electrospinning technique, employing biodegradable polymers such as polyvinyl alcohol (PVA), polycaprolactone (PCL) and Eudragit® (EUD). The nanofibrous inserts exhibited adequate mechanical strength for ocular use with an average diameter < 250 nm. In the initial 12-h period, a burst drug release was observed, followed by a controlled release for 120 h. Cell viability test confirmed the non-toxicity and safety of the nanofibers. The in vivo study demonstrated that the inserts sustain a drug concentration exceeding the minimum inhibitory concentration (MIC) of Pseudomonas aeruginosa and Staphylococcus aureus for 4 and 5 days, respectively. The AUC 0 – 120 for CAZ-PVA-PCL was reported 11,882.81 ± 80.5 μg·h/ml and for CAZ-PVA-EUD was 9649.39 ± 86.84 μg·h/ml. The nanofibrous inserts' extended drug release maintains effective antimicrobial concentrations, avoids the fluctuations of eye drops, and, by being preservative-free, eliminates cytotoxicity. • Ceftazidime-loaded nanofibers were fabricated by electrospinning using polyvinyl alcohol, polycaprolactone, and Eudragit. • The sustained-release nanofibrous inserts exhibited sufficient mechanical strength for ocular use. • In vivo study showed that the inserts maintained drug levels above the minimum inhibitory concentration for about 5 days. • Extended drug release from the preservative-free inserts avoids eye drop fluctuations and eliminates cytotoxicity.

Source: International Journal of Pharmaceutics X

DOI: 10.1016/j.ijpx.2024.100297

Authors: Shiva Taghe, Shahla Mirzaeei

Institution: Kermanshah University of Medical Sciences

Language: English

Topic: Advanced Drug Delivery Systems

Subfield: Pharmaceutical Science

Field: Pharmacology, Toxicology and Pharmaceutics

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: gold

Estimated APC paid: $2,700