Evaluation of single-dose inhalation of clarithromycin-loaded solid lipid nanoparticles in rat model

Authors : Namık Bilici, İlknur Kulcanay Şahin, Ömer Ersoy, Mustafa Cengiz, Nurullah Özdemir, Rıfat Ertekin, Adnan Ayhancı

Pages : 31-41

Doi:10.58605/bingolsaglik.1594508

View : 43 | Download : 45

Publication Date : 2025-04-26

Article Type : Review Paper

Abstract :This study aimed to explore the effective utilization of clarithromycin (CLA) through the development of clarithromycin-loaded solid lipid nanoparticles (CLA-loaded SLN), designed for nebulizer-based delivery for the first time. Wistar albino rats were divided into seven groups (n=8) based on time points (0.5, 1, 2, 4, 12, 24 hours, and a control group). At the respective time points, lung tissues and blood samples were collected and analyzed for CLA concentrations using HPLC-MS/MS. The maximum serum concentration (Cmax) was 6.74 µg/mL, with average serum CLA concentrations of 5.06, 2.5, 2.18, 1.13, and 0.5 µg/mL across the groups. CLA was undetectable in the control group and in the serum of the last group. Using the linear trapezoidal method (LTM), the area under the curve (AUC 0-24) for serum CLA was calculated as 17.06 µg*h/mL. Significant differences (p<0.001) were observed between several groups in serum CLA levels. In lung tissue, the highest Cmax was 2.66 µg/g, with average concentrations of 1.99, 1.8, 1.76, 0.36, 0.14, and 0.04 µg/g. The AUC for lung CLA concentration was 7.43 µg*h/g. These findings indicate that inhalation of CLA-loaded SLN achieves adequate plasma concentrations and sustained lung tissue levels for up to 12 hours post-inhalation. However, serum CLA levels were undetectable after 12 hours. Accurate characterization may facilitate CLA\\\'s application as an inhalable therapy.
Keywords : Klaritromisin, Klaritromisin aerosol, İlaç maruziyeti, Tek doz farmakokinetiği, Katı lipid nanopartikül inhaler ilacı