AN INSIGHT INVESTIGATION ON STEADY-STATE PHARMACOKINETICS OF LOBEGLITAZONE-LOADED DISSOLVING MICRONEEDLES IN RATS
DOI:
https://doi.org/10.22159/ajpcr.2025v18i9.55996Keywords:
Dissolving microneedles, Lobeglitazone, Steady-state pharmacokinetics, Transdermal delivery, Type 2 diabetes mellitusAbstract
Objectives: This study aimed to investigate the steady-state pharmacokinetics of lobeglitazone administered through a dissolving microneedle array (DMNA) compared to conventional oral delivery in rats, addressing limitations such as first-pass metabolism and fluctuating plasma concentrations associated with oral therapy.
Methods: Lobeglitazone-loaded DMNAs were fabricated using a micromolding technique with polyvinylpyrrolidone K90 and hyaluronic acid. Structural characteristics were confirmed through SEM. Male Wistar rats were divided into two groups (n=6): oral and DMNA (0.5 mg/day for 7 days). Plasma samples were collected over a period of 216 h and analyzed using a validated liquid chromatography–mass spectrometry/mass spectrometry method. Pharmacokinetic parameters, including Cmin,ssCmax, Tmax, AUC, kel, T1/2, and mean residence time (MRT), were determined by non-compartmental analysis.
Results: DMNA administration resulted in significantly enhanced systemic exposure (AUC168–216: 26072.26±1510.30 ng·h/mL vs. 13658.04±1659.16 ng·h/mL, p<0.00001), prolonged half-life (10.05±0.68 h vs. 6.16±0.55 h), and a higher MRT (14.51±0.98 h vs. 8.88±0.80 h). The DMNA group maintained stable plasma concentrations with reduced fluctuation between peak and trough levels, indicating effective steady-state achievement and sustained drug release compared to oral delivery.
Conclusion: Dissolving microneedle-based transdermal delivery of lobeglitazone offers a superior pharmacokinetic profile over oral administration, supporting its potential in improving long-term glycemic control. Further studies are warranted to confirm efficacy and safety in clinical settings.
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Copyright (c) 2025 Sukanta Roy, Dibya Das, Jayanta Kumar Chaudhury, Kamalakanta Ray, Soumik Laha, Anirbandeep Bose, Subas Chandra Dinda

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