ENHANCED BIOAVAILABILITY OF LOBEGLITAZONE VIA DISSOLVING MICRONEEDLE PATCHES IN RATS
DOI:
https://doi.org/10.22159/ijap.2025v17i5.54818Keywords:
Lobeglitazone, Dissolving microneedles, Pharmacokinetics, Transdermal delivery, LC-MS/MS, Type 2 diabetesAbstract
Objective: To compare the pharmacokinetics of lobeglitazone administered via oral suspension and transdermal dissolving microneedle array (DMNA) patch in rats using a validated LC-MS/MS method.
Methods: Male Wistar rats were administered a single 0.5 mg/kg dose of lobeglitazone either orally or via a DMNA patch. Plasma samples were collected at predefined intervals up to 48 h. Lobeglitazone concentrations were analyzed using a validated LC-MS/MS method. Pharmacokinetic parameters, including Cmax, Tmax, AUC₀–t, AUC₀–∞, elimination rate constant (Kel), and half-life (T₁/₂) were calculated and statistically compared between the groups.
Results: Oral administration resulted in a higher Cmax (1786.25 ± 66.68 ng/ml) and a shorter Tmax (2.67 ± 0.52 h), while DMNA delivery produced a lower Cmax (1207.69 ± 25.70 ng/ml) and a delayed Tmax (5.33 ± 1.03 h). However, systemic exposure was significantly higher in the DMNA group (AUC₀–∞: 24,250.57 ± 650.92 ng·h/ml) compared to the oral group (12,036.84 ± 860.47 ng·h/ml; p < 0.00001). The DMNA group also exhibited an extended half-life (10.13 ± 0.34 h) relative to oral administration (4.85 ± 0.60 h). The calculated relative bioavailability of the DMNA formulation was 201.47%, indicating enhanced systemic exposure.
Conclusion: Transdermal DMNA delivery of lobeglitazone significantly enhances bioavailability and prolongs systemic retention compared to oral administration. These findings suggest that DMNA patches represent a promising, patient-friendly alternative for the sustained delivery of lobeglitazone in the chronic management of type 2 diabetes mellitus.
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Copyright (c) 2025 SUKANTA ROY, BALARAM GHOSH, ANANYA CHANDRA, DIBYA DAS, PARAG GHOSH, SANGEETA CHOUDHURY, ANIRBANDEEP BOSE, SUBAS CHANDRA DINDA
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