Development and evaluation of vildagliptin-loaded nanoemulsion for enhancement of permeability and oral bioavailability

Heena Mahurkar*, Vikash Gupta

Ravishankar College of Pharmacy, Bypass Road, Bhanpur Square, Bhopal, Madhya Pradesh, India

Refer this article

Heena Mahurkar, Vikash Gupta, 2026. Development and evaluation of vildagliptin-loaded nanoemulsion for enhancement of permeability and oral bioavailability. Journal of medical pharmaceutical and allied sciences, V 15, I 3, Pages 71 – 79. Doi: https://doi.org/10.55522/jmpas.V15I3.7087.

ABSTRACT

Type 2 Diabetes Mellitus (T2DM) is a chronic metabolic disorder characterized by impaired insulin secretion and insulin resistance, resulting in persistent hyperglycemia. Vildagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, is widely used for the management of T2DM. However, enhancement of its permeability and oral bioavailability may further improve its therapeutic performance. Nanoemulsion-based drug delivery systems have emerged as a promising approach for enhancing drug solubility, permeability, and absorption. The present study aimed to develop and evaluate a Vildagliptin-loaded nanoemulsion for enhancing permeability and oral bioavailability following oral administration. Vildagliptin nanoemulsions were prepared using the spontaneous emulsification method employing Capryol 90 as the oil phase, Tween 80 as the surfactant, and Transcutol P as the co-surfactant. Preformulation studies including solubility analysis, partition coefficient determination, and FTIR compatibility studies were performed. Various formulations (F1–F6) were prepared and optimized based on Smix ratio and oil concentration. The formulations were evaluated for physical appearance, droplet size, polydispersity index (PDI), zeta potential, drug content, pH, viscosity, refractive index, and percentage transmittance. In vitro drug release studies, release kinetics, ex vivo permeability studies using goat intestinal membrane, and stability studies were also conducted. Among all formulations, F5 was identified as the optimized batch. The optimized nanoemulsion exhibited a droplet size of 76.8 ± 1.2 nm, PDI of 0.164, zeta potential of −32.4 mV, drug content of 98.52%, and transmittance of 98.8%. The formulation demonstrated 96.8% cumulative drug release within 12 hours. Release kinetic analysis indicated that drug release followed the Korsmeyer–Peppas model (R⊃2; = 0.991). Ex vivo permeability studies revealed a 2.9-fold enhancement in permeability compared to pure drug suspension. Stability studies confirmed the physical and chemical stability of the optimized formulation without significant changes in formulation characteristics. The developed Vildagliptin nanoemulsion successfully enhanced drug release and intestinal permeability, indicating its potential to improve oral bioavailability. The optimized formulation exhibited desirable physicochemical properties, excellent stability, and superior performance compared to conventional drug formulations. Therefore, nanoemulsion technology represents a promising strategy for improving the oral delivery and therapeutic efficacy of Vildagliptin in the management of Type 2 Diabetes Mellitus.

Keywords:

Vildagliptin, Nanoemulsion, Oral Bioavailability, Permeability Enhancement, DPP-4 Inhibitor, Type 2 Diabetes Mellitus, Spontaneous emulsification.

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