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7th International Symposium on ADVANCES IN PHARMACEUTICAL ANALYSIS

Synthesis and Characterization of Mitiglinide Loaded β, γ-Cyclodextrins/Alginate Nanoparticles as a Novel Drug Delivery System Against Lung Cancer and Theoretical Calculation of their Inclusion Complexes

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Exploring Innovations in Pharmaceutical Analysis: The 7th International Symposium on Advances in Pharmaceutical Analysis (APA 2025)
Conference: APA 2025 – 7th International Symposium on Advances in Pharmaceutical Analysis
Dates & Venue: August 24–27, 2025 | Ankara University, Ankara, Türkiye
Organized by: Prof. Dr. Sibel A. Özkan (Conference Chair), Assoc. Prof. Mehmet Gümüştaş (Co-chair)
Official Website: https://apa2025.net
Background & Objectives

Nanotechnology has enabled innovative approaches to drug delivery, enhancing therapeutic efficacy and specificity of various pharmaceutical compounds. In this study, we focused on encapsulating the antidiabetic drug mitiglinide within nanoparticles based on beta-cyclodextrin/alginate and gamma-cyclodextrin/alginate matrices, prepared using the Ionic Gelation method. Our aim was to investigate the potential benefits of these encapsulation strategies in terms of drug delivery and anticancer effects.

Methods: The prepared nanoparticles were characterized through particle size analysis, Zeta potential measurements, and Polydispersity Index (PDI) determination. Quantification of excess mitiglinide in nanoparticles was conducted using HPLC. 
Results: The results indicated that the particle size was influenced by the concentration of mitiglinide, with the smallest particle size observed at 1% concentration for both beta-cyclodextrin/alginate and gamma-cyclodextrin/alginate nanoparticles with 81.88 nm and 129.0 nm, respectively. Negative average zeta potential values (-10 to -30 mV) demonstrated an increasing trend with mitiglinide concentration, and the low PDI values (≤0.3) suggested homogeneity in particle size distribution for most formulations.
Interaction studies were conducted through Scanning Electron Microscopy (SEM) and computational methods. The SEM images revealed distinct morphologies for different formulations, shedding light on the encapsulation process. Computational analysis highlighted the alteration of charge distribution in the encapsulated complexes, emphasizing the impact of encapsulation on the guest and host molecules.
A High-Performance Liquid Chromatography (HPLC) method was developed to accurately quantify the concentration of mitiglinide. The calibration curve exhibited high linearity (R2 = 0.9939) across a concentration range of 0.05 - 250 µg/mL, with low limits of detection (LOD) and quantification (LOQ) of 0.015 and 0.036, respectively, which means high method sensitivity.
Further, the anticancer potential of the prepared nanoparticles was evaluated against the A549 lung cancer cell line. Loaded beta-cyclodextrin/alginate nanoparticles demonstrated superior effects, displaying the lowest IC50 value (95.7 µM) compared to other formulations. Notably, loaded gamma-cyclodextrin/alginate nanoparticles exhibited a unique behavior with no observable IC50 value, potentially due to strong complexation hindering the drug's effect on cancer cells.​

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