Optimization of Glyburide-Loaded Nanosuspensions via Ball Milling and Homogenization Techniques: A Central Composite Design Approach for Enhanced Solubility.
Damla Gungor, Eren Aytekin, Yagmur Akdag, Selma Sahin, Tugba Gulsun
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Abstract
Introduction: Glyburide is a drug for the treatment of diabetes mellitus and has a potential effect on Alzheimer's disease. It is also a BCS Class 2 drug with low solubility and low permeability. Developing a nanosuspension formulation and increasing the solubility and dissolution rate of glyburide is required to overcome this challenge.
Methods: Thus, the goal of this work was to create glyburide nanosuspensions by ball milling and homogenizing glyburide to increase its solubility and rate of dissolution. To achieve this, the nanosuspension formulation was optimized using a central composite design. Zeta potential, particle size distribution and solubility were selected by way of dependent variables, and ball milling time, homogenization cycles, and Pluronic F-127/glyburide ratio were chosen as independent variables. Glyburide nanosuspensions were obtained with a particle size of 244.6 ± 2.685 nm. In vitro release and solubility studies were conducted following optimization.
Results: The saturation solubility of glyburide was nearly doubled as a result of the nanocrystal formation. Xray diffraction (XRD), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier-transform infrared spectroscopy (FT-IR) were used to assess the nanosuspension. SEM images confirmed that the nanocrystal formation process was successful. Glyburide and the excipients have no incompatibilities, their physical states have not changed, and the preparation method has not affected the stability of glyburide, according to DCS, XRD, and FT-IR analyses.
Conclusion: These studies indicated that a combination of ball milling and homogenization techniques significantly enhanced the solubility of glyburide and its release from the formulation. Consequently, this approach can be applied to formulations characterized by low absorption and limited bioavailability.
期刊介绍：
Current Pharmaceutical Design publishes timely in-depth reviews and research articles from leading pharmaceutical researchers in the field, covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area guest edited by an acknowledged authority in the field.
Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design including: medicinal chemistry, pharmacology, drug targets and disease mechanism.
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