2. Academic Validation
  3. Physicochemical Characterization, Molecular Docking, and In Vitro Dissolution of Glimepiride-Captisol Inclusion Complexes

Physicochemical Characterization, Molecular Docking, and In Vitro Dissolution of Glimepiride-Captisol Inclusion Complexes

  • ACS Omega. 2020 Aug 4;5(32):19968-19977. doi: 10.1021/acsomega.0c01228.
Arpita Pal 1,  Sudeep Roy 2,  Akhil Kumar 3,  Syed Mahmood 4 5,  Nasrin Khodapanah 6,  Sabu Thomas 7,  Christian Agatemor 8,  Kajal Ghosal 1
Affiliations

Affiliations

  • 1 Dr. B. C. Roy College of Pharmacy and AHS, Durgapur 713206, India.
  • 2 Department of Biomedical Engineering, Faculty of Electrical Engineering and Communication, Brno University of Technology, 61600 Brno, Czech Republic.
  • 3 Department of Biotechnology, CSIR-CIMAP Kukrail Picnic Spot, Lucknow 226015, India.
  • 4 Department of Pharmaceutical Engineering, Faculty of Chemical and Process Engineering Technology, University Malaysia Pahang, Gambang 26300, Malaysia.
  • 5 Centre of Excellence for Advanced Research in Fluid Flow (CARIFF), University Malaysia Pahang, Gambang 26300, Malaysia.
  • 6 Faculty of Engineering Technology, University Malaysia Pahang, Gambang 26300, Malaysia.
  • 7 International and Inter-University Center for Nanoscience and Nanotechnology (IIUCNN), Mahatma Gandhi University, Priyadarshini Hill, Kottayam 686560, Kerala, India.
  • 8 Department of Biomedical Engineering, School of Medicine, Johns Hopkins University, Baltimore 21231, United States.
PMID: 32832751 DOI: 10.1021/acsomega.0c01228
Abstract

This present study investigated the effect of Captisol, a chemically modified cyclodextrin, on the in vitro dissolution of glimepiride. We prepared glimepiride-Captisol complexes of different mass ratios (1:1, 1:2, and 1:3 w/w) by a physical mixing or freeze-drying technique, and found that complexation with Captisol enhanced the water solubility of glimepiride. Molecular docking and dynamic simulation predicted complex formation; at the same time, Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, and scanning electron microscope indicated molecular interactions that support complexation. We also found that an inclusion complex was better than a physical mixture in enhancing the complexation of glimepiride with Captisol and enhancing water solubility. Phase solubility study of the glimepiride-Captisol complex showed an AL-type profile, implying the formation of a 1:1 inclusion complex. The study also revealed that pH influenced the stability of the complex because the stability constant of the glimepiride-Captisol complex was higher in distilled water of pH ∼6.0 than in phosphate buffer of pH 7.2.

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