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ORIGINAL RESEARCH article

Front. Chem.
Sec. Nanoscience
Volume 12 - 2024 | doi: 10.3389/fchem.2024.1449380

Formulation and characterization of cholesterol and stearic acidbased nanoparticles of gabapentin protecting from retinal injury

Provisionally accepted
Hatem Mokhtar Hatem Mokhtar 1*Dina Khodeer Dina Khodeer 2Sharifa Alzahrani Sharifa Alzahrani 3Mona Qushawy Mona Qushawy 4Reem Alshaman Reem Alshaman 4Nehal M. Elsherbiny Nehal M. Elsherbiny 4Esam S. Ahmed Esam S. Ahmed 5Mohamed K. El-kherbetawy Mohamed K. El-kherbetawy 6Ahmed R. Gardouh Ahmed R. Gardouh 2Sawsan A. Zaitone Sawsan A. Zaitone 2,4*
  • 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sinai University, Kantara, Ismailia., Egypt
  • 2 Faculty of Pharmacy, Suez Canal University, Ismaïlia, Egypt
  • 3 Faculty of Medicine, University of Tabuk, Tabuk, Tabuk, Saudi Arabia
  • 4 Faculty of Pharmacy, University of Tabuk, Tabuk, Saudi Arabia
  • 5 Department of Ophthalmology, Al-Azher Asyut Faculty of Medicine for Men, Asyut, Egypt, Asyut, Egypt
  • 6 Faculty of Medicine, Suez Canal University, Ismaïlia, Ismailia, Egypt

The final, formatted version of the article will be published soon.

    Introduction: This study aimed to prepare cholesterol and stearic acid-based solid lipid nanoparticles of gabapentin (GAB-SLNs) for protection against streptozotocin (STZ)-induced retinal injury in rats. Methods: We prepared four preparations of GAB-SLNs using a hot high-shear homogenization ultrasonication process, and the best formulation was selected and tested for biological activity. The retinal injury was brought in male adult albino rats while gabapentin doses continued for six weeks. Six groups of rats were assigned as the vehicle, diabetic, diabetic + gabapentin (10-20mg/kg), and diabetic + GAB-SLNs (10-20mg/kg). GAB-SLN#2 was selected as the optimized formulation with high entrapment efficacy (EE%, 98.64±1.97%), small particle size (185.65±2.41nm), high negative Zeta potential (-32.18±0.98 mV), low polydispersity index (0.28±0.02), and elevated drug release (99.27±3.48%). The TEM image of GAB-SLN#2 revealed a smooth surface with a spherical shape. Results: GAB-SLNs provided greater protection against retinal injury than free gabapentin as indicated by the histopathology data which demonstrated more organization of retinal layers and less degeneration in ganglion cell layer in rats treated with GAB-SLN#2.Further, GAB-SLN#2 reduced the inflammatory proteins (IL-6/JAK2/STAT3) and vascular endothelial growth factor (VEGF). Conclusion: The preparation of GAB-SLNs enhanced the physical properties of gabapentin and improved its biological activity as a neuroprotectant.Further studies are warranted to validate this technique for the use of oral gabapentin in other neurological disorders.

    Keywords: gabapentin, IL6/JAK2/STAT3 signaling, Retinal injury, rat, Solid lipid nanoparticles

    Received: 14 Jun 2024; Accepted: 27 Sep 2024.

    Copyright: © 2024 Mokhtar, Khodeer, Alzahrani, Qushawy, Alshaman, Elsherbiny, Ahmed, El-kherbetawy, Gardouh and Zaitone. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

    * Correspondence:
    Hatem Mokhtar, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sinai University, Kantara, Ismailia., Egypt
    Sawsan A. Zaitone, Faculty of Pharmacy, University of Tabuk, Tabuk, 71421, Saudi Arabia

    Disclaimer: All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.