Formulation and characterization of cholesterol-based nanoparticles of gabapentin protecting from retinal injury.

IF 3.8 3区化学 Q2 CHEMISTRY, MULTIDISCIPLINARY Frontiers in Chemistry Pub Date : 2024-10-21 eCollection Date: 2024-01-01 DOI:10.3389/fchem.2024.1449380

Hatem I Mokhtar, Dina M Khodeer, Sharifa Alzahrani, Mona Qushawy, Reem Alshaman, Nehal M Elsherbiny, Esam Sayed Ahmed, Esam Ghanem Abu El Wafa, Mohamed K El-Kherbetawy, Ahmed R Gardouh, Sawsan A Zaitone

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Abstract

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 6 weeks. Six groups of rats were assigned as the vehicle, diabetic, diabetic + gabapentin (10-20 mg/kg), and diabetic + GAB-SLNs (10-20 mg/kg). GAB-SLN#2 was selected as the optimized formulation with high entrapment efficacy (EE%, 98.64% ± 1.97%), small particle size (185.65 ± 2.41 nm), 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.

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保护视网膜免受损伤的加巴喷丁胆固醇基纳米颗粒的制备和表征。

引言：本研究旨在制备基于胆固醇和硬脂酸的加巴喷丁固体脂质纳米颗粒（GAB-SLNs），以防止链脲佐菌素（STZ）诱导的大鼠视网膜损伤：我们采用热高剪切匀浆超声工艺制备了四种 GAB-SLNs 制剂，并选择了最佳制剂进行生物活性测试。对雄性成年白化大鼠进行视网膜损伤，同时持续服用加巴喷丁 6 周。六组大鼠被分配为载体组、糖尿病组、糖尿病+加巴喷丁（10-20 mg/kg）组和糖尿病+GAB-SLNs（10-20 mg/kg）组。GAB-SLN#2 被选为优化制剂，它具有较高的夹持效力（EE%，98.64% ± 1.97%）、较小的粒径（185.65 ± 2.41 nm）、较高的负 Zeta 电位（-32.18 ± 0.98 mV）、较低的多分散指数（0.28 ± 0.02）和较高的药物释放率（99.27% ± 3.48%）。GAB-SLN#2 的 TEM 图像显示其表面光滑，呈球形：组织病理学数据表明，GAB-SLNs 比游离加巴喷丁能更好地保护大鼠免受视网膜损伤，GAB-SLN#2 治疗后的大鼠视网膜层组织更多，神经节细胞层退化更少。此外，GAB-SLN#2 还能减少炎症蛋白（IL-6/JAK2/STAT3）和血管内皮生长因子（VEGF）：结论：GAB-SLNs 的制备增强了加巴喷丁的物理性质，提高了其作为神经保护剂的生物活性。我们有必要开展进一步研究，以验证该技术在其他神经系统疾病中口服加巴喷丁的有效性。

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来源期刊

Frontiers in Chemistry Chemistry-General Chemistry

CiteScore

8.50

自引率

3.60%

发文量

1540

审稿时长

12 weeks

期刊介绍： Frontiers in Chemistry is a high visiblity and quality journal, publishing rigorously peer-reviewed research across the chemical sciences. Field Chief Editor Steve Suib at the University of Connecticut is supported by an outstanding Editorial Board of international researchers. This multidisciplinary open-access journal is at the forefront of disseminating and communicating scientific knowledge and impactful discoveries to academics, industry leaders and the public worldwide. Chemistry is a branch of science that is linked to all other main fields of research. The omnipresence of Chemistry is apparent in our everyday lives from the electronic devices that we all use to communicate, to foods we eat, to our health and well-being, to the different forms of energy that we use. While there are many subtopics and specialties of Chemistry, the fundamental link in all these areas is how atoms, ions, and molecules come together and come apart in what some have come to call the “dance of life”. All specialty sections of Frontiers in Chemistry are open-access with the goal of publishing outstanding research publications, review articles, commentaries, and ideas about various aspects of Chemistry. The past forms of publication often have specific subdisciplines, most commonly of analytical, inorganic, organic and physical chemistries, but these days those lines and boxes are quite blurry and the silos of those disciplines appear to be eroding. Chemistry is important to both fundamental and applied areas of research and manufacturing, and indeed the outlines of academic versus industrial research are also often artificial. Collaborative research across all specialty areas of Chemistry is highly encouraged and supported as we move forward. These are exciting times and the field of Chemistry is an important and significant contributor to our collective knowledge.