Sharadha M, Vishal Gupta N, Rahamathulla Mohamed, Muqtader Ahmed Mohammed, Ayesha Farhana Syeda, Osmani Riyaz Ali M, Veeranna Balamuralidhara, Koteshwara K B
Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education and Research (JSS AHER), Mysuru-570015, Karnataka, India.
Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education and Research (JSS AHER), Mysuru-570015, Karnataka, India.
Int J Pharm. 2023 Nov 5;646:123443. doi: 10.1016/j.ijpharm.2023.123443. Epub 2023 Sep 23.
The expression of inflammatory markers and vascular endothelial growth factor (VEGF) was found to be upregulated in various posterior ocular disorders, including diabetic retinopathy (DR). Effective delivery of therapeutic agents to the retina poses a significant challenge in ophthalmic drug delivery due to biological ocular barriers. Triamcinolone acetonide (TA) was selected as the model corticosteroid drug targeting cytokines and VEGF in DR. However, despite TA's low molecular weight and hydrophobicity, which enable it to bypass the conjunctival epithelial barrier, it doesn't efficiently exert its effect at the target site. Nanocarriers have emerged as a solution to enhance drug delivery to the retina and improve bioavailability. This study aimed to compare the effects of Triamcinolone-loaded cubic liquid crystalline nanoparticles (TA-cubic LCNPs) and TA-Suspension in an experimental DR model administered via the subconjunctival (SCJ) route. The results demonstrated that TA-cubic LCNPs enhanced TA periocular delivery efficacy by reducing inflammatory and VEGF markers through the advanced glycation end products (AGE)/protein kinase C pathway. They were identified as promising nano-carriers, exhibiting potential for targeted delivery to the retina.
研究发现,在包括糖尿病视网膜病变(DR)在内的各种后部眼部疾病中,炎症标志物和血管内皮生长因子(VEGF)的表达上调。由于眼部生物屏障的存在,将治疗药物有效递送至视网膜在眼科药物递送中构成了重大挑战。曲安奈德(TA)被选为针对DR中细胞因子和VEGF的模型皮质类固醇药物。然而,尽管TA分子量低且具有疏水性,使其能够绕过结膜上皮屏障,但它在靶位点并不能有效地发挥作用。纳米载体已成为一种增强药物递送至视网膜并提高生物利用度的解决方案。本研究旨在比较通过结膜下(SCJ)途径给药的载曲安奈德立方液晶纳米粒(TA-立方LCNPs)和TA混悬液在实验性DR模型中的效果。结果表明,TA-立方LCNPs通过晚期糖基化终产物(AGE)/蛋白激酶C途径降低炎症和VEGF标志物,从而增强了TA的眼周递送效果。它们被确定为有前景的纳米载体,具有靶向递送至视网膜的潜力。