Development of surface modified nanoparticles of curcumin for topical treatment of diabetic retinopathy: In vitro, ex vivo and in vivo investigation

体内 PLGA公司 姜黄素 糖尿病性视网膜病变 药理学 离体 粒径 化学 析因实验 纳米颗粒 材料科学 色谱法 体外 生物医学工程 医学 纳米技术 糖尿病 生物化学 数学 生物 内分泌学 生物技术 物理化学 统计
作者
Umesh D. Laddha,Sanjay J. Kshirsagar,Layba S. Sayyad,Musab T. Ahmed,Sachin S. Gaikwad,Pavan B. Udavant,Abhijeet D. Kulkarni
出处
期刊:Journal of Drug Delivery Science and Technology [Elsevier]
卷期号:76: 103835-103835 被引量:6
标识
DOI:10.1016/j.jddst.2022.103835
摘要

Diabetic retinopathy (DR) is the worst microvascular complication of diabetes that results in blindness. Present treatment of DR is invasive and associated with pain and inflammation. There is a need to develop painless treatment. The surface-modified PLGA (50:50) nanoparticles of Curcumin, which is a peroxisome proliferator-activated receptor-gamma agonist, were prepared to target DR by topical administration. Nanoparticles were optimized by a 32 factorial design. The Concentration of PLGA and number of HPH cycles at fixed pressure were independent variables whereas particle size. PDI and % entrapment efficiency were the dependent variables. Batch F6 with particle size, PDI, and % EE 194.7 nm, 0.231, and 90% respectively was selected as the optimized batch. The optimized batch was further subjected to spray drying and evaluated for various parameters. Residual solvent analysis was carried out by Gas chromatography. In vitro drug release study showed a biphasic drug release pattern of 70.17 ± 1.38% cumulative drug release at the end of 10 h. The release profile of curcumin from nanoparticles appeared to fit best with the Higuchi model. XRD study confirmed the molecular dispersion of the drug. The formulation showed satisfactory results in sterility testing, histology and isotonicity testing. In vivo study on rats showed dose dependent reduction in vascular endothelial growth factor (VEGF) concentration in vitreous fluid. Based on available evidences it can be concluded that the prepared formulation possesses great potential to manage diabetic retinopathy.
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