کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2083286 1545329 2015 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Intracellular delivery of dendrimer triamcinolone acetonide conjugates into microglial and human retinal pigment epithelial cells
ترجمه فارسی عنوان
تحویل داخل سلولی تجمع تریامسینولون استون به سلول های اپیتلیال
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی بیوتکنولوژی یا زیست‌فناوری
چکیده انگلیسی


• Dendrimer-triamcinolone acetonide conjugates were prepared with high drug pay load.
• D-TA conjugates showed superior solubility compared to free TA.
• The conjugates enhance the intracellular entry and delivery of drugs.
• D-TA conjugates demonstrate enhanced anti-inflammatory and anti-angiogenic properties.
• Potential therapeutic vehicle for the treatment of retinal diseases..

Triamcinolone acetonide (TA) is a potent, intermediate-acting, steroid that has anti-inflammatory and anti-angiogenic activity. Intravitreal administration of TA has been used for diabetic macular edema, proliferative diabetic retinopathy and exudative age-related macular degeneration (AMD). However, the hydrophobicity, lack of solubility, and the side effects limit its effectiveness in the treatment of retinal diseases. In this study, we explore a PAMAM dendrimer-TA conjugate (D-TA) as a potential strategy to improve intracellular delivery and efficacy of TA to target cells. The conjugates were prepared with a high drug payload (∼21%) and were readily soluble in saline. Compared to free TA, D-TA demonstrated a significantly improved toxicity profile in two important target [microglial and human retinal pigment epithelium (RPE)] cells. The D-TA was ∼100-fold more effective than free TA in its anti-inflammatory activity (measured in microglia), and in suppressing VEGF production (in hypoxic RPE cells). Dendrimer-based delivery may improve the efficacy of TA towards both its key targets of inflammation and VEGF production, with significant clinical implications.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutics and Biopharmaceutics - Volume 95, Part B, September 2015, Pages 239–249
نویسندگان
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