کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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2504303 | 1557456 | 2010 | 9 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Prostaglandin E1 encapsulated into lipid nanoparticles improves its anti-inflammatory effect with low side-effect Prostaglandin E1 encapsulated into lipid nanoparticles improves its anti-inflammatory effect with low side-effect](/preview/png/2504303.png)
Prostaglandin E1 (PGE1) shows various pharmacological activities including anti-inflammation. However, the rapid metabolization and inactivation of the intravenously administered PGE1 during the first passage through the lungs result in significant non-compliance in clinical trials which greatly limits its application. The aim of this work was to prepare the lipid nanoparticles loading PGE1 to improve its anti-inflammatory effect with low side-effect. The experimental results showed that PGE1 loaded lipid nanoparticles (PLNs) could be successfully prepared by high pressure homogenization with particle size 68.1 ± 4.7 nm, zeta potential −3.32 ± 0.37 mV and entrapment efficiency 92.1 ± 1.3%. PLNs exhibited a sustained release with low burst drug release. PLNs could improve the inhibition effects of PGE1 on lipopolysaccharides (LPS)-induced TNF-α expression on macrophage RAW264.7 cells, and improve the inhibition of lymphocyte to endothelial cell adhesion and ICAM-1 adhesion molecule expression on HUVEC and MDA-MB-468 cell membrane. No allergenicity, vascular and muscle irritation were induced in animals by PLNs even at double of the highest drug concentration of clinical infusion. As a result, PLNs could be a more potential delivery system for PGE1 in the treatment of inflammation-related diseases.
Journal: International Journal of Pharmaceutics - Volume 387, Issues 1–2, 15 March 2010, Pages 263–271