کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10162290 1114324 2014 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Peptide-Micelle Hybrids Containing Fasudil for Targeted Delivery to the Pulmonary Arteries and Arterioles to Treat Pulmonary Arterial Hypertension
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی اکتشاف دارویی
پیش نمایش صفحه اول مقاله
Peptide-Micelle Hybrids Containing Fasudil for Targeted Delivery to the Pulmonary Arteries and Arterioles to Treat Pulmonary Arterial Hypertension
چکیده انگلیسی
This study investigates the respirability and efficacy of peptide-micelle hybrid nanoparticles as carriers for inhalational therapy of pulmonary arterial hypertension (PAH). CARSKNKDC (CAR), a cell‐penetrating and lung‐homing peptide, conjugated polyethylene glycol-distearoyl‐phosphoethanolamine micelles containing fasudil, an investigational anti‐PAH drug, were prepared by solvent evaporation method and characterized for various physicochemical properties. The pharmacokinetics and pharmacological efficacy of hybrid particles containing fasudil were evaluated in healthy rats and monocrotaline‐induced PAH rats. CAR micelles containing fasudil had an entrapment efficiency of approximately 58%, showed controlled release of the drug, and were monodispersed with an average size of approximately 14 nm. Nuclear magnetic resonance scan confirmed the drug's presence in the core of peptide-micelle hybrid particles. Compared with plain micelles, CAR peptide increased the cellular uptake by approximately 1.7‐fold and extended the drug half‐life by approximately fivefold. The formulations were more prone to accumulate in the pulmonary vasculature than in the peripheral blood, which is evident from the ratio of the extent of reduction of pulmonary and systemic arterial pressures. On the whole, this study demonstrates that peptide-polymer hybrid micelles can serve as inhalational carriers for PAH therapy. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:3743-3753, 2014
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 103, Issue 11, November 2014, Pages 3743-3753
نویسندگان
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