کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
877501 911030 2012 10 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Peptide PHSCNK as an integrin α5β1 antagonist targets stealth liposomes to integrin-overexpressing melanoma
موضوعات مرتبط
مهندسی و علوم پایه سایر رشته های مهندسی مهندسی پزشکی
پیش نمایش صفحه اول مقاله
Peptide PHSCNK as an integrin α5β1 antagonist targets stealth liposomes to integrin-overexpressing melanoma
چکیده انگلیسی

As an integrin α5β1 antagonist, N-acetyl-proline-histidine-serine-cysteine-asparagine-amide (Ac-PHSCN-NH2) is currently in phase II trials for various cancer therapies. In this study Ac-PHSCNK-NH2 (PHSCNK) was used as a novel homing peptide to prepare ligand-targeted liposomes loaded with doxorubicin (PHSCNK-PL-DOX), with the hypothesis that the therapy target of integrin α5β1 may also serve as a delivery target. The stealth liposomes loaded with doxorubicin (PL-DOX) were used as the control. PHSCNK-PL-DOX demonstrated an enhanced intracellular uptake and a greater cytotoxicity against melanoma B16F10 cells in comparison with PL-DOX. The novel targeted formulation displayed stronger tumor inhibition and prolonged survival time in comparison with controls in C57BL/6 mice bearing B16F10 tumors, and it exhibited less heart toxicity in hematoxylin-eosin (H&E) staining of tissues. Taking the pharmacokinetics and biodistribution results into account, the authors conclude that α5β1 integrin-mediated liposomes might be used as a potential delivery system for targeted tumor therapy.From the Clinical EditorLactosyl-norcantharidin TMC nanoparticles were found superior in comparison with Lac-NCTD and Lac-NCTD chitosan nanoparticles from the standpoint of antitumor activity on murine hepatocarcinoma 22 subcutaneous model.

Graphical AbstractAs an integrin α5β1 antagonist, N-acetyl-proline-histidine-serine-cysteine-asparagine-amide (Ac-PHSCN-NH2) is currently in phase II trials for various cancer therapies. In the present work, Ac-PHSCNK-NH2 (PHSCNK) was used as a novel homing peptide to prepare ligand-targeted liposomes loaded with doxorubicin (PHSCNK-PL-DOX), with the hypothesis that the therapy target of integrin α5β1 may also be served as a delivery target. The stealth liposomes loaded with doxorubicin (PL-DOX) were used as the control. PHSCNK-PL-DOX demonstrated an enhanced intracellular uptake and a greater cytotoxicity against melanoma B16F10 cells compared with PL-DOX. The novel targeted formulation displayed stronger tumor inhibition and prolonged survival time compared with controls in C57BL/6 mice bearing B16F10 tumor, while it exhibited less heart toxicity in H&E staining of tissues. Taking the pharmacokinetics and biodistribution results into account, it is concluded that α5β1 integrin-mediated liposomes might be used as a potential delivery system for targeted tumor therapy.Figure optionsDownload high-quality image (195 K)Download as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Nanomedicine: Nanotechnology, Biology and Medicine - Volume 8, Issue 7, October 2012, Pages 1152–1161
نویسندگان
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