Encapsulation of eptifibatide in RGD-modified nanoliposomes improves platelet aggregation inhibitory activity

被引：32

作者：

Bardania, Hassan ^{[1
,2
]}

Shojaosadati, Seyed Abbas ^{[3
]}

Kobarfard, Farzad ^{[4
,5
]}

Dorkoosh, Farid ^{[6
]}

Zadeh, Marjan Esfahani ^{[5
]}

Naraki, Mahmoud ^{[2
]}

Faizi, Mehrdad ^{[7
]}

机构：

[1] Tarbiat Modares Univ, Fac Biol Sci, Dept Nanobiotechnol, Tehran, Iran

[2] Yasuj Univ Med Sci, Cellular & Mol Res Ctr, Yasuj, Iran

[3] Tarbiat Modares Univ, Biotechnol Grp, Fac Chem Engn, Ale Ahmad Highway,POB 14115-143, Tehran, Iran

[4] Shahid Beheshti Univ Med Sci, Sch Pharm, Dept Med Chem, Vali E Asr Ave, Tehran, Iran

[5] Shahid Beheshti Univ Med Sci, Sch Pharm, Phytochem Res Ctr, Tehran, Iran

[6] Univ Tehran Med Sci, Sch Pharm, Dept Pharmaceut, Tehran, Iran

[7] Shahid Beheshti Univ Med Sci, Sch Pharm, Dept Pharmacol & Toxicol, Tehran, Iran

来源：

JOURNAL OF THROMBOSIS AND THROMBOLYSIS | 2017年 / 43卷 / 02期

基金：

美国国家科学基金会;

关键词：

RGD-modified nanoliposomes (RGD-MNL); Eptifibatide; Antiplatelet activity; Cytotoxicity; RGD-MNL encapsulated eptifibatide; THROMBOLYTIC AGENTS; DRUG-DELIVERY; INTEGRIN RECEPTORS; TARGETED DELIVERY; IN-VITRO; LIPOSOMES; TOXICITY; ATHEROSCLEROSIS; STRATEGIES; RELEASE;

D O I：

10.1007/s11239-016-1440-6

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

Eptifibatide is an antiplatelet drug used for the treatment of thrombosis. However, as a result of its accumulation in non-targeted tissues and short half-life, it has a limited efficacy. In this study, RGD-modified nano-liposomes (RGD-MNL) were prepared as carriers for the targeted delivery of eptifibatide to activated platelets. The nano-liposomes were about 90 +/- 10 nm in size, with an encapsulation efficiency of 37 +/- 5 % and a good stability during 21 days, with a negligible change in the size of nanoliosomes. The in vitro cytotoxicity of nanoliposomes was examined using MTT assay. The results obtained from the ex vivo study showed that the antiplatelet activity of eptifibatide encapsulated nanoliposomes was higher in comparison with the free drug (81.63 vs. 46.17 % for RGD-MNL) and (66.67 vs. 46.17 % for UNL), and this increase was more significant for nanoliposomes targeted with RGD peptide (81.63 %; p < 0.05). The results indicated that RGD-MNL encapsulated eptifibatide had no significant cytotoxic effect on cells. In conclusion, the present nanoliposome formulation can be regarded as a new delivery system for protection and enhancement of the antiplatelet activity of eptifibatide.

引用

页码：184 / 193

页数：10

共 36 条

[1] Liposomal pegylated doxorubicin plus vinorelbine combination as first-line chemotherapy for metastatic breast cancer in elderly women ≥65 years of age [J].