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含有亲脂性免疫调节剂的可生物降解纳米胶囊:体外药物保留及对巨噬细胞的耐受性

Biodegradable nanocapsules containing a lipophilic immunomodulator: drug retention and tolerance towards macrophages in vitro.

作者信息

Morin C, Barratt G, Fessi H, Devissaguet J P, Puisieux F

机构信息

URA CNRS 1218, Laboratoire de Pharmacie Galénique et Biopharmacie, Faculté de Pharmacie, Université de Paris Sud, Chatenay-Malabry, France.

出版信息

J Drug Target. 1993;1(2):157-64. doi: 10.3109/10611869308996072.

DOI:10.3109/10611869308996072
PMID:8069554
Abstract

Nanocapsules (250 nm diameter) were prepared from poly (D, L-lactide) containing a lipophilic immunomodulator: MDP-L-alanyl cholesterol (MTP-Chol). High encapsulation rates were obtained at 37 degrees C in culture medium or in buffers imitating phagosomes and lysosomes. The tolerance of these particles by rat alveolar macrophages in vitro was tested. A slight toxicity was observed which was the result of two factors: the capacity of the immunomodulator to stimulate the generation of nitrite oxide by the L-arginine-dependent pathway and the polymer itself. The latter toxicity seemed to be mediated by a different mechanism.

摘要

纳米胶囊(直径250纳米)由含有亲脂性免疫调节剂:MDP-L-丙氨酰胆固醇(MTP-Chol)的聚(D,L-丙交酯)制备而成。在37摄氏度的培养基或模拟吞噬体和溶酶体的缓冲液中可获得较高的包封率。测试了这些颗粒在体外对大鼠肺泡巨噬细胞的耐受性。观察到轻微的毒性,这是由两个因素导致的:免疫调节剂通过L-精氨酸依赖性途径刺激一氧化氮生成的能力以及聚合物本身。后一种毒性似乎是由不同的机制介导的。

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