Design of surface-modified poly(D,L-lactide-co-glycolide) nanoparticles for targeted drug delivery to bone
Design of surface-modified poly(D,L-lactide-co-glycolide) nanoparticles for targeted drug delivery to bone
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DOI：
10.1016/j.jconrel.2007.06.003
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发表时间：
2007-09-11
影响因子：
10.8
通讯作者：
Kim, Jung-Hyun
中科院分区：
文献类型：
--
作者：
Choi, Sung-Wook;Kim, Jung-Hyun
在不添加表面活性剂的情况下，通过透析法制备了阿仑膦酸钠和聚乙二醇（PEG）修饰的聚（D，L-丙交酯-乙交酯）（PLGA）纳米颗粒，以评估骨靶向药物递送的效力。阿仑膦酸钠是一种对骨具有强亲和力的靶向部分，通过碳二亚胺化学与 PLGA 聚合物缀合。合成了具有不同mPEG分子量（M 550、750和2000）的单甲氧基PEG（mPEG）-PLGA嵌段共聚物，并将其用于纳米颗粒表面的亲水层以避免网状内皮系统（RES）。通过对羟基磷灰石 (HA) 的吸附研究，对表面具有不同比例的阿仑膦酸盐和 mPEG 密度的表面改性 PLGA 纳米颗粒进行了评估。证实阿仑膦酸钠修饰的纳米粒子对HA具有强烈且特异性的吸附作用。当阿仑膦酸钠的含量降低时，HA上吸附的纳米颗粒的量趋于减少，并且发现mPEG的大嵌段长度会降低阿仑膦酸钠的效力。 (c) 2007 Elsevier B.V. 保留所有权利。
Poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles, modified with both alendronate and polyethylene glycol (PEG), were prepared by dialysis method without additional surfactant to evaluate the potency of the bone-targeted drug delivery. Alendronate, a targeting moiety that has a strong affinity for bone, was conjugated to PLGA polymer via carbodiimide chemistry. Monomethoxy PEG(mPEG)-PLGA block copolymers with different molecular weights of mPEG (M 550, 750, and 2000) were synthesized and used for a hydrophilic layer on the surface of the nanoparticles to avoid reticuloendothelial system (RES). The surface-modified PLGA nanoparticles with various ratios of alendronate and mPEG densities on their surface were evaluated by adsorption study onto hydroxyapatite (HA). It was confirmed that alendronate-modified nanoparticles had a strong and specific adsorption to HA. The amount of nanoparticles absorbed onto HA tended to be smaller when the content of alendronate was decreased and the large block length of mPEG was found to reduce the potency of alendronate. (c) 2007 Elsevier B.V. All rights reserved.