Choi Sung-Wook, Kim Jung-Hyun
Nanosphere Process and Technology Laboratory, Department of Chemical Engineering, Yonsei University, 134 Shinchon-dong, Sudaemoon-ku, Seoul, South Korea.
J Control Release. 2007 Sep 11;122(1):24-30. doi: 10.1016/j.jconrel.2007.06.003. Epub 2007 Jun 14.
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(n) 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.
通过透析法制备了同时用阿仑膦酸盐和聚乙二醇（PEG）修饰的聚（d，l-丙交酯-共-乙交酯）（PLGA）纳米颗粒，未添加额外的表面活性剂，以评估骨靶向药物递送的效能。阿仑膦酸盐是一种对骨具有强烈亲和力的靶向部分，通过碳二亚胺化学法与PLGA聚合物偶联。合成了具有不同分子量的甲氧基PEG（mPEG）（M(n) 550、750和2000）的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，评估了表面具有不同阿仑膦酸盐和mPEG密度比例的表面改性PLGA纳米颗粒。证实阿仑膦酸盐改性的纳米颗粒对HA具有强烈且特异性的吸附。当阿仑膦酸盐含量降低时，吸附到HA上的纳米颗粒数量趋于减少，并且发现mPEG的大嵌段长度会降低阿仑膦酸盐的效能。
