Wang Qin, Xu Huibi, Yang Xiangliang, Yang Yajiang
Department of Chemistry and Chemical Engineering, Huazhong University of Science and Technology, Wuhan 430074, China.
Int J Pharm. 2008 Sep 1;361(1-2):189-93. doi: 10.1016/j.ijpharm.2008.05.011. Epub 2008 May 16.
In situ gellable thermosensitive poly(N-isopropylacrylamide-co-acrylamide) (designated as PNIP/AAm) nanogel aqueous dispersions were prepared through precipitation polymerization. Their thermosensitive volume phase transition and in situ gel-forming behavior were investigated. 5-Fluorouracil (5-Fu) and bovine serum albumin (BSA) were used as model drugs. The drug-loading properties of PNIP/AAm nanogel particles and release behavior from in situ gelatinized PNIP/AAm nanogel aqueous dispersions were investigated. The prepared PNIP/AAm nanogel particles and aqueous dispersions show good thermosensitivity. The presence of the drugs in the systems has no significant influence upon the thermosensitivity of the systems. In addition, the amount of cross-linker used in the preparation of the PNIP/AAm nanogel has little influence upon the drug-loading capability of PNIP/AAm nanogel particles and also on the release behavior from gelatinized dispersions. It was found that the drug-loading efficacy and entrapment efficiency of PNIP/AAm nanogel particles for low molecular weight 5-Fu was higher than that for biomacromolecular BSA. Furthermore, the cumulative release ratios of 5-Fu from in situ gelatinized PNIP/AAm nanogel aqueous dispersions were distinctly higher than that of BSA. These results imply potential application of prepared thermosensitive nanogel dispersions as embolizing and tissue engineering materials.
通过沉淀聚合法制备了原位可凝胶化的热敏性聚(N-异丙基丙烯酰胺-co-丙烯酰胺)(命名为PNIP/AAm)纳米凝胶水分散体。研究了它们的热敏体积相转变和原位凝胶形成行为。使用5-氟尿嘧啶(5-Fu)和牛血清白蛋白(BSA)作为模型药物。研究了PNIP/AAm纳米凝胶颗粒的载药性能以及原位凝胶化的PNIP/AAm纳米凝胶水分散体的释药行为。所制备的PNIP/AAm纳米凝胶颗粒和水分散体表现出良好的热敏性。体系中药物的存在对体系的热敏性没有显著影响。此外,制备PNIP/AAm纳米凝胶时所用交联剂的量对PNIP/AAm纳米凝胶颗粒的载药能力以及凝胶化分散体的释药行为影响很小。发现PNIP/AAm纳米凝胶颗粒对低分子量5-Fu的载药效率和包封率高于对生物大分子BSA的载药效率和包封率。此外,原位凝胶化的PNIP/AAm纳米凝胶水分散体中5-Fu的累积释放率明显高于BSA的累积释放率。这些结果表明所制备的热敏性纳米凝胶分散体作为栓塞和组织工程材料具有潜在的应用价值。