新型壳交联聚己二酸丁二酯- N-琥珀酰壳聚糖纳米凝胶的设计、表征及体外评价：通过控制药物释放增强治疗效果的新系统，载洛昔芬依托泊苷。
Design, characterization and in vitro evaluation of novel shell crosslinked poly(butylene adipate)-co-N-succinyl chitosan nanogels containing loteprednol etabonate: A new system for therapeutic effect enhancement via controlled drug delivery.
机构信息
Polymer Laboratory, Chemistry Department, School of Science, University of Tehran, P.O. Box 14155-6455, Tehran, Iran.
Polymer Laboratory, Chemistry Department, School of Science, University of Tehran, P.O. Box 14155-6455, Tehran, Iran.
出版信息
Eur J Med Chem. 2015 Sep 18;102:132-42. doi: 10.1016/j.ejmech.2015.07.045. Epub 2015 Aug 1.
This study reports on the development of a novel mucoadhesive and biocompatible shell-crosslinked nanogel system based on poly(butylene adipate) (PBA) and N-succinyl chitosan (S-Cs) by coupling reaction with a new formulation method. For this purpose, two different molecular weights of dendrimerized PBA with amine terminated functional groups were synthesized separately and characterized well by FT-IR, (1)HNMR and GPC. The PBA nanoparticles containing loteprednol etabonate (LPE) prepared by O/W emulsion technique were reacted immediately with modified carboxylated chitosan via carbodiimide chemistry. TEM photographs of the nanoparticles and crosslinked nanoparticles displayed a spherical morphology closely corresponding to the results obtained by DLS. On The other hand, biodegradability, biocompatibility and bioadhesiveness of the prepared nanoparticles were also studied. It is concluded that the core-shell structured nanogels can be used as novel ocular drug delivery systems with appropriate loading capacity for slightly water soluble LPE as an anti-inflammatory drug.
本研究报告了一种新型的基于聚（己二酸丁二醇酯）（PBA）和 N-琥珀酰壳聚糖（S-Cs）的通过偶联反应与新的制剂方法开发的具有黏膜黏附性和生物相容性的壳交联纳米凝胶系统。为此，分别合成了两种不同分子量的具有胺端基官能团的树枝状 PBA，并通过 FT-IR、（1）HNMR 和 GPC 进行了很好的表征。通过 O/W 乳液技术制备的含有洛美前列素（LPE）的 PBA 纳米颗粒通过碳二亚胺化学立即与改性羧化壳聚糖反应。纳米颗粒和交联纳米颗粒的 TEM 照片显示出与 DLS 结果非常吻合的球形形态。另一方面，还研究了制备的纳米颗粒的生物降解性、生物相容性和生物黏附性。结论是，具有核壳结构的纳米凝胶可用作具有适当载药量的新型眼部药物传递系统，可作为具有轻微水溶性的 LPE 等抗炎药物。
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