Design of sustained release liquid formulations using thereto-responsible intelligent polymers and nanoparticles

1.本研究的目的是利用Pluronic F-127的热致凝胶和木聚糖或果胶的离子致凝胶为老年人和婴儿开发缓释液体配方。所有这些都被设计成液体剂型，并在胃的酸性环境中原位形成凝胶。通过体外和体内研究，我们已经证明了口服这些智能聚合物水溶液后原位形成的凝胶的缓释载体的潜力。所有这些配方的粘度都足够低，没有吞咽困难的设想。2.如果将纳米颗粒载体系统加入到智能聚合物液体制剂中，可能会改善口服给药。本研究采用界面聚合法制备了吲哚美辛纳米胶囊。采用高效液相色谱法测定PNBCA纳米胶囊的药物含量，扫描电镜分析其粒径，对其进行理化表征。结果表明，F'NBCA纳米胶囊的载药量为76.6%，平均粒径为188 nm。本研究的数据表明，与传统凝胶制剂相比，吲哚美辛纳米胶囊可以改善口服给药。这可能是由于它们的超细颗粒尺寸和它们的亲疏水表面特性。

1.The purpose of this study was concerned with the development of sustained release liquid formulatios for the elderly and the infant using thermo-responsible gelation of Pluronic F-127 and xyloglucan or ionic-responsible gelation of Pectin. All of which were designed to be administered in liquid dosage forms and to form gels in situ in the acidic environment of stomach. We have demonstratated the potential as sustained release vehicles of gels formed in situ following the oral administration of aqueous solutions of these intelligent polymers by in vitro and in vivo studies. The viscosities of all of these formulations were sufficiently low that no difficulties with swallowing were envisaged. 2.An oral drug delivery could possibly be improved if nanoparticle carrier system was incorporated into an intelligent polymer liquid formulation. In this study, poly n-butylcyanoacrylate(PNBCA) nanocapsules of indomethacin were prepared by interfacial polymerization. The physicochemical characterization of the PNBCA nanocapsules was performed by measuring the drug content by HPLC and analyzing the particle size using SEM. The drug loading results indicated that 76.6% of indomethacin was loaded onto the F'NBCA nanocapsules, the average particle size was 188 nm. The presented data expected that indomethacin loaded PNBCA nanocapsules could improve the oral drug delivery compared to a conventional gel formulation. This might be due to their ultra fine particle size and their hydrophilic and hydrophobic surface characteristics.