Reddy L Harivardhan, Murthy R S R
Drug Delivery Research Laboratory, Center of Relevance and Excellence in New Drug Delivery Systems (NDDS), Pharmacy Department, MS University, Fatehgunj, Baroda-390002, Gujarat, India.
AAPS PharmSciTech. 2005 Sep 30;6(2):E158-66. doi: 10.1208/pt060224.
The aim of the study was to prepare etoposide-loaded nanoparticles with glyceride lipids and then characterize and evaluate the in vitro steric stability and drug release characteristics and stability. The nanoparticles were prepared by melt emulsification and homogenization followed by spray drying of nanodispersion. Spray drying created powder nanoparticles with excellent redispersibility and a minimal increase in particle size (20-40 nm). Experimental variables, such as homogenization pressure, number of homogenization cycles, and surfactant concentration, showed a profound influence on the particle size and distribution. Spray drying of Poloxamer 407-stabilized nanodispersion lead to the formation of matrix-like structures surrounding the nanoparticles, resulting in particle growth. The in vitro steric stability test revealed that the lipid nanoparticles stabilized by sodium tauroglycocholate exhibit excellent steric stability compared with Poloxamer 407. All 3 glyceride nanoparticle formulations exhibited sustained release characteristics, and the release pattern followed the Higuchi equation. The spray-dried lipid nanoparticles stored in black polypropylene containers exhibited excellent long-term stability at 25 degrees C and room light conditions. Such stable lipid nanoparticles with in vitro steric stability can be a beneficial delivery system for intravenous administration as long circulating carriers for controlled and targeted drug delivery.
本研究的目的是制备负载依托泊苷的甘油酯脂质纳米粒,然后对其进行表征,并评估其体外空间稳定性、药物释放特性及稳定性。通过熔融乳化和均质化,随后对纳米分散体进行喷雾干燥来制备纳米粒。喷雾干燥产生了具有优异再分散性且粒径增加最小(20 - 40纳米)的粉末状纳米粒。诸如均质化压力、均质化循环次数和表面活性剂浓度等实验变量对粒径和分布有深远影响。泊洛沙姆407稳定的纳米分散体的喷雾干燥导致在纳米粒周围形成基质样结构,从而导致颗粒生长。体外空间稳定性测试表明,与泊洛沙姆407相比,牛磺胆酸钠稳定的脂质纳米粒表现出优异的空间稳定性。所有3种甘油酯纳米粒制剂均表现出缓释特性,且释放模式符合 Higuchi 方程。储存在黑色聚丙烯容器中的喷雾干燥脂质纳米粒在25℃和室内光照条件下表现出优异的长期稳定性。这种具有体外空间稳定性的稳定脂质纳米粒作为用于控释和靶向给药的长循环载体,可成为有益的静脉给药系统。