Dillen Kathleen, Vandervoort Jo, Van den Mooter Guy, Ludwig Annick
Laboratory of Pharmaceutical Technology and Biopharmacy, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, 2610 Antwerp, Belgium.
Int J Pharm. 2006 May 11;314(1):72-82. doi: 10.1016/j.ijpharm.2006.01.041. Epub 2006 Apr 5.
The objective of present study was to prepare positively charged ciprofloxacin-loaded nanoparticles providing a controlled release formulation. The particles were prepared by water-in-oil-in-water (w/o/w) emulsification and solvent evaporation, followed by high-pressure homogenisation. Two non-biodegradable positively charged polymers, Eudragit RS100 and RL100, and the biodegradable polymer poly(lactic-co-glycolic acid) or PLGA were used alone or in combination, with varying ratios. The formulations were evaluated in terms of particle size and zeta potential. Differential scanning calorimetry measurements were carried out on the nanoparticles and on the pure polymers Eudragit and PLGA. Drug loading and release properties of the nanoparticles were examined. The antimicrobial activity against Pseudomonas aeruginosa and Staphylococcus aureus was determined. During solvent evaporation, the size and zeta potential of the nanoparticles did not change significantly. The mean diameter was dependent on the presence of Eudragit and on the viscosity of the organic phase. The zeta potential of all Eudragit containing nanoparticles was positive in ultrapure water (around +21/+25 mV). No burst effect but a prolonged drug release was observed from all formulations. The particles' activity against P. aeruginosa and S. aureus was comparable with an equally concentrated ciprofloxacin solution.
本研究的目的是制备带正电荷的载环丙沙星纳米颗粒，提供一种控释制剂。通过水包油包水（w/o/w）乳化和溶剂蒸发法制备颗粒，随后进行高压均质处理。使用两种不可生物降解的带正电荷聚合物，即Eudragit RS100和RL100，以及可生物降解的聚合物聚乳酸-乙醇酸共聚物（PLGA）单独或按不同比例组合使用。对制剂进行了粒径和zeta电位评估。对纳米颗粒以及纯聚合物Eudragit和PLGA进行了差示扫描量热法测量。考察了纳米颗粒的载药量和释放特性。测定了对铜绿假单胞菌和金黄色葡萄球菌的抗菌活性。在溶剂蒸发过程中，纳米颗粒的粒径和zeta电位没有显著变化。平均直径取决于Eudragit的存在以及有机相的粘度。所有含Eudragit的纳米颗粒在超纯水中的zeta电位均为正值（约+21/+25 mV）。所有制剂均未观察到突释效应，而是呈现药物的持续释放。颗粒对铜绿假单胞菌和金黄色葡萄球菌的活性与同等浓度的环丙沙星溶液相当。
