Shilpi Satish, Vimal Vishnoo Dayal, Soni Vandana
Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar, 470 003, Madhya Pradesh, India.
Ravishankar College of Pharmacy, Bhopal, 462 010, Madhya Pradesh, India.
Prog Biomater. 2015 Mar;4(1):55-63. doi: 10.1007/s40204-015-0037-z. Epub 2015 Mar 27.
The aim of the present study was to develop a target oriented drug delivery system for the lungs. Lactoferrin (Lf)-coupled solid lipid nanoparticles (SLNs) bearing rifampicin was prepared by a solvent injection method. The prepared nanoparticles were characterized for shape, particle size, polydispersity and percentage drug entrapment. An optimized formulation was then studied for its in vivo performance in animals and to determine its targeting efficiency. It was observed that, upon coupling with Lf, the size of SLNs increased while the percent entrapment efficiency decreases. In in vitro release, determined by a dialysis technique, analysis showed that uncoupled SLNs exhibited higher drug release as compared to coupled SLNs. An in vivo biodistribution study shows 47.7 ±0.4 drug uptakes by the lungs, which was 3.05 times higher in comparison to uncoupled SLNs. These biodistribution studies are further supported by the fluorescence study that revealed enhanced uptake of Lf-coupled SLNs in the lung. From the presented results, it can be concluded that Lf-coupled SLNs enhanced drug uptake in the lung. Moreover, lactoferrin is an efficient molecule that can be used for targeting active agents directly to the lung.
本研究的目的是开发一种针对肺部的靶向给药系统。通过溶剂注入法制备了负载利福平的乳铁蛋白（Lf）偶联固体脂质纳米粒（SLNs）。对制备的纳米粒进行了形状、粒径、多分散性和药物包封率的表征。然后研究了优化后的制剂在动物体内的性能，并确定其靶向效率。观察到，与Lf偶联后，SLNs的尺寸增大，而包封效率百分比降低。通过透析技术测定的体外释放分析表明，未偶联的SLNs比偶联的SLNs表现出更高的药物释放。体内生物分布研究显示肺部药物摄取量为47.7±0.4，与未偶联的SLNs相比高出3.05倍。荧光研究进一步支持了这些生物分布研究，该研究表明Lf偶联的SLNs在肺部的摄取增强。从给出的结果可以得出结论，Lf偶联的SLNs增强了肺部的药物摄取。此外，乳铁蛋白是一种有效的分子，可用于将活性剂直接靶向肺部。
