Li Ning, Zhuang Chunyang, Wang Mi, Sun Xiyang, Nie Shufang, Pan Weisan
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Int J Pharm. 2009 Sep 8;379(1):131-8. doi: 10.1016/j.ijpharm.2009.06.020. Epub 2009 Jun 25.
In this study liposome coated with low molecular weight chitosan (LCH) was proposed and investigated its in vitro and in vivo properties, and its potential use in ocular drug delivery was evaluated. LCH with a molecular weight of 8kDa was prepared and coated on liposome loaded with diclofenac sodium. The LCH coating changed the liposome surface charge and slightly increased its particle size, while the drug encapsulation was not affected. After coating, the liposome displayed a prolonged in vitro drug release profile. LCH coated liposome also demonstrated an improved physicochemical stability at 25 degrees C in a 30-day storage period. The ocular bioadhesion property was evaluated by rabbit in vivo precorneal retention, and LCH coated liposome achieved a significantly prolonged retention compared with non-coated liposome or drug solution. The LCH coating also displayed a potential penetration enhancing effect for transcorneal delivery of the drug. In the ocular tolerance study, no irritation or toxicity was caused by continual administration of LCH coated liposome in a total period of 7 days. In conclusion, the LCH coating significantly modified the properties of liposome and brought a series of notable advantages for ocular drug delivery.
在本研究中，提出了一种用低分子量壳聚糖（LCH）包衣的脂质体，并对其体外和体内性质进行了研究，评估了其在眼部给药中的潜在应用。制备了分子量为8 kDa的LCH，并将其包衣在负载双氯芬酸钠的脂质体上。LCH包衣改变了脂质体的表面电荷并使其粒径略有增加，而药物包封率不受影响。包衣后，脂质体呈现出延长的体外药物释放曲线。LCH包衣的脂质体在25℃下储存30天期间也表现出改善的物理化学稳定性。通过兔体内角膜前滞留评估眼部生物粘附性能，与未包衣的脂质体或药物溶液相比，LCH包衣的脂质体实现了显著延长的滞留时间。LCH包衣对药物的角膜渗透传递也显示出潜在的增强作用。在眼部耐受性研究中，连续7天给予LCH包衣的脂质体未引起刺激或毒性。总之，LCH包衣显著改变了脂质体的性质，并为眼部给药带来了一系列显著优势。
