A potential carrier based on liquid crystal nanoparticles for ophthalmic delivery of pilocarpine nitrate

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• 作者：Jing Li ; Lin Wu ; Weijun Wu ; Baoyan Wang ; Zhongyuan Wang ; Hongliang Xin ; Qunwei Xu
• 关键词：Pilocarpine nitrate ; Liquid crystal nanoparticle ; Glycerol monooleate ; Reverse hexagonal phase ; Corneal permeability
• 刊名：International Journal of Pharmaceutics
• 出版年：2013
• 出版时间：15 October, 2013
• 年：2013
• 卷：455
• 期：1-2
• 页码：75-84
• 全文大小：1427 K

文摘

Poor corneal penetration and short preocular retention of a clinical hydrophilic drug, pilocarpine nitrate (PN), for the treatment of open-angle glaucoma and acute angle-closure glaucoma, limit its ocular application. The purpose of this study was to investigate the potential of liquid crystal nanoparticles (LCNPs) for ocular delivery of PN. LCNPs were developed by a top-down method using glyceryl monoolein (GMO) and water in the presence of stabilizer Poloxamer 407. They were characterized by transmission electron microscopy (TEM) and small angle X-ray diffraction (SAXS). The size of LCNP is 202.28 ¡À 19.32 nm and the encapsulation efficiency reached 61.03 % . The in vitro release profiles indicated that PN could keep sustained release from PN-loaded LCNPs for 8 h. An ex vivo corneal permeation study revealed that the apparent permeability coefficient of PN-loaded LCNPs was 2.05-fold higher than that of commercial eye drops. In addition, the topical administration test showed that PN-loaded LCNPs had a prolonged effect on decreasing intraocular pressure (IOP) of rabbits compared with commercial drug and physiological saline. In conclusion, LCNPs had been demonstrated to be potential for controlled-release ocular drug delivery.