Tan Guoxin, Yu Shihui, Li Jinyu, Pan Weisan
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Int J Biol Macromol. 2017 Oct;103:941-947. doi: 10.1016/j.ijbiomac.2017.05.132. Epub 2017 May 22.
This study aims to explore a novel composite thermosensitive in situ gelling formulation which the nanostructured lipid carriers (NLC) was incorporated into hydroxypropyltrimethyl ammonium chloride chitosan (HACC)-based hydrogels, and the resulting formulation investigated for its potential to act as a potential sustained ocular delivery system. NLC formulation loaded with dexamethasone (DXM) were prepared using the melt-emulsification method. The particle size, zeta potential, encapsulation efficiency, and morphological properties of the NLC were characterized. The HACC was synthesized and structure was analyzed by FT-IR and H NMR. A thermosensitive hydrogel was designed and prepared by simply mixing HACC and β-glycerophosphate (β-GP). The obtained formulation showed a rapid solution-to-gel transition at 35°C. The NLC were then incorporated in HACC/β-GP hydrogel to form a NLC-loaded hydrogel carrier. In vitro release studies, 88.65% of total DXM was released from the NLC-HACC/GP gel within 3days, indicating DXM-based NLC-gel could release drug sustainably. Taken together, DXM-based NLC-HACC/GP gel is a promising drug delivery system.
本研究旨在探索一种新型的复合热敏原位凝胶制剂,即将纳米结构脂质载体(NLC)掺入基于羟丙基三甲基氯化铵壳聚糖(HACC)的水凝胶中,并对所得制剂作为潜在的持续眼部给药系统的潜力进行研究。采用熔融乳化法制备了载有地塞米松(DXM)的NLC制剂。对NLC的粒径、zeta电位、包封率和形态学性质进行了表征。合成了HACC,并通过傅里叶变换红外光谱(FT-IR)和氢核磁共振(H NMR)对其结构进行了分析。通过简单混合HACC和β-甘油磷酸酯(β-GP)设计并制备了一种热敏水凝胶。所得制剂在35℃时显示出快速的溶液-凝胶转变。然后将NLC掺入HACC/β-GP水凝胶中,形成载有NLC的水凝胶载体。体外释放研究表明,3天内88.65%的总DXM从NLC-HACC/GP凝胶中释放出来,表明基于DXM的NLC-凝胶能够持续释放药物。综上所述,基于DXM的NLC-HACC/GP凝胶是一种很有前景的药物递送系统。