School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Drug Deliv. 2012 Jan;19(1):28-35. doi: 10.3109/10717544.2011.621994. Epub 2011 Nov 9.
In this study, low molecular weight chitosan coated liposomes (LCHL) were designed and prepared for ocular drug delivery, the coating mechanism was studied, and in vitro and in vivo characterization was conducted. The effects of molecular weight and concentration of low molecular weight chitosan on the liposomal coating were studied. The numeric relations between coating variables and coating efficiency were established using a mathematical model. Morphology of LCHL was examined by transmission electron microscopy (TEM). Cytotoxicity and cell internalization of FITC-BSA labeled LCHL in a rabbit conjunctival epithelium (RCE) cell line were studied. Cyclosporin A (CsA) was encapsulated as a model drug, and in vitro drug release and in vivo drug absorption were investigated. LCHL demonstrated low toxicity to RCE cells. In vitro drug release measurement showed that LCHL had a delayed release profile compared with non-coated liposomes. In vivo study in rabbits showed that the concentrations of CsA in cornea, conjunctiva, and sclera were remarkably increased by LCHL. In conclusion, LCHL might be a potential ocular drug carrier with characteristics such as prolonged drug retention, enhanced drug permeation, and biocompatibility.
在这项研究中，设计并制备了低分子量壳聚糖包覆的脂质体（LCHL）用于眼部药物传递，研究了包封机制，并进行了体外和体内表征。研究了低分子量壳聚糖的分子量和浓度对脂质体包封的影响。使用数学模型建立了包封变量与包封效率之间的数值关系。通过透射电子显微镜（TEM）检查了 LCHL 的形态。研究了 FITC-BSA 标记的 LCHL 在兔结膜上皮（RCE）细胞系中的细胞毒性和细胞内吞作用。环孢素 A（CsA）被包封作为模型药物，研究了体外药物释放和体内药物吸收。LCHL 对 RCE 细胞的毒性较低。体外药物释放测量表明，与未包封的脂质体相比，LCHL 具有延迟释放的特征。在兔体内研究中，LCHL 使角膜、结膜和巩膜中的 CsA 浓度显著增加。总之，LCHL 可能是一种具有延长药物滞留、增强药物渗透和生物相容性等特点的潜在眼部药物载体。
