Eye Hospital, Harbin Medical University, Harbin, Heilongjiang Province, China.
J Ocul Pharmacol Ther. 2012 Oct;28(5):497-501. doi: 10.1089/jop.2011.0263. Epub 2012 Jun 12.
To investigate the varied effects of sperminated pullulans (SP) with different amino residues on cornea permeability and its local toxicity.
Three groups of rabbits were used: control, low-amino residue content SP (SP-L), and high-amino residue content SP (SP-H). The in vitro and in vivo spreading assays were combined with high performance liquid chromatography (HPLC) to measure the concentration of puerarin in the external medium or aqueous humor when 0% SP, 0.2% SP-L, and 0.2% SP-H were included. The toxicity of SP was determined by corneal hydration values, Draize score, aqueous humor protein concentration, corneal endothelial evaluation, as well as light microscopy and electron microscopy.
The application of 0.2% SP-L and 0.2% SP-H to the cornea in vitro increased puerarin apparent permeability coefficient by 1.96-fold (P<0.05) and 2.95-fold (P<0.01), respectively. SP-H showed stronger effect than SP-L (P<0.05). For the in vivo assay, those were 1.81-fold (P<0.05) and 3.71-fold (P<0.01), respectively. With the SP application, the corneal hydration values were <83% and Draize scores were <4, with no apparent changes in histological observations.
SP is one potential adjuvant promoting puerarin permeability to the cornea, and the high-content amino residue SP showed stronger effect, without ocular toxicity.
研究不同氨基酸残基含量的精氨酸聚糖（SP）对角膜通透性的不同影响及其局部毒性。
使用三组兔子：对照组、低氨基酸残基含量 SP（SP-L）和高氨基酸残基含量 SP（SP-H）。将体外和体内扩展测定与高效液相色谱（HPLC）相结合，当 0%SP、0.2%SP-L 和 0.2%SP-H 时，测量外部介质或房水中葛根素的浓度。通过角膜水合值、Draize 评分、房水蛋白浓度、角膜内皮评估以及光镜和电镜来确定 SP 的毒性。
将 0.2%SP-L 和 0.2%SP-H 应用于体外角膜，分别使葛根素表观渗透系数增加 1.96 倍（P<0.05）和 2.95 倍（P<0.01）。SP-H 比 SP-L 作用更强（P<0.05）。在体内试验中，分别增加了 1.81 倍（P<0.05）和 3.71 倍（P<0.01）。使用 SP 后，角膜水合值<83%，Draize 评分<4，组织学观察无明显变化。
SP 是一种促进葛根素透过角膜的潜在佐剂，高含量氨基酸残基 SP 作用更强，无眼部毒性。
