Institute of Biomedical Engineering, School of Ophthalmology and Eye Hospital, Wenzhou Medical College, 270 Xueyuan Road, Wenzhou 325027, China.
Colloids Surf B Biointerfaces. 2013 Dec 1;112:30-4. doi: 10.1016/j.colsurfb.2013.06.047. Epub 2013 Jul 24.
Polymeric nanoparticles have been developed to improve the bioavailability of drugs applied in ocular drug delivery. However, there are few information on ocular biocompatibility of polymeric nanoparticles applied topically onto the eye. In this paper, the ocular biocompatibility and tolerance of methoxy poly(ethylene glycol)-poly(ɛ-caprolactone) (MPEG-PCL) micelles (∼50nm) were investigated in rabbit eyes after a single intracameral and intravitreal injections. In vitro cytotoxicity assays showed that MPEG-PCL micelles had no apparent cytotoxicity against human corneal epithelial cells (HCEC), human lens epithelial cells (HLEC), and retinal pigment epithelial cells (RPE cells) at micelle concentrations of 0-2mg/mL. After a single intracameral injection of 0.2mL MPEG-PCL micelles (200mg/mL) into rabbit eyes, MPEG-PCL micelles were slowly removed from aqueous humor in a period of 14 days, while the intraocular pressure (IOP) was maintained at nearly the same level for 15 days. Three days after intracameral injection, dual staining of corneal endothelium showed that the endothelial cells were nearly regular hexagon-shape with well-defined organization, similar to normal endothelial cells. Hematoxylin and eosin staining indicated that there was absence of any obvious changes in microstructure of the corneal tissue and retina after a single intracameral and intravitreal injection of 0.2mL MPEG-PCL micelles (100mg/mL, 150mg/mL, and 200mg/mL). This study provides valuable information (safety and biocompatibility) for biomedical researchers to develop MPEG-PCL micelles as candidates for ocular drug delivery.
聚合物纳米粒已被开发用于提高眼部药物传递中应用的药物的生物利用度。然而，关于局部应用于眼部的聚合物纳米粒的眼部生物相容性的信息很少。在本文中，研究了单房内和玻璃体内注射后甲氧基聚（乙二醇）-聚（己内酯）（MPEG-PCL）胶束（约 50nm）在兔眼内的眼生物相容性和耐受性。体外细胞毒性试验表明，MPEG-PCL 胶束在浓度为 0-2mg/mL 时对人角膜上皮细胞（HCEC）、人晶状体上皮细胞（HLEC）和视网膜色素上皮细胞（RPE 细胞）无明显细胞毒性。单次房内注射 0.2mL MPEG-PCL 胶束（200mg/mL）进入兔眼后，MPEG-PCL 胶束在 14 天内从房水中缓慢清除，而眼内压（IOP）在 15 天内维持在几乎相同的水平。房内注射后 3 天，角膜内皮的双重染色显示内皮细胞呈近乎规则的六边形，排列整齐，与正常内皮细胞相似。苏木精和伊红染色表明，单次房内和玻璃体内注射 0.2mL MPEG-PCL 胶束（100mg/mL、150mg/mL 和 200mg/mL）后，角膜组织和视网膜的微观结构无明显变化。该研究为生物医学研究人员提供了有价值的信息（安全性和生物相容性），以开发 MPEG-PCL 胶束作为眼部药物传递的候选物。
