a Department of Geriatrics , Qilu Hospital of Shandong University , Jinan , PR China.
b Department of Ophthalmology , The Affiliated Hospital of Taishan Medical University , Taian , PR China.
Drug Deliv. 2019 Dec;26(1):188-198. doi: 10.1080/10717544.2019.1571122.
As a leading cause of vision impairment of the retina, macular edema (ME) has one of the highest clinical demands for treatment. Current treatment of ME relies heavily on invasive techniques resulting in complications and poor patient compliance. To enhance the efficiency of triamcinolone acetonide as eye drop to the posterior segment of the eye, we developed and characterized a novel formulation, namely, triamcinolone acetonide chitosan-coated liposomes (TA-CHL), prepared by the calcium acetate gradient method with some modifications. TA-CHL provided the mean particle size of 135.46 ± 4.49 nm and high entrapment efficiency (90.66 ± 3.21%), exhibited a sustained release profile, excellent physical stability, and no significant toxicity on cornea, conjunctiva, and retina. Optical coherence tomography system (OCT) was used to detect pharmacokinetics of CHL in vivo, indicating that CHL had good potency for drug delivery. Cellular uptake experiments showed CHL had the higher transduction efficiency into HCEC and ARPE-19 than liposomes. TA-CHL was shown to be potentially effective eye drop to contribute to the posterior segment of the eye.
作为视网膜视力损害的主要原因之一，黄斑水肿 (ME) 是治疗需求最高的疾病之一。目前的 ME 治疗方法主要依赖于侵入性技术，这会导致并发症和较差的患者依从性。为了提高曲安奈德作为滴眼剂用于眼部后段的效率，我们开发并表征了一种新型制剂，即醋酸曲安奈德壳聚糖包被的脂质体 (TA-CHL)，通过醋酸钙梯度法并进行了一些修改制备得到。TA-CHL 的平均粒径为 135.46±4.49nm，包封率高（90.66±3.21%），具有持续释放特性、出色的物理稳定性，对角膜、结膜和视网膜无明显毒性。光学相干断层扫描系统 (OCT) 用于检测体内 CHL 的药代动力学，表明 CHL 具有良好的药物传递能力。细胞摄取实验表明，CHL 比脂质体具有更高的转导效率进入 HCEC 和 ARPE-19。TA-CHL 有可能成为有效的滴眼剂，有助于眼部后段的治疗。
