Cyclosporine Amicellar delivery system for dry eyes.
Cyclosporine Amicellar delivery system for dry eyes.
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DOI：
10.2147/ijn.s107569
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发表时间：
2016
影响因子：
8
通讯作者：
Hwang SJ
中科院分区：
文献类型：
--
作者：
Kang H;Cha KH;Cho W;Park J;Park HJ;Sun BK;Hyun SM;Hwang SJ
本研究的目的是开发稳定的环孢素A（CsA）眼用胶束溶液治疗干眼综合征，并评价其理化性质和治疗效果。CsA-胶束溶液（MS-CsA）通过一种简单的方法与Cremophor EL，乙醇和磷酸盐缓冲液创建。我们研究了粒径、pH值和渗透压。此外，观察到MS-CsA的长期物理和化学稳定性。为了确认治疗功效，使用Schirmer泪液试验（STT）评估干眼诱导的兔中的泪液产生。与市售产品Restasis相比，MS-CsA显示出杯状细胞密度和结膜上皮形态的改善，如组织学苏木精和伊红染色所示。MS-CsA具有较小的粒径（平均直径14-18 nm）和窄的粒径分布。理化参数，如粒度、pH值、渗透压摩尔浓度和剩余CsA浓度均在60天的预期范围内。MS-CsA治疗组STT评分较Restasis治疗组明显改善（P<0.05）。MS-CsA给药后兔结膜杯状细胞数量为94.83±8.38，显著高于Restasis的65.17±11.51。干眼诱导的兔结膜上皮形态变薄，杯状细胞丢失。然而，在用药物制剂处理5天后，兔结膜恢复上皮细胞并显示杯状细胞数量的相对增加。这项研究的结果表明，一种新的MS的潜在用途的眼输送CsA治疗干眼症。
The objectives of this study were to develop stable cyclosporine A (CsA) ophthalmic micelle solutions for dry-eye syndrome and evaluate their physicochemical properties and therapeutic efficacy. CsA-micelle solutions (MS-CsA) were created by a simple method with Cremophor EL, ethanol, and phosphate buffer. We investigated the particle size, pH, and osmolarity. In addition, long-term physical and chemical stability for MS-CsA was observed. To confirm the therapeutic efficacy, tear production in dry eye-induced rabbits was evaluated using the Schirmer tear test (STT). When compared to a commercial product, Restasis, MS-CsA demonstrated improvement in goblet-cell density and conjunctival epithelial morphology, as demonstrated in histological hematoxylin and eosin staining. MS-CsA had a smaller particle size (average diameter 14–18 nm) and a narrow size distribution. Physicochemical parameters, such as particle size, pH, osmolarity, and remaining CsA concentration were all within the expected range of 60 days. STT scores significantly improved in MS-CsA treated groups (P<0.05) in comparison to those of the Restasis-treated group. The number of goblet cells for rabbit conjunctivas after the administration of MS-CsA was 94.83±8.38, a significantly higher result than the 65.17±11.51 seen with Restasis. The conjunctival epithelial morphology of dry eye-induced rabbits thinned with loss of goblet cells. However, after 5 days of treatment with drug formulations, rabbit conjunctivas recovered epithelia and showed a relative increase in the number of goblet cells. The results of this study indicate the potential use of a novel MS for the ophthalmic delivery of CsA in treating dry eyes.