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黏附性 olaminosomes:一种新型的阿戈美拉汀延长释放纳米载体,用于治疗眼高压。

Mucoadhesive olaminosomes: A novel prolonged release nanocarrier of agomelatine for the treatment of ocular hypertension.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

出版信息

Int J Pharm. 2019 Apr 5;560:235-245. doi: 10.1016/j.ijpharm.2019.01.070. Epub 2019 Feb 11.

Abstract

Mucoadhesive olaminosomes are novel nanocarriers designed to control agomelatine release and enhance its bioavailability. Olaminosomes were prepared using oleic acid, oleylamine and sorbitan monooleate adopting thin film hydration technique. Chitosan HCl was added to impart the mucoadhesive properties to the olaminosomes. Mucoadhesive olaminosomes were characterized for their particle size, in-vitro drug release and irritation potentiality in rabbit eyes. The reduction in intraocular pressure (IOP) through 8 h in male New Zealand Albino rabbits was measured after administration of the selected formulations. Histopathological changes in rabbits' eye were also evaluated. Results revealed that increasing the amount of the added oleylamine decreased the particle size of the resulted vesicles and increased the drug release rate. Olaminosomes showed enhanced drug absorption, hence more reduction in IOP was observed. Moreover, using chitosan HCl might increase the residence time of the formulation in the eye and hence improved the absorption of the drug. No histopathological changes in rabbits' eye were detected after the application of mucoadhesive olaminosomes concluding their safety on the ocular tissues. In conclusion, mucoadhesive olaminosomes succeeded in enhancing agomelatine bioavailability in rabbits' eyes confirming the development of a novel ocular nanocarrier for insoluble drugs.

摘要

黏附性奥拉米诺osomes 是一种新型纳米载体,旨在控制阿戈美拉汀的释放并提高其生物利用度。奥拉米诺osomes 是采用油酸、油胺和山梨醇单油酸酯通过薄膜水化技术制备的。盐酸壳聚糖被添加到奥拉米诺osomes 中以赋予其黏附性。对黏附性奥拉米诺osomes 的粒径、体外药物释放和对兔眼的刺激性进行了表征。通过对新西兰白兔进行给药,测量了 8 小时内降低眼压(IOP)的效果。还评估了兔子眼睛的组织病理学变化。结果表明,增加添加的油胺的量会降低所得囊泡的粒径并增加药物释放速率。奥拉米诺osomes 显示出增强的药物吸收能力,因此观察到 IOP 更大幅度的降低。此外,使用盐酸壳聚糖可能会增加制剂在眼睛中的停留时间,从而改善药物的吸收。在应用黏附性奥拉米诺osomes 后,兔子的眼睛没有观察到组织病理学变化,这证明了它们对眼部组织的安全性。总之,黏附性奥拉米诺osomes 成功地提高了阿戈美拉汀在兔子眼睛中的生物利用度,证实了为难溶性药物开发新型眼部纳米载体的成功。

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