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使用载药型亲水性隐形眼镜经角膜递药治疗眼部感染的莫西沙星和地塞米松联合治疗。

Corneal delivery of moxifloxacin and dexamethasone combination using drug-eluting mucoadhesive contact lens to treat ocular infections.

机构信息

Department of Pharmacy, Birla Institute of Technology and Science (BITS) Pilani, Hyderabad Campus, Shameerpet, Hyderabad 500078, Telangana, India; Tej Kohli Cornea Centre, L. V. Prasad Eye Institute, Hyderabad 500034, Telangana, India.

Department of Pharmacy, Birla Institute of Technology and Science (BITS) Pilani, Hyderabad Campus, Shameerpet, Hyderabad 500078, Telangana, India.

出版信息

Int J Pharm. 2020 Dec 15;591:120023. doi: 10.1016/j.ijpharm.2020.120023. Epub 2020 Oct 27.

Abstract

The important causes of loss of vision are ocular infections, including keratitis and conjunctivitis. Attaining an adequate concentration of topically applied antibiotics to prevent or treat infections within the cornea is challenging. The study aimed to design and develop a drug-eluting polymeric contact lens for the effective delivery of moxifloxacin (MF) and dexamethasone (DM). The polymeric contact lens was prepared using chitosan, glycerol, and polyethylene glycol. MF and DM were loaded into the contact lens, both separately and in combination. The MF and DM loaded contact lenses were characterized for thickness, swelling index, surface topography, and mucoadhesion strength. Furthermore, studies were performed to understand the in vitro drug release behavior, ex vivo corneal permeation, and in vitro and in vivo antimicrobial activity. The drug-loaded contact lens was compared with the standard drug solutions. The physical characteristics of the polymeric contact lens were similar to the commercially available contact lens. Compared to the topically applied standard drug solutions, the drug-loaded contact lens showed significantly (p < 0.05) greater corneal drug distribution after 24 h incubation. In vitro and in vivo antimicrobial activity of the MF loaded contact lens was superior to the standard drug solution. In vivo drug distribution studies showed greater tissue concentration of MF in cornea, sclera, and aqueous humor with contact lens application compared with drug solutions. Overall, the polymeric contact lens was efficient in delivering MF and DM at required therapeutic concentrations. The findings from the present study show that drug-eluting contact lenses could be used in post-operative conditions to prevent ocular infections.

摘要

导致视力丧失的重要原因是眼部感染,包括角膜炎和结膜炎。为了预防或治疗角膜内感染,将局部应用的抗生素充分集中在感染部位是具有挑战性的。本研究旨在设计和开发一种载药聚合物隐形眼镜,以有效递送达氟沙星(MF)和地塞米松(DM)。该聚合物隐形眼镜是由壳聚糖、甘油和聚乙二醇制备而成。MF 和 DM 分别或联合载入隐形眼镜中。对载 MF 和 DM 的隐形眼镜进行厚度、溶胀指数、表面形貌和粘膜粘附强度的特性研究。此外,还进行了体外药物释放行为、体外角膜渗透以及体外和体内抗菌活性的研究。将载药隐形眼镜与标准药物溶液进行了比较。聚合物隐形眼镜的物理特性与市售隐形眼镜相似。与局部应用的标准药物溶液相比,载药隐形眼镜在 24 小时孵育后显示出显著(p < 0.05)更大的角膜药物分布。载 MF 的隐形眼镜的体外和体内抗菌活性优于标准药物溶液。体内药物分布研究表明,与药物溶液相比,应用隐形眼镜后,角膜、巩膜和房水中的 MF 组织浓度更高。总的来说,该聚合物隐形眼镜能够以所需的治疗浓度有效递送 MF 和 DM。本研究的结果表明,载药隐形眼镜可用于术后条件,以预防眼部感染。

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