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Brimonidine-montmorillonite hybrid formulation for topical drug delivery to the eye.
Journal of Materials Chemistry B ( IF 6.1 ) Pub Date : 2020-07-22 , DOI: 10.1039/d0tb01213k
Chun Gwon Park 1 , Goeun Choi , Myung Hun Kim , Se-Na Kim , Hanna Lee , Na Kyeong Lee , Young Bin Choy , Jin-Ho Choy
Affiliation  

Brimonidine (BMD) is often prescribed as an eye drop to reduce the intraocular pressure (IOP) for glaucoma treatment. However, eye drops are limited by rapid clearance from the preocular surface, and hence a low ocular drug bioavailability. Therefore, in this study, we propose montmorillonite (MMT), as a delivery carrier, hybridized with BMD (BMD–MMT) for topical drug delivery to the eye. The BMD–MMT hybrid was prepared by intercalating the BMD molecules in the interlayer space of the MMT lattice via ion-exchange reaction; it was then formulated with polyvinyl alcohol (PVA) to produce a dry tablet (i.e., BMD–MMT@PVA). The BMD–MMT@PVA hybrid drug released BMD in a sustained manner for more than 5 h under in vitro conditions. When the hybrid drug was administered to rabbit eyes in vivo, 43% and 18.5% BMD–MMT still remained on the preocular surface for 10 and 60 min after administration, respectively. Thus, the BMD–MMT@PVA hybrid drug exhibited a prolonged decrease in IOP, that is, for 12 h, which was approximately two times longer than that observed with the commercially available BMD eye drop, Alphagan® P.

中文翻译:

溴莫尼定-蒙脱土混合制剂,用于局部向眼睛输送药物。

通常将溴莫尼定(BMD)用作滴眼剂,以降低用于青光眼的眼内压(IOP)。但是,滴眼液受眼前表面快速清除的限制,因此眼药的生物利用度低。因此,在这项研究中,我们提出将蒙脱石(MMT)作为递送载体,与BMD(BMD–MMT)杂交,以局部向眼睛递送药物。BMD-MMT杂化物是通过离子交换反应将BMD分子插入MMT晶格的层间空间中而制备的。然后将其与聚乙烯醇(PVA)配制成干片(BMD–MMT @ PVA)。BMD–MMT @ PVA杂合药物在体外持续释放BMD 5小时以上条件。当在体内对兔眼施用这种杂合药物后,分别在施用后10分钟和60分钟内,仍有43%和18.5%的BMD-MMT残留在眼前表面上。因此,BMD-MMT @ PVA杂合药物的眼压延长时间延长,即持续12小时,比市售BMD眼药水Alphagan®P观察到的时间长约两倍。
更新日期:2020-09-16
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