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地塞米松眼内植入剂的制备:体外释放曲线的比较研究。

Preparation of dexamethasone ophthalmic implants: a comparative study of in vitro release profiles.

机构信息

a Faculty of Pharmacy , University of Coimbra , Coimbra , Portugal.

b CIEPQPF, Department of Chemical Engineering , University of Coimbra , Coimbra , Portugal.

出版信息

Pharm Dev Technol. 2018 Mar;23(3):218-224. doi: 10.1080/10837450.2017.1306560. Epub 2017 Mar 30.

DOI:10.1080/10837450.2017.1306560
PMID:28300463
Abstract

Diseases affecting the posterior segment of the eye are the most common cause of visual disorders in industrialized countries. This scenario has encouraged the development of new treatment modalities for these diseases, such as drug loaded implants with prolonged drug release. The aim of the present work was to create a polymeric based biodegradable ophthalmic implant for the delivery of dexamethasone. For this purpose, we prepared and compared the in vitro release profiles of dexamethasone ophthalmic implants produced by two methods: melting casting and solvent casting. The type of the biodegradable polymer used - poly (ɛ-caprolactone) (PCL) and poly(lactic acid) (PLA); the drug loading (10% and 25%, w/w), the molecular weight of PCL (37 kDa and 14 kDa) and the form of the drug (dexamethasone and dexamethasone disodium phosphate) were also investigated. The results show that the preparation method has little influence on the obtained release profiles, being the type of polymer the most significant factor affecting the release profiles; nonetheless, a better distribution of dexamethasone was obtained for the devices prepared by melting casting.

摘要

影响眼睛后节的疾病是工业化国家视觉障碍的最常见原因。这种情况促使人们为这些疾病开发新的治疗方法,例如具有延长药物释放的载药植入物。本工作的目的是为了制备一种用于递送达塞米松的基于聚合物的可生物降解的眼科植入物。为此,我们通过两种方法(熔融浇铸和溶剂浇铸)制备和比较了载有地塞米松的眼科植入物的体外释放曲线:使用的可生物降解聚合物的类型-聚(ε-己内酯)(PCL)和聚乳酸(PLA);药物载量(10%和 25%,w/w),PCL 的分子量(37kDa 和 14kDa)和药物形式(地塞米松和地塞米松二钠盐)。结果表明,制备方法对获得的释放曲线几乎没有影响,聚合物的类型是影响释放曲线的最显著因素;尽管如此,熔融浇铸制备的装置中地塞米松的分布更好。

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