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SUPERCRITICAL DEVELOPMENT OF SUSTAINED DRUG DELIVERY INTRAOCULAR LENSES

机译:超临界发育持续的药物输送人工晶状体

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Controlled drug delivery systems (DDS) are receiving an increasing interest since they enhance the drug efficacy by a target action in the body and a sustained release profile. Most of these DDS are polymer based where the polymer is biocompatible and sometimes biodegradable and acts as a reservoir or a matrix for the drug. Supercritical technologies have been demonstrated to be a clean and effective alternative to traditional methods of drug and polymer processing. Recent developments are focusing on the elaboration of DDS. For that purpose, classical supercritical processes of particle generation (RESS, SAS, PGSS...) can be applied to form polymer/drug capsules or coprecipitates. Supercritical fluids can also be used as an impregnation vehicle of the drug within the polymeric matrix. The present work deals with supercritical impregnation of intraocular lenses (IOLs) to prevent postoperative endophthalmitis in cataract surgery. Commercially available rigid IOLs made from derivative of Poly (Methyl MethAcrylate) (PMMA) were impregnated with cefuroxime sodium, an antibiotic, and dexamethasone, an anti-inflammatory drug, through a discontinuous process. The impregnation efficacy was determined in term of impregnation yield as well as in term of in-vitro drug release. The influence of some experimental operating conditions was studied by varying the pressure (8 and 20 MPa), the temperature (308 and 333 K), or by adding a cosolvent (ethanol). The influence of the IOLs dioptre was also studied (+21.0 D, +30.0 D). At rapid depressurization rates, a non desired foaming phenomenon was observed in most of the experimental conditions. This phenomenon was avoided by carrying out slow depressurizations (0.2 MPa/min).
机译:受控药物递送系统(DDS)正在接受增加的兴趣,因为它们通过体内的靶作用和持续的释放曲线增强药物功效。这些DD中的大部分是基于聚合物的聚合物,其中聚合物是生物相容性的,有时可生物降解和用作药物的储层或基质。已经证明超临界技术是传统的药物和聚合物加工方法的清洁有效的替代方法。最近的发展专注于阐述DDS。为此目的,可以应用颗粒生成(RESS,SAS,PGSS ...)的经典超临界方法以形成聚合物/药物胶囊或共胶质胶。超临界流体也可以用作聚合物基质内药物的浸渍载体。目前的工作涉及超临界浸渍的眼内透镜(IOL),以防止白内障手术中的术后眼球炎。由聚(甲基丙烯酸甲酯)(PMMA)的衍生物制成的市售刚性IOL通过不连续的方法浸渍着CEFUROXIME钠,抗生素和地塞米松,抗炎药。浸渍效果在浸渍产率和体外药物释放期间确定。通过改变压力(8和20MPa),温度(308和333k)或加入助理剂(乙醇)来研究一些实验操作条件的影响。还研究了IOLS屈光度的影响(+21.0d,+ 30.0d)。在快速减压速率下,在大多数实验条件下观察到非所需的发泡现象。通过进行缓慢的减压(0.2MPa / min)来避免这种现象。

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