Formulation, characterization and cytotoxicity studies of alendronate sodium-loaded solid lipid nanoparticles
Formulation, characterization and cytotoxicity studies of alendronate sodium-loaded solid lipid nanoparticles
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DOI：
10.1016/j.colsurfb.2014.01.055
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发表时间：
2014-05-01
影响因子：
5.8
通讯作者：
Valizadeh, Hadi
中科院分区：
文献类型：
--
作者：
Dolatabadi, Jafar Ezzati Nazhad;Hamishehkar, Hamed;Valizadeh, Hadi
目的：固体脂质纳米粒（SLN）是一种新型药物递送系统，可用于胃肠外、口服、眼用和局部等多种给药途径的药物靶向。这些载体具有一些优点，例如高药物有效载荷、增加的药物稳定性、掺入亲脂性和亲水性药物的可能性以及低生物毒性。本研究以阿仑膦酸钠为亲水性模型药物，将其包封于SLNs中。方法：采用热均质法制备阿仑膦酸钠SLNs，采用离心超滤法测定药物在SLNs中的包封率。扫描电子显微镜（SEM）研究了制备的SLN的球形等形态学行为。结果：采用邻苯二甲醛衍生化法测定药物包封率，药物包封率达70-85%，药物包封率为100%，药物包封率为100%。载药SLN在水性分散体中的物理稳定性在两周内的大小和药物渗漏方面进行了评估。扫描电子显微镜图像显示了纳米范围内的球形颗粒，证实了从尺寸分析仪获得的数据。包括MU、DAPI染色和DNA片段化测定以及流式细胞术分析在内的几项细胞毒性研究证实了负载阿仑膦酸钠的SLN的低毒性。成本有效的方法，避免使用有机溶剂，可接受的再现性，在温和的制备条件下易于制造，高水平的药物包封，所需的物理稳定性和生物相容性是所提出的SLN制剂的优点。(C)2014爱思唯尔有限公司版权所有。
Aim: Solid lipid nanoparticles (SLNs) are novel drug delivery system for drug targeting in various routs of administration such as parenteral, oral, ophthalmic and topical. These carriers have some advantages such as high drug payload, increased drug stability, the possibility of incorporation of lipophilic and hydrophilic drugs, and low biotoxicity. In this study, alendronate sodium was used as a hydrophilic model drug and was incorporated into SLNs.Methods: Hot homogenization method was used for preparation of alendronate sodium-loaded SLN formulations and the encapsulation efficiency of drug in SLNs was determined by ultrafiltration method using centrifugal devices. Scanning electron microscopy (SEM) was carried out to study the morphological behaviors of prepared SLNs like sphericity. Several cytotoxicity studies including MU, DAPI staining and DNA fragmentation assays were used for biocompatibility assays.Results: High drug encapsulation efficiency (70-85%) was achieved by drug determination through derivatization with o-phthalaldehyde. The physical stability of drug-loaded SLNs in aqueous dispersions was assessed in terms of size and drug leakage during two weeks. Scanning electron microscopy images showed spherical particles in the nanometer range confirming the obtained data from size analyzer. Several cytotoxicity studies including MU, DAPI staining and DNA fragmentation assays as well as flow cytometry analysis confirmed the low toxicity of alendronate-loaded SLNs.Conclusion: The cost-efficient procedure, the avoidance of organic solvents application, acceptable reproducibility, ease of manufacturing under mild preparation conditions, high level of drug encapsulation, desirable physical stability and biocompatibility are the advantages of the proposed SLN formulations. (C) 2014 Elsevier B.V. All rights reserved.