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首页> 外文期刊>International Journal of Pharmaceutics >Development of semisolid self-microemulsifying drug delivery systems (SMEDDSs) filled in hard capsules for oral delivery of aciclovir
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Development of semisolid self-microemulsifying drug delivery systems (SMEDDSs) filled in hard capsules for oral delivery of aciclovir

机译：开发半固体自微乳化药物递送系统（SMEDDS），用于口服递送ACICLOVIR的硬胶囊

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The study aimed to develop semisolid self-microemulsifying drug delivery systems (SMEDDSs) as carriers for oral delivery of aciclovir in hard hydroxypropylmethyl cellulose (HPMC) capsules. Six selfdispersing systems (SD1-SD6) were prepared by loading aciclovir into the semisolid formulations consisting of medium chain length triglycerides (lipid), macrogolglycerol hydroxystearate (surfactant), polyglyceryl-3-dioleate (cosurfactant), glycerol (hydrophilic cosolvent), and macrogol 8000 (viscosity modifier). Their characterization was performed in order to identify the semisolid system with rheological behaviour suitable for filling in hard HPMC capsules and fast dispersibility in acidic and alkaline aqueous media with formation of oil-in-water microemulsions. The optimal SMEDDS was loaded with aciclovir at two levels (2% and 33.33%) and morphology and aqueous dispersibility of the obtained systems were examined by applying light microscopy and photon correlation spectroscopy (PCS), respectively. The assessment of diffusivity of aciclovir from the SMEDDSs by using an enhancer cell model, showed that it was increased at a higher drug loading. Differential scanning calorimetry (DSC) analysis indicated that the SMEDDSs were semisolids at temperatures up to 50 degrees C and physically stable and compatible with HPMC capsules for 3 months storage at 25 degrees C and 4 degrees C. The results of in vitro release study revealed that the designed solid dosage form based on the semisolid SMEDDS loaded with the therapeutic dose of 200 mg, may control partitioning of the solubilized drug from in situ formed oil-inwater microemulsion carrier into the sorrounding aqueous media, and hence decrease the risk for precipitation of the drug. (C) 2017 Elsevier B.V. All rights reserved.
机译：旨在研究开发半固体自微乳化药物递送系统（SMEDDSs）作为硬羟丙基甲基纤维素（HPMC）胶囊口服给药阿昔洛韦的载体。六个selfdispersing系统（SD1-SD6）通过装载阿昔洛韦制备成由中等链长的三酸甘油酯（类脂），聚乙二醇甘油羟基硬脂酸酯（表面活性剂），聚甘油-3-二油酸酯（助表面活性剂），甘油（亲水助溶剂），和聚乙二醇的半固体制剂8000（粘度改进剂）。其特征是为了识别具有适合于在硬HPMC胶囊和快速的分散性与形成油包水型微乳液的填充酸性和碱性水溶液介质的流变特性的半固体系统执行。最佳SMEDDS以两个水平（2％和33.33％）和所得到的系统的形态学和水分散负载有阿昔洛韦分别通过施加光显微镜和光子相关光谱法（PCS），检查。从SMEDDSs阿昔洛韦的扩散的使用增强细胞模型评估，结果表明它是在一个较高的载药量增加。差示扫描量热法（DSC）分析表明，该SMEDDSs是在温度高达50℃和半固体物理稳定的，并与HPMC胶囊持续3个月储存在25℃和4℃兼容的体外释放研究的结果表明，基于所述半固体SMEDDS所设计的固体剂型装载有200毫克的治疗剂量，可以控制从在形成水包油型微滴乳状液载体进入sorrounding水性介质原位溶解的药物的分区，并且因此降低危险的沉淀药品。 （c）2017年Elsevier B.V.保留所有权利。

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