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首页> 外文期刊>European journal of pharmaceutical sciences >Are nanostructured lipid carriers (NLCs) better than solid lipid nanoparticles (SLNs): Development, characterizations and comparative evaluations of clotrimazole-loaded SLNs and NLCs?
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Are nanostructured lipid carriers (NLCs) better than solid lipid nanoparticles (SLNs): Development, characterizations and comparative evaluations of clotrimazole-loaded SLNs and NLCs?

机译:纳米结构脂质载体(NLC)是否优于固体脂质纳米颗粒(SLN):克霉唑负载的SLN和NLC的开发,表征和比较评估?

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摘要

In recent years, solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are among the popular research topics for the delivery of lipophilic drugs. Although SLNs have demonstrated several beneficial properties as drug-carrier, limited drug-loading and expulsion of drug during storage led to the development of NLCs. However, the superiority of NLCs over SLNs has not been fully established yet due to the contradictory results. In this study, SLNs and NLCs were developed using clotrimazole as model drug. Size, polydispersity index (PI), zeta potential (ZP), drug-loading (L), drug encapsulation efficiency (EE), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffractometry (XRD), drug release and stability of SLNs and NLCs were compared. Critical process parameters exhibited significant impact on the nanoparticles' properties. Size, PI, ZP and EE of the developed SLNs and NLCs were <100 nm, <0.17, <-22 mV and >82%, respectively. SEM images of SLNs and NLCs revealed spherical shaped particles (~100 nm). DSC and XRD studies indicated slight difference between SLNs and NLCs as well as disappearance of the crystalline peak(s) of the encapsulated drug. NLCs demonstrated faster drug release than SLNs at low drug-loading, whereas there was no significant difference in drug release from SLNs and NLCs at high drug-loading. However, sustained/prolonged drug release was observed from both formulations. Furthermore, this study suggests that the drug release experiment should be designed considering the final application (topical/oral/parenteral) of the product. Regarding stability, NLCs showed better stability (in terms of size, PI, EE and L) than SLNs at 25 °C. Moreover, there was no significant difference in drug release profile of NLCs after 3 months storage in compare to fresh NLCs, while significant change in drug release rate was observed in case of SLNs. Therefore, NLCs have an edge over SLNs.
机译:近年来,固体脂质纳米颗粒(SLN)和纳米结构脂质载体(NLC)成为亲脂药物递送的热门研究主题。尽管SLNs已显示出作为药物载体的几种有益特性,但在储存过程中有限的载药量和驱逐药物导致了NLC的发展。但是,由于矛盾的结果,NLC在SLN上的优势尚未完全确立。在这项研究中,使用克霉唑为模型药物开发了SLN和NLC。尺寸,多分散指数(PI),ζ电位(ZP),载药量(L),药物封装效率(EE),扫描电子显微镜(SEM),差示扫描量热法(DSC),X射线衍射法(XRD),比较了SLN和NLC的药物释放和稳定性。关键的工艺参数对纳米颗粒的性能表现出重大影响。已开发的SLN和NLC的尺寸,PI,ZP和EE分别为<100 nm,<0.17,<-22 mV和> 82%。 SLNs和NLCs的SEM图像显示球形颗粒(〜100 nm)。 DSC和XRD研究表明SLN和NLC之间存在细微差异,并且封装药物的结晶峰消失。 NLCs在低载药量下比SLNs释放的药物更快,而在高载药量下从SLNs和NLCs释放的药物没有显着差异。然而,从两种制剂中观察到持续/延长的药物释放。此外,这项研究表明药物释放实验应考虑产品的最终应用(局部/口服/胃肠外)来设计。关于稳定性,在25°C时,NLC表现出比SLN更好的稳定性(就尺寸,PI,EE和L而言)。此外,与新鲜NLC相比,储存3个月后NLC的药物释放曲线没有显着差异,而在SLN的情况下,观察到药物释放速率的显着变化。因此,NLC比SLN具有优势。

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