Ethyl oleate-containing nanostructured lipid carriers improve oral bioavailability of trans-ferulic acid ascompared with conventional solid lipid nanoparticles.
Ethyl oleate-containing nanostructured lipid carriers improve oral bioavailability of trans-ferulic acid ascompared with conventional solid lipid nanoparticles.
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DOI：
10.1016/j.ijpharm.2016.06.131
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发表时间：
2016-09
影响因子：
5.8
通讯作者：
Yongtai Zhang;Zhe Li;Kai Zhang;Gang Yang;Zhi Wang;Jihui Zhao;Rongfeng Hu;Nianping Feng
中科院分区：
文献类型：
--
作者：
Yongtai Zhang;Zhe Li;Kai Zhang;Gang Yang;Zhi Wang;Jihui Zhao;Rongfeng Hu;Nianping Feng
反式阿魏酸（TFA）具有抗氧化、抗炎和心脏保护作用，但当以标准剂量常规给药时，其在水中的溶解度差导致口服生物利用度不令人满意。然而，TFA有限的生物利用度可以通过在纳米结构脂质载体（NLC）中递送来克服。本研究采用基于微乳液（ME）的方法制备了以油酸乙酯为液体脂质成分、二十二烷酸甘油酯为固体脂质成分的NLC。然后将这些NLC和固体脂质纳米颗粒（SLN）用作TFA的载体。比较了它们的包封率、贮存稳定性、体外释药特性和体内药代动力学。NLC制剂提供的药物包封效率显著高于使用单一固体脂质制备的SLN制剂。此外，分散在NLC制剂的无序二元脂质基质中的TFA比SLN制剂中的TFA更稳定，因此在储存期间显示出更少的从媒介物中排出。在体内药代动力学研究中，NLC TFA制剂产生的Cmax和AUC大于SLN制剂和TFA水混悬液产生的Cmax和AUC。这表明，通过包装在NLC中，TFA的口服生物利用度显著提高。因此，NLC是口服TFA给药的有前途的载体，与SLN相比具有显著优势。
trans-Ferulic acid (TFA) has antioxidative, anti-inflammatory, and cardioprotective effects, but its poor solubility in water results in unsatisfactory oral bioavailability when administered conventionally at a standard dosage. However, the limited bioavailability of TFA can be overcome by delivering it in nanostructured lipid carriers (NLCs). In this study, a microemulsion (ME)-based method was used to prepare NLCs with ethyl oleate as the liquid lipid component and glyceryl behenate as the solid lipid component. These NLCs and solid lipid nanoparticles (SLNs) were then used as vehicles for TFA. Their entrapment efficiencies (EE), stability during storage,in vitrorelease profiles, andin vivopharmacokinetics were compared. The NLC formulation afforded a drug entrapment efficiency that was significantly greater than that of the SLN formulation, which was made using a single solid lipid. Furthermore, the TFA that was dispersed in the disordered binary lipid matrix of the NLC formulation was more stable than that in the SLN formulation, and thus showed less expulsion from the vehicle during storage. Inin vivopharmacokinetic studies, the NLC TFA formulation yielded a greater Cmaxand AUC than that produced by the SLN formulation and an aqueous TFA suspension. This showed that the oral bioavailability of TFA was markedly improved by packaging in NLCs. NLCs are thus a promising vehicle for oral TFA administration, with significant advantages over SLNs.