Recent advances in oral delivery of drugs and bioactive natural products using solid lipid nanoparticles as the carriers.
Recent advances in oral delivery of drugs and bioactive natural products using solid lipid nanoparticles as the carriers.
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DOI：
10.1016/j.jfda.2017.02.001
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发表时间：
2017-04
影响因子：
3.6
通讯作者：
Fang, Jia-You
中科院分区：
文献类型：
--
作者：
Lin, Chih-Hung;Chen, Chun-Han;Lin, Zih-Chan;Fang, Jia-You
胃肠道中的化学和酶屏障阻碍了许多不稳定药物的口服递送。胃肠道上皮也导致许多药物的渗透性差。水溶性差的药物难以在胃肠道中溶解，导致生物利用度低。纳米医学为提高口服药物的给药效率提供了机会。固体脂质纳米颗粒（sln）是由完整的固体脂质基质组成的新一代脂质纳米颗粒。与传统制剂相比，用于口服的sln具有多种优点，包括溶解度增加、稳定性增强、改善上皮通透性和生物利用度、延长半衰期、组织靶向性和最小的副作用。sln的无毒辅料和复杂的材料工程使纳米颗粒具有可控的物理化学性质，可通过粘膜或淋巴运输穿透胃肠道。在这篇综述中，我们重点介绍了用于疾病治疗的sln的最新进展。口服sln的近期应用包括癌症、中枢神经系统相关疾病、心血管相关疾病、感染、糖尿病和骨质疏松症的治疗。除了在SLN中可能是活性货物的药物外，一些具有药理活性的天然化合物也适合用于SLN包封，以提高口服生物利用度。本文系统地介绍了载药和载天然化合物sln纳米医学技术的概念和改进机制。
Chemical and enzymatic barriers in the gastrointestinal (GI) tract hamper the oral delivery of many labile drugs. The GI epithelium also contributes to poor permeability for numerous drugs. Drugs with poor aqueous solubility have difficulty dissolving in the GI tract, resulting in low bioavailability. Nanomedicine provides an opportunity to improve the delivery efficiency of orally administered drugs. Solid lipid nanoparticles (SLNs) are categorized as a new generation of lipid nanoparticles consisting of a complete solid lipid matrix. SLNs used for oral administration offer several benefits over conventional formulations, including increased solubility, enhanced stability, improved epithelium permeability and bioavailability, prolonged half-life, tissue targeting, and minimal side effects. The nontoxic excipients and sophisticated material engineering of SLNs tailor the controllable physicochemical properties of the nanoparticles for GI penetration via mucosal or lymphatic transport. In this review, we highlight the recent progress in the development of SLNs for disease treatment. Recent application of oral SLNs includes therapies for cancers, central nervous system-related disorders, cardiovascular-related diseases, infection, diabetes, and osteoporosis. In addition to drugs that may be active cargos in SLNs, some natural compounds with pharmacological activity are also suitable for SLN encapsulation to enhance oral bioavailability. In this article, we systematically introduce the concepts and amelioration mechanisms of the nanomedical techniques for drug- and natural compound-loaded SLNs.
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