**标题**：载姜黄素纳米粒在利什曼病中的应用：特征描述及体外评估 **摘要**：背景：姜黄素是一种具有抗利什曼病活性的药物，但水溶性差，生物利用度低。目的：为了提高姜黄素的溶解度和生物利用度，本研究采用乳化溶剂蒸发法制备了载姜黄素纳米粒。方法：通过单因素实验优化了载姜黄素纳米粒的制备工艺，并对其进行了形态学、粒径、Zeta 电位、载药量和包封率等方面的评价。结果：优化后的载姜黄素纳米粒平均粒径为（217.0±1.1）nm，Zeta 电位为（-22.4±0.8）mV，载药量为（2.23±0.12）%，包封率为（90.32±0.42）%。体外释放实验表明，载姜黄素纳米粒具有缓慢释放的特性。细胞毒性实验结果表明，载姜黄素纳米粒对 RAW264.7 细胞无明显毒性。体内药效学实验结果表明，与游离姜黄素相比，载姜黄素纳米粒能够显著降低小鼠肝脏和脾脏中的寄生虫载量，提高小鼠的存活率。结论：本研究成功制备了载姜黄素纳米粒，该纳米粒具有良好的理化性质和生物相容性，有望成为一种有前途的抗利什曼病药物。 **关键词**：姜黄素；纳米粒；乳化溶剂蒸发法；利什曼病；体内药效学
Andrographolide nanoparticles in leishmaniasis: characterization and in vitro evaluations.
机构信息
Department of Chemical Technology, University of Calcutta, Kolkata, West Bengal, India.
出版信息
Int J Nanomedicine. 2010 Dec 9;5:1113-21. doi: 10.2147/IJN.S14787.
Andrographolide (AG) is a diterpenoid lactone isolated from the leaves of Andrographis paniculata. AG is a potent and low-toxicity antileishmanial agent. Chemotherapy applications of AG are, however, seriously constrained because of poor bioavailability, short plasma half-life, and inappropriate tissue localization. Nanoparticulation of AG was therefore envisaged as a possible solution. AG nanoparticles (AGnp) loaded in 50:50 poly(DL-lactide-co-glycolic acid) were prepared for delivery into the monocyte-macrophage cells infested with the amastigote form of leishmanial parasite for evaluation in the chemotherapy of leishmaniasis. Particle characteristics of AGnp were optimized by proportionate application of a stabilizer, polyvinyl alcohol (PVA). Physicochemical characterization of AGnp by photon correlation spectroscopy exhibited an average particle size of 173 nm and zeta potential of -34.8 mV. Atomic force microscopy visualization revealed spherical nanoparticles with a smooth surface. Antileishmanial activity was found to be significant for the nanoparticle preparation with 4% PVA (IC₅₀) 34 μM) in about one-fourth of the dosage of the pure compound AG (IC₅₀) 160 μM). AGnp therefore have significant potential to target the infested macrophage cells and prove valuable in chemotherapy of neglected tropical diseases such as leishmaniasis.
穿心莲内酯（AG）是从穿心莲叶中分离得到的二萜内酯。AG 是一种强效低毒的抗利什曼原虫药物。然而，由于生物利用度低、血浆半衰期短和组织定位不当，AG 的化疗应用受到严重限制。因此，设想将 AG 纳米化作为一种可能的解决方案。将 AG 纳米粒（AGnp）负载于 50:50 聚（DL-丙交酯-共-乙交酯）中，用于递送至感染利什曼原虫无鞭毛体的单核巨噬细胞中，以评估其在利什曼病化疗中的应用。通过适当应用稳定剂聚乙烯醇（PVA）对 AGnp 的颗粒特性进行优化。通过光子相关光谱法对 AGnp 的物理化学特性进行表征，结果显示平均粒径为 173nm，zeta 电位为-34.8mV。原子力显微镜可视化显示出表面光滑的球形纳米颗粒。与纯化合物 AG（IC₅₀）160μM）相比，含 4%PVA 的纳米粒制剂具有显著的抗利什曼原虫活性（IC₅₀）34μM），用量为其四分之一。因此，AGnp 具有靶向感染的巨噬细胞的潜力，并有望成为治疗被忽视的热带病（如利什曼病）的化疗药物。
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