Laboratório de Controle de Qualidade Farmacêutico/Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul (UFRGS), Av. Ipiranga, Porto Alegre, Brazil.
Department of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy.
Int J Pharm. 2019 Aug 15;567:118487. doi: 10.1016/j.ijpharm.2019.118487. Epub 2019 Jul 2.
Fucoxanthin (FUCO) is a marine carotenoid characterized by antiproliferative properties against hyperproliferative cells. The aim of this work was to design and develop nanostructured lipidic carriers (NLCs) based on bacuri butter and tucumã oil and loaded with FUCO, intended for skin application to prevent skin hyperproliferative diseases and in particular psoriasis. The presence of FUCO should control the hyperproliferation of skin diseased cells and the lipids forming the NLC core, rich in antioxidants and characterized by wound healing properties, should favor the restoring of skin integrity. NLCs were coated with chitosan (CS) to improve their biopharmaceutical properties (bio/mucoadhesion and wound healing) and to combine the advantages of lipidic nanoparticles with the biological properties of CS. Chitosan coated and non-coated NLC were prepared by means of high shear homogenization and characterized for chemico-physical and biopharmaceutical properties (in vitro biocompatibility and cell uptake towards normal dermal human fibroblasts). Moreover, the pharmacological activity of FUCO loaded in NLCs was assessed in psoriatic-like cellular model. NLCs were characterized by dimensions ranging from about 250 to 400 nm. Moreover, the CS coating and FUCO loading determined an increase of size. Moreover, TEM and zeta potential analysis confirmed the presence of CS coating on nanoparticle surface, thus conferring to nanoparticle good bioadhesion properties. NLCs uptake in fibroblasts was observed and NLC-FUCO-CS caused a reduction of cell viability with a less marked effect in fibroblasts rather than in psoriatic cells, highlighting the capability of this system to control skin hyperproliferation and inflammation. The loading of NLC-FUCO-CS in pullulan film should render NLCs application easy, without impair prompt interaction of the drug with the skin. Considering the overall results skin application of CS coated NLCs loaded with FUCO seems a promising approach to control skin hyperproliferation and to preserve skin integrity in psoriatic skin.
岩藻黄质（FUCO）是一种海洋类胡萝卜素，具有抗过度增殖细胞增殖的特性。本工作旨在设计和开发基于巴库利黄油和图库玛油的纳米结构脂质载体（NLC），并负载 FUCO，用于皮肤应用，以预防皮肤过度增殖性疾病，特别是银屑病。FUCO 的存在应控制皮肤病变细胞的过度增殖，而 NLC 核心富含抗氧化剂且具有伤口愈合特性的脂质应有利于皮肤完整性的恢复。用壳聚糖（CS）对 NLC 进行包被，以改善其生物药剂学特性（生物/黏膜黏附性和伤口愈合性），并结合脂质纳米粒的优势与 CS 的生物学特性。通过高剪切匀化制备壳聚糖包被和未包被的 NLC，并对其进行化学物理和生物药剂学性质（体外生物相容性和对正常皮肤人成纤维细胞的细胞摄取）的表征。此外，还评估了载于 NLC 中的 FUCO 的药理活性在银屑病样细胞模型中。NLC 的尺寸范围约为 250 至 400nm。此外，CS 包被和 FUCO 负载会导致粒径增大。此外，TEM 和 zeta 电位分析证实了 CS 涂层存在于纳米颗粒表面，从而赋予纳米颗粒良好的生物黏附特性。观察到 NLC 向成纤维细胞的摄取，NLC-FUCO-CS 导致细胞活力降低，而对成纤维细胞的影响不如对银屑病细胞的影响明显，这突出了该系统控制皮肤过度增殖和炎症的能力。将 NLC-FUCO-CS 载入普鲁兰薄膜中，应该使 NLC 的应用变得容易，而不会影响药物与皮肤的快速相互作用。考虑到整体结果，载有 FUCO 的 CS 包被 NLC 经皮给药似乎是控制皮肤过度增殖和维持银屑病皮肤完整性的一种有前途的方法。
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