Bensa Veronica, Calarco Enzo, Giusto Elena, Perri Patrizia, Corrias Maria Valeria, Ponzoni Mirco, Brignole Chiara, Pastorino Fabio
Laboratory of Experimental Therapies in Oncology, IRCCS Istituto Giannina Gaslini, 16147 Genoa, Italy.
Pharmaceuticals (Basel). 2021 Aug 26;14(9):854. doi: 10.3390/ph14090854.
Retinoids are a class of natural and synthetic compounds derived from vitamin A. They are involved in several biological processes like embryogenesis, reproduction, vision, growth, inflammation, differentiation, proliferation, and apoptosis. In light of their important functions, retinoids have been widely investigated for their therapeutic applications. Thus far, their use for the treatment of several types of cancer and skin disorders has been reported. However, these therapeutic agents present several limitations for their widespread clinical translatability, i.e., poor solubility and chemical instability in water, sensitivity to light, heat, and oxygen, and low bioavailability. These characteristics result in internalization into target cells and tissues only at low concentration and, consequently, at an unsatisfactory therapeutic dose. Furthermore, the administration of retinoids causes severe side-effects. Thus, in order to improve their pharmacological properties and circulating half-life, while minimizing their off-target uptake, various retinoids delivery systems have been recently developed. This review intends to provide examples of retinoids-loaded nano-delivery systems for cancer treatment. In particular, the use and the therapeutic results obtained by using fenretinide-loaded liposomes against neuroectodermal-derived tumors, such as melanoma, in adults, and neuroblastoma, the most common extra-cranial solid tumor of childhood, will be discussed.
类视黄醇是一类源自维生素A的天然和合成化合物。它们参与多种生物学过程，如胚胎发育、生殖、视觉、生长、炎症、分化、增殖和细胞凋亡。鉴于其重要功能，类视黄醇已被广泛研究其治疗应用。迄今为止，已有报道其用于治疗多种类型的癌症和皮肤疾病。然而，这些治疗剂在广泛的临床转化方面存在若干限制，即水溶性差、化学稳定性低、对光、热和氧气敏感以及生物利用度低。这些特性导致仅在低浓度下才能内化到靶细胞和组织中，因此治疗剂量不理想。此外，类视黄醇的给药会引起严重的副作用。因此，为了改善其药理性质和循环半衰期，同时尽量减少其非靶向摄取，最近开发了各种类视黄醇递送系统。本综述旨在提供用于癌症治疗的载类视黄醇纳米递送系统的实例。特别是，将讨论使用载有芬维A胺的脂质体治疗成人神经外胚层来源的肿瘤（如黑色素瘤）和儿童最常见的颅外实体瘤神经母细胞瘤的用途和治疗结果。
