Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas-UNICAMP, Campinas 13083-862, Brazil.
Molecules. 2021 Nov 17;26(22):6929. doi: 10.3390/molecules26226929.
Ideally, antineoplastic treatment aims to selectively eradicate cancer cells without causing systemic toxicity. A great number of antineoplastic agents (AAs) are available nowadays, with well-defined therapeutic protocols. The poor bioavailability, non-selective action, high systemic toxicity, and lack of effectiveness of most AAs have stimulated the search for novel chemotherapy protocols, including technological approaches that provide drug delivery systems (DDS) for gold standard medicines. Nanostructured lipid carriers (NLC) are DDS that contain a core of solid and lipid liquids stabilised by surfactants. NLC have high upload capacity for lipophilic drugs, such as the majority of AAs. These nanoparticles can be prepared with a diversity of biocompatible (synthetic or natural) lipid blends, administered by different routes and functionalised for targeting purposes. This review focused on the research carried out from 2000 to now, regarding NLC formulations for AAs (antimetabolites, antimitotics, alkylating agents, and antibiotics) encapsulation, with special emphasis on studies carried out in vivo. NLC systems for codelivery of AAs were also considered, as well as those for non-classical drugs and therapies (natural products and photosensitisers). NLC have emerged as powerful DDS to improve the bioavailability, targeting and efficacy of antineoplastics, while decreasing their toxic effect in the treatment of different types of cancer.
理想情况下，抗肿瘤治疗旨在选择性地根除癌细胞，而不引起全身毒性。如今，有大量的抗肿瘤药物（AAs），并有明确的治疗方案。大多数 AAs 的生物利用度低、非选择性作用、高全身毒性和缺乏有效性，这刺激了人们对新的化疗方案的研究，包括提供金标准药物的药物递送系统（DDS）的技术方法。纳米结构脂质载体（NLC）是一种 DDS，其中包含固体和脂质液体的核心，由表面活性剂稳定。NLC 对脂溶性药物（如大多数 AAs）具有高载药能力。这些纳米粒子可以用多种生物相容性（合成或天然）脂质混合物制备，通过不同的途径给药，并进行靶向功能化。本综述重点介绍了 2000 年至今关于 NLC 制剂用于包裹 AAs（抗代谢物、抗有丝分裂剂、烷化剂和抗生素）的研究，特别强调了体内研究。还考虑了用于 AAs 共递送的 NLC 系统，以及用于非经典药物和疗法（天然产物和光敏剂）的 NLC 系统。NLC 已成为提高抗肿瘤药物生物利用度、靶向性和疗效的有力 DDS，同时降低了它们在治疗不同类型癌症中的毒性作用。
