Müller Rainer H, Shegokar Ranjita, Keck Cornelia M
Department of Pharmaceutics, Biopharmaceutics & NutriCosmetics, Freie Universität Berlin, Germany.
Curr Drug Discov Technol. 2011 Sep;8(3):207-27. doi: 10.2174/157016311796799062.
In 1990, the lipid nanoparticles were invented in the laboratories, the first patent filings took place in 1991. The lipid nanoparticles were developed as alternative to traditional carriers such as polymeric nanoparticles and liposomes. After 20 years of lipid nanoparticles, the present state of development is reviewed - academic progress but also the development state of pharmaceutical products for the benefit of patients. Meanwhile many research groups are active worldwide, their results are reviewed which cover many different administration routes: dermal and mucosal, oral, intravenous/parenteral, pulmonary but also ocular. The lipid nanoparticles are also used for peptide/protein delivery, in gene therapy and various miscellaneous applications (e.g. vaccines). The questions of large scale production ability, accepted regulatory status of excipients, and - important for the public perception - lack of nanotoxicity are discussed, important pre-requisites for the use of each nanocarrier in products. Identical to the liposomes, the lipid nanoparticles entered first the cosmetic market, product examples are presented. Presently the pharmaceutical product development focuses on products for unmet needs and on niche products with lower development costs (e.g. ocular delivery), which can be realized also by smaller companies. A pharmaceutical perspective for the future is given, but also outlined the opportunities for non-pharmaceutical use, e.g. in nutraceuticals.
1990年，脂质纳米颗粒在实验室中被发明，1991年首次提交专利申请。脂质纳米颗粒作为传统载体（如聚合物纳米颗粒和脂质体）的替代品而被开发。在脂质纳米颗粒问世20年后，本文回顾了其发展现状——包括学术进展以及为患者造福的药品开发状况。与此同时，全球许多研究团队都很活跃，本文对他们的研究成果进行了综述，这些成果涵盖了许多不同的给药途径：皮肤和黏膜给药、口服、静脉内/肠胃外给药、肺部给药以及眼部给药。脂质纳米颗粒还用于肽/蛋白质递送、基因治疗以及各种其他应用（如疫苗）。文中讨论了大规模生产能力、辅料的公认监管状态以及——对公众认知很重要的——纳米毒性缺失等问题，这些都是每种纳米载体在产品中应用的重要先决条件。与脂质体一样，脂质纳米颗粒首先进入了化妆品市场，并列举了产品实例。目前，药品开发侧重于满足未满足的需求的产品以及开发成本较低的利基产品（如眼部给药），小公司也可以实现这些产品的开发。本文给出了药品未来的发展前景，同时也概述了非药品用途的机会，如在营养保健品中的应用。
