Scalia Santo, Young Paul M, Traini Daniela
Università di Ferrara, Dipartimento di Scienze Chimiche e Farmaceutiche , Ferrara , Italy.
Expert Opin Drug Deliv. 2015 Apr;12(4):583-99. doi: 10.1517/17425247.2015.980812. Epub 2014 Nov 13.
Solid lipid particles were introduced in the early 1990s as an alternative drug carrier system to emulsions, liposomes and polymeric microparticles. Although lipid nanoparticles have been the object of a substantial number of reviews, fewer are available on lipid microparticles (LMs), despite their distinct advantages, including biocompatibility, ease of production and characterisation, extended release properties and high loading.
This review presents an overview of the advantages and drawbacks of LMs, that is, lipid-based particles with dimensions in the micrometre range. Specific focus is on the role of the main excipients used for LM formulations, lipids and surfactants and their effects on LM properties. An update on preparation techniques and characterisation methods are also presented, with particular emphasis on more recent technologies. The interaction of LMs with biological systems and with cells in particular is reviewed. The various LM administration routes are examined, with special attention to most recent applications (i.e., pulmonary and nasal delivery).
LMs represent attractive and versatile carrier systems; however, their pharmaceutical applicability has been rather limited. Investigation on the use of LMs for less-established administration routes, such as pulmonary delivery, may provide further interest within the area of LM-based systems, both in industry and in the clinic.
固体脂质颗粒于20世纪90年代初被引入,作为乳液、脂质体和聚合物微粒的替代药物载体系统。尽管脂质纳米颗粒已成为大量综述的对象,但关于脂质微粒(LMs)的综述较少,尽管它们具有明显的优势,包括生物相容性、易于生产和表征、缓释特性以及高载药量。
本综述概述了脂质微粒(即尺寸在微米范围内的基于脂质的颗粒)的优缺点。特别关注用于脂质微粒制剂的主要辅料、脂质和表面活性剂的作用及其对脂质微粒性质的影响。还介绍了制备技术和表征方法的最新进展,尤其强调了最新技术。综述了脂质微粒与生物系统特别是与细胞的相互作用。研究了脂质微粒的各种给药途径,特别关注最新应用(即肺部和鼻腔给药)。
脂质微粒是有吸引力且通用的载体系统;然而,它们在制药方面的适用性相当有限。对脂质微粒用于不太成熟的给药途径(如肺部给药)的研究可能会在基于脂质微粒的系统领域引起更多关注,无论是在工业界还是临床。