Department of Anatomy and Structural Biology, University of Otago, Otago School of Medical Sciences, PO Box 913, Dunedin 9054, New Zealand.
Expert Opin Drug Deliv. 2010 Oct;7(10):1133-44. doi: 10.1517/17425247.2010.515584.
Self-assembling lipid-based liquid crystalline systems are a broad and active area of research. Of these mesophases, the cubic phase with its highly twisted bilayer and two non-intersecting water channels has been investigated extensively for drug delivery. The cubic phase has been shown to accommodate and control the release of drugs with varying physicochemical properties. Also, the lipids used to prepare these delivery systems are generally cheap, safe and biodegradable, making these systems highly attractive. Early research investigating the potential of cubic phases as delivery systems showed that several peptides or proteins entrapped within these gel-based systems showed retarded release. Furthermore, entrapment within the cubic phase protected the selected peptide or protein from chemical and physical degradation with its native confirmation and bioactivity retained.
In this review, the literature pertaining to the delivery of various bioactives from cubic liquid crystalline phases is examined, with a particular focus on peptides and proteins. The scope and limitations of the cubic phases in this respect and the future of cubic liquid crystalline systems as sustained delivery systems are highlighted.
The reader will be able to gain an understanding of the properties of the bicontinuous cubic phase and how its structural attributes make these systems desirable for sustained delivery of bioactives, in particular peptides and proteins, but also how these same structural properties have hindered progress towards clinical applications. Current strategies to overcome these issues will also be discussed.
The bicontinuous cubic phase offers great potential in the field of peptide and protein delivery, but limited research in this area precludes definite conclusions to its future in this respect.
自组装脂质基液晶系统是一个广泛而活跃的研究领域。在这些中间相中,具有高度扭曲双层和两个不相交的水通道的立方相已经被广泛研究用于药物传递。已经表明,立方相能够容纳和控制具有不同物理化学性质的药物的释放。此外,用于制备这些递送系统的脂质通常廉价、安全且可生物降解,这使得这些系统极具吸引力。早期研究表明,几种肽或蛋白质被包埋在这些基于凝胶的系统中,其释放速度会减慢。此外,包埋在立方相中可以保护所选的肽或蛋白质免受化学和物理降解,同时保持其天然构象和生物活性。
在这篇综述中,检查了关于各种生物活性物质从立方液晶相递送到的文献,特别关注肽和蛋白质。本文重点介绍了立方相在这方面的范围和局限性,以及立方液晶系统作为持续递药系统的未来。
读者将能够了解双连续立方相的性质以及其结构属性如何使这些系统成为生物活性物质,特别是肽和蛋白质持续递药的理想选择,但同样的结构属性也如何阻碍了其向临床应用的进展。还将讨论当前克服这些问题的策略。
双连续立方相在肽和蛋白质递药领域具有巨大的潜力,但该领域的研究有限,无法对其在这方面的未来做出明确的结论。