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环糊精增强型固体脂质纳米粒(SLNs)和纳米结构脂质载体(NLCs)的制剂策略综述

A Review of Formulation Strategies for Cyclodextrin-Enhanced Solid Lipid Nanoparticles (SLNs) and Nanostructured Lipid Carriers (NLCs).

作者信息

Alloush Tarek, Demiralp Burcu

机构信息

Institute of Health Sciences, Istanbul University, Istanbul 34126, Türkiye.

Department of Pharmaceutical Technology, Faculty of Pharmacy, Istanbul University, Istanbul 34126, Türkiye.

出版信息

Int J Mol Sci. 2025 Jul 6;26(13):6509. doi: 10.3390/ijms26136509.

Abstract

The advancement of efficient drug delivery systems continues to pose a significant problem in pharmaceutical sciences, especially for compounds with limited water solubility. Lipid-based systems, including solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs), have emerged as viable options owing to their biocompatibility, capability to safeguard labile chemicals, and potential for prolonged release. Nonetheless, the encapsulation efficiency (EE) and release dynamics of these carriers can be enhanced by including cyclodextrins (CDs)-cyclic oligosaccharides recognized for their ability to form inclusion complexes with hydrophobic compounds. This article offers an extensive analysis of CD-modified SLNs and NLCs as multifunctional drug delivery systems. The article analyses the fundamental principles of these systems, highlighting the pre-complexation of the drug with cyclodextrins before lipid incorporation, co-encapsulation techniques, and surface adsorption after formulation. Attention is concentrated on the physicochemical interactions between cyclodextrins and lipid matrices, which influence essential factors such as particle size, encapsulation efficiency, and colloidal stability. The review includes characterization techniques, such as particle size analysis, zeta potential measurement, drug release studies, and Fourier-transform infrared spectroscopy (FT-IR)/Nuclear Magnetic Resonance (NMR) analyses. The study highlights the application of these systems across many routes of administration, including oral, topical, and mucosal, illustrating their adaptability and potential for targeted delivery. The review outlines current formulation challenges, including stability issues, drug leakage, and scalability concerns, and proposes solutions through advanced approaches, such as stimuli-responsive release mechanisms and computer modeling for system optimization. The study emphasizes the importance of regulatory aspects and outlines future directions in the development of CD-lipid hybrid nanocarriers, showcasing its potential to revolutionize the delivery of poorly soluble drugs.

摘要

高效药物递送系统的发展在制药科学领域仍然是一个重大问题,尤其是对于水溶性有限的化合物。基于脂质的系统,包括固体脂质纳米粒(SLNs)和纳米结构脂质载体(NLCs),因其生物相容性、保护不稳定化学物质的能力以及延长释放的潜力而成为可行的选择。尽管如此,通过加入环糊精(CDs)——一种以能够与疏水性化合物形成包合物而闻名的环状寡糖,可以提高这些载体的包封效率(EE)和释放动力学。本文对CD修饰的SLNs和NLCs作为多功能药物递送系统进行了广泛分析。文章分析了这些系统的基本原理,强调了在脂质掺入之前药物与环糊精的预络合、共包封技术以及制剂后的表面吸附。重点关注环糊精与脂质基质之间的物理化学相互作用,这些相互作用会影响诸如粒径、包封效率和胶体稳定性等关键因素。综述包括表征技术,如粒径分析、zeta电位测量、药物释放研究以及傅里叶变换红外光谱(FT-IR)/核磁共振(NMR)分析。该研究突出了这些系统在包括口服、局部和粘膜在内的多种给药途径中的应用,说明了它们的适应性和靶向递送潜力。综述概述了当前制剂面临的挑战,包括稳定性问题、药物泄漏和可扩展性问题,并通过先进方法提出了解决方案,如刺激响应释放机制和用于系统优化的计算机建模。该研究强调了监管方面的重要性,并概述了CD-脂质杂化纳米载体开发的未来方向,展示了其在难溶性药物递送方面带来变革的潜力。

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