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利用基于脂质的纳米耳蜗结构进行靶向治疗递送:解决制剂瓶颈与进展

Harnessing lipid based nanocochleates for targeted therapeutic delivery: Addressing formulation bottlenecks and advancements.

作者信息

Mahanur Vishal B, Khandale Nikhil Bhimsing, Tekade Mayur Sanjay, Singh Sachin Kumar

机构信息

Kamalprakash Pharmacy College and Research Centre, Kherda, Maharashtra 444107, India.

Department of Pharmaceutical Quality Assurance, L. J. Institute of Pharmacy, L J University, Ahmedabad, Gujarat, India.

出版信息

Colloids Surf B Biointerfaces. 2026 Feb;258:115287. doi: 10.1016/j.colsurfb.2025.115287. Epub 2025 Nov 19.

DOI:10.1016/j.colsurfb.2025.115287
PMID:41265316
Abstract

Novel lipid-based drug delivery systems have gained considerable attention in recent years, with nanocochleates are emerging as a particularly promising lipid-based delivery system, recognized for their ability to enhance the stability, bioavailability, and site-directed delivery of a broad spectrum of therapeutic and nutraceutical agents. Nanocochleates are supramolecular, cylindrical lipid-based carriers formed through the interaction of negatively charged phospholipid such as phosphatidylserine with divalent cations like calcium. Their unique multilamellar structure imparts high physicochemical stability, enabling efficient encapsulation and protection of both hydrophilic and hydrophobic bioactives from environmental and physiological degradation. Compared to conventional lipid-based systems such as liposomes or solid lipid nanoparticles, nanocochleates provide sustained release, improved gastrointestinal stability, and reduced systemic toxicity, making them suitable for oral, mucosal, and systemic administration. Applications include both pharmaceutical and nutraceutical sectors, including functional foods, where nanocochleates enhance the solubility, sensory properties, and shelf-life of bioactives such as curcumin, vitamin D₃, and omega-3 fatty acids. Various formulation techniques, including the liposome-to-cochleate transition, trapping methods, and freeze-drying, have been developed to optimize particle size, entrapment efficiency, and release behavior. Despite their potential, key challenges remain in the form of large-scale production, batch consistency, regulatory validation, and long-term safety assessment. This review highlights the formulation strategies, functional attributes, and biomedical relevance of nanocochleates while addressing their current limitations and translational prospects. Their distinct advantages underscore the importance of continued interdisciplinary efforts toward realizing their full potential in drug delivery and nutrition-based interventions.

摘要

近年来,新型脂质基药物递送系统受到了广泛关注,其中纳米耳蜗状结构作为一种特别有前景的脂质基递送系统崭露头角,因其能够提高多种治疗剂和营养剂的稳定性、生物利用度以及靶向递送能力而受到认可。纳米耳蜗状结构是超分子圆柱形脂质基载体,由带负电荷的磷脂(如磷脂酰丝氨酸)与二价阳离子(如钙)相互作用形成。其独特的多层结构赋予了高物理化学稳定性,能够有效封装和保护亲水性和疏水性生物活性物质免受环境和生理降解。与传统的脂质基系统(如脂质体或固体脂质纳米粒)相比,纳米耳蜗状结构具有缓释性、改善的胃肠道稳定性和降低的全身毒性,使其适用于口服、黏膜和全身给药。其应用涵盖制药和营养领域,包括功能性食品,在这些领域中,纳米耳蜗状结构可提高姜黄素、维生素D₃和ω-3脂肪酸等生物活性物质的溶解度、感官特性和保质期。已经开发了各种制剂技术,包括脂质体向耳蜗状结构的转变、包封方法和冷冻干燥,以优化粒径、包封效率和释放行为。尽管它们具有潜力,但在大规模生产、批次一致性、监管验证和长期安全性评估方面仍存在关键挑战。本综述强调了纳米耳蜗状结构的制剂策略、功能特性和生物医学相关性,同时探讨了它们目前的局限性和转化前景。它们的独特优势凸显了持续跨学科努力以充分发挥其在药物递送和基于营养的干预措施中全部潜力的重要性。

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