新型肉碱脂质体制剂的开发和体外表征。

IF 3.6 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Stefano Russo, Anna Privitera, Giuliana Greco, Lucia Di Pietro, Vincenzo Cardaci, Giuseppe Carota, Maria Grazia Sarpietro, Giuseppe Caruso
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引用次数: 0

摘要

肌肽是一种内源性二肽,具有多模式作用机制。然而,血清和细胞质肌肽酶大大降低了它的生物利用度,从而限制了它的临床潜力。基于此,不同的研究小组致力于开发新的策略,不仅能防止其快速代谢,还能改善其分布和特异性靶向性。在本研究中,介绍了含有肌肽的新型脂质体制剂的开发和体外表征。首先研究了通过薄层水合挤压法生产的纳米脂质体的理化稳定性。光子相关光谱法和电泳光散射法评估了制剂的稳定性,结果表明,在长达两个月的时间里,制剂具有很强的均一性。通过动态光散射和电泳光散射测定了粒度、多分散指数和 zeta 电位,结果表明制剂的电荷几乎呈中性,并能有效地包裹肌肽。通过扫描电子显微镜进行的形态学评估显示了良好的一致性和多分散性。差示扫描量热法测量结果表明,肌肽能够稳定大的单拉米尔囊泡。最后,新开发的肌肽脂质体制剂在人类小胶质细胞中也显示出良好的安全性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and in vitro characterization of new carnosine-loaded liposomal formulations.

Carnosine is an endogenous dipeptide characterized by a multimodal mechanism of action. However, its clinical potential is limited by serum and cytosolic carnosinases, which significantly reduce its bioavailability. Based on that, different research groups have worked on the development of new strategies able not only to prevent its rapid metabolization but also to improve its distribution and specific targeting. In the present study, the development and in vitro characterization of new liposomal formulations loaded with carnosine are described. Nanoliposomes, produced through Thin-Layer Hydration followed by Extrusion method, were first investigated for their physicochemical stability. Photon correlation spectroscopy and electrophoretic light scattering, assessing the stability of the formulations, showed a strong homogeneity-oriented tendency for up to two months. Particle size, polydispersity index, and zeta potential were determined through dynamic light scattering and electrophoretic light scattering, demonstrating an almost neutral charge of the formulation and an effective encapsulation of carnosine. The morphology assessment performed via scanning electron microscopy showed good conformity and polydispersity. Differential scanning calorimetry measurements suggest the ability of carnosine to stabilize the large unilamellar vesicles. Lastly, the newly developed carnosine-loaded liposomal formulations also showed a good safety profile in human microglia.

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来源期刊
Journal of Liposome Research
Journal of Liposome Research 生物-生化与分子生物学
CiteScore
10.50
自引率
2.30%
发文量
24
审稿时长
3 months
期刊介绍: The Journal of Liposome Research aims to publish original, high-quality, peer-reviewed research on the topic of liposomes and related systems, lipid-based delivery systems, lipid biology, and both synthetic and physical lipid chemistry. Reviews and commentaries or editorials are generally solicited and are editorially reviewed. The Journal also publishes abstracts and conference proceedings including those from the International Liposome Society. The scope of the Journal includes: Formulation and characterisation of systems Formulation engineering of systems Synthetic and physical lipid chemistry Lipid Biology Biomembranes Vaccines Emerging technologies and systems related to liposomes and vesicle type systems Developmental methodologies and new analytical techniques pertaining to the general area Pharmacokinetics, pharmacodynamics and biodistribution of systems Clinical applications. The Journal also publishes Special Issues focusing on particular topics and themes within the general scope of the Journal.
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