Paroxetine HCl-loaded hybrid nanoparticles for intranasal application to brain delivery: evaluation and cell culture studies

IF 2.6 4区 材料科学 Q3 CHEMISTRY, MULTIDISCIPLINARY
Elif Simsek, Ozge Esim, Canan Hascicek
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引用次数: 0

Abstract

Depression, ranked as the fourth leading cause of disability worldwide, is typically treated with oral antidepressants. However, the inability of this treatment to achieve the intended effect prompts the search for alternative methods. The aim of this research was to develop a paroxetine HCl-loaded lipid-polymer-based nanoparticulate drug delivery system for depression treatment via intranasal administration. Lipid-polymer hybrid nanoparticles were synthesized by using a modified double-emulsion solvent evaporation method and characterized in terms of physicochemical properties. The permeability and cytotoxicity of the nanoparticles were investigated on the Caco-2 cell line. The developed lipid-polymer-based nanoparticles were functionalized with chitosan to enhance the permeability of the nanoparticles through the blood–brain barrier. The optimum nanoparticle formulation was achieved at about 300 nm and a low polydispersity index. Paroxetine HCl, a highly water-soluble drug, was encapsulated into nanoparticles with an encapsulation efficiency of 77.144%. The cationic nanoparticles exhibited mucoadhesive characteristics, which support the permeability through the Caco-2 cell monolayer. Consequently, the proposed nanoformulation exhibited significant potential for treating depression intranasally.

Abstract Image

帕罗西汀hcl负载混合纳米颗粒鼻内应用于脑递送:评估和细胞培养研究
抑郁症是全球第四大致残原因,通常用口服抗抑郁药治疗。然而,这种治疗方法无法达到预期效果,这促使人们寻找替代方法。本研究的目的是开发一种帕罗西汀hcl负载的脂质聚合物纳米颗粒药物输送系统,通过鼻内给药治疗抑郁症。采用改进的双乳液溶剂蒸发法制备了脂聚合物杂化纳米颗粒,并对其理化性质进行了表征。在Caco-2细胞株上研究了纳米颗粒的渗透性和细胞毒性。制备的脂质聚合物基纳米颗粒经壳聚糖功能化,增强了其通过血脑屏障的渗透性。最佳的纳米颗粒配方在300 nm左右,具有较低的多分散指数。盐酸帕罗西汀是一种高水溶性药物,其包封率为77.144%。阳离子纳米颗粒具有黏附特性,支持Caco-2细胞单层的渗透性。因此,所提出的纳米制剂在鼻内治疗抑郁症方面表现出显著的潜力。
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来源期刊
Journal of Nanoparticle Research
Journal of Nanoparticle Research 工程技术-材料科学:综合
CiteScore
4.40
自引率
4.00%
发文量
198
审稿时长
3.9 months
期刊介绍: The objective of the Journal of Nanoparticle Research is to disseminate knowledge of the physical, chemical and biological phenomena and processes in structures that have at least one lengthscale ranging from molecular to approximately 100 nm (or submicron in some situations), and exhibit improved and novel properties that are a direct result of their small size. Nanoparticle research is a key component of nanoscience, nanoengineering and nanotechnology. The focus of the Journal is on the specific concepts, properties, phenomena, and processes related to particles, tubes, layers, macromolecules, clusters and other finite structures of the nanoscale size range. Synthesis, assembly, transport, reactivity, and stability of such structures are considered. Development of in-situ and ex-situ instrumentation for characterization of nanoparticles and their interfaces should be based on new principles for probing properties and phenomena not well understood at the nanometer scale. Modeling and simulation may include atom-based quantum mechanics; molecular dynamics; single-particle, multi-body and continuum based models; fractals; other methods suitable for modeling particle synthesis, assembling and interaction processes. Realization and application of systems, structures and devices with novel functions obtained via precursor nanoparticles is emphasized. Approaches may include gas-, liquid-, solid-, and vacuum-based processes, size reduction, chemical- and bio-self assembly. Contributions include utilization of nanoparticle systems for enhancing a phenomenon or process and particle assembling into hierarchical structures, as well as formulation and the administration of drugs. Synergistic approaches originating from different disciplines and technologies, and interaction between the research providers and users in this field, are encouraged.
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