含有巴巴苏油的聚合纳米颗粒:一种用于控制亲水化合物释放的药物递送系统

IF 3.4 3区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
João Vitor Raupp de Oliveira , Pedro Leardin Silveira , Gabriela Spingolon , Gabriel Antonio Lopes Alves , Flávia Pires Peña , Tanira Alessandra Silveira Aguirre
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引用次数: 0

摘要

在纳米尺度上制备不同的药物递送系统以改善药物配方的性能,例如纳米颗粒或纳米乳剂。聚合物纳米颗粒被用于包封药物,因为这些载体具有控制药物递送、将分子运输到特定组织、保护药物和提高药物生物利用度的一些特性。当使用纳米胶囊时,包被不同的亲水或亲脂分子的一个基本参数是核心的特性。巴巴苏油(BBS)是巴西的一种天然产品,主要由短链饱和脂肪酸组成。BBS具有较高的亲水-亲脂平衡(HLB),这可能促进了油与亲水药物的相互作用。在这项研究中,我们开发并表征了含有巴巴苏油的颗粒,在核心中单独或与山梨糖单硬脂酸酯(Span®60)或中链甘油三酯(MCT)结合,以测试不同的HLB并评估模型亲水性分子的包封性。使用不同的技术来表征所有制剂的大小和分布,并通过透析技术进行体外药物释放。BBS的月桂酸和肉豆蔻酸含量分别为46.05±1.11%和15.38±0.06%;皂化指数为248.87±0.64 mg KOH / g,过氧化指数表明油无氧化。室内携带溶剂的蒸发或压力的降低影响颗粒的大小;然而,所有的z-平均值都小于220 nm。水相与有机相之比为2.8的纳米颗粒被认为足以包封双氯芬酸钠。BBS + MCT、BBS和BBS + Span®60制备的纳米粒子的粒径/zeta电位分别为189.83±7.86 nm /−10.39±2.52 mV、156.80±4.77 nm /−9.27±4.61 mV和168.87±5.22 nm /−12.98±4.66 mV。所有制剂的药物含量均接近理论量(1.0 mg mL−1),三种纳米颗粒的释放谱无差异。仅含巴巴苏油的配方对双氯芬酸钠的包封率为66.78±15.62%,在所有试验配方中最高。结果表明,含有BBS的新型纳米颗粒促进了模型亲水分子的包封性,而其他成分可以改变分子的亲水性和包封性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Polymeric nanoparticles containing babassu oil: A proposed drug delivery system for controlled release of hydrophilic compounds

Polymeric nanoparticles containing babassu oil: A proposed drug delivery system for controlled release of hydrophilic compounds

Different drug delivery systems are prepared on the nanoscale to improve performance in drug formulations, such as nanoparticles or nanoemulsions. Polymeric nanoparticles have been used to encapsulate drugs for several applications because of some characteristics of these carriers to control drug delivery, transport molecules to a specific tissue, protect the drugs, and increase drug bioavailability. When using nanocapsules, an essential parameter for encapsulating different hydrophilic or lipophilic molecules is the characteristics of the core. Babassu oil (BBS) is a natural product from Brazil, composed majoritary of short-chain saturated fatty acids. BBS has an elevated hydrophilic-lipophilic balance (HLB), which may promote interaction of the oil with hydrophilic drugs. In this study, we developed and characterized particles containing babassu oil, solely or combined with sorbitan monostearate (Span® 60) or medium chain triglycerides (MCT) in the core to test different HLB and evaluated the encapsulation of a model hydrophilic molecule. Different techniques were used to characterize all formulations in terms of size and distribution, and in vitro drug release by dialysis technique was performed. The BBS was also characterized and presented 46,05 ± 1,11% and 15,38 ± 0,06% of lauric and myristic acid, respectively; saponification index of 248.87 ± 0.64 mg of KOH per gram of BBS, and no oxidation of the oil was indicated by means of peroxide index. Evaporation of solvent carried in the room or reduced pressure influenced the particles' size; nevertheless, all had a z-average smaller than 220 nm. Nanoparticles with a ratio among aqueous phase and organic phase of 2.8 were considered adequate to encapsulate diclofenac sodium. The particles size/zeta potential were 189.83 ± 7.86 nm / − 10.39 ± 2.52 mV, 156.80 ± 4.77 nm / − 9.27 ± 4.61 mV, and 168.87 ± 5.22 nm / − 12.98 ± 4.66 mV to nanoparticles prepared with BBS + MCT, BBS, and BBS + Span® 60, respectively. All formulations exhibited an amount of drug content close to the theoretical amount (1.0 mg mL−1), and no difference was observed in the release profile among the three nanoparticles. Formulation containing only babassu oil in the core displayed 66.78 ± 15.62% of encapsulation efficiency to diclofenac sodium, the highest value among all formulations tested. Results demonstrate that the innovative nanoparticles containing BBS promote the encapsulation of a model hydrophilic molecule, and other components can be evaluated to change the core’s hydrophilicity and encapsulation of molecules.

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来源期刊
Chemistry and Physics of Lipids
Chemistry and Physics of Lipids 生物-生化与分子生物学
CiteScore
7.60
自引率
2.90%
发文量
50
审稿时长
40 days
期刊介绍: Chemistry and Physics of Lipids publishes research papers and review articles on chemical and physical aspects of lipids with primary emphasis on the relationship of these properties to biological functions and to biomedical applications. Accordingly, the journal covers: advances in synthetic and analytical lipid methodology; mass-spectrometry of lipids; chemical and physical characterisation of isolated structures; thermodynamics, phase behaviour, topology and dynamics of lipid assemblies; physicochemical studies into lipid-lipid and lipid-protein interactions in lipoproteins and in natural and model membranes; movement of lipids within, across and between membranes; intracellular lipid transfer; structure-function relationships and the nature of lipid-derived second messengers; chemical, physical and functional alterations of lipids induced by free radicals; enzymatic and non-enzymatic mechanisms of lipid peroxidation in cells, tissues, biofluids; oxidative lipidomics; and the role of lipids in the regulation of membrane-dependent biological processes.
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