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含巴巴苏油的聚合物纳米粒:一种用于控制释放亲水性化合物的药物传递系统。

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

机构信息

Curso de Química Medicinal, Universidade Federal de Ciências da Saúde de Porto Alegre, 90050-170, Porto Alegre, RS, Brasil.

Programa de Pós-Graduação em Biociências, Universidade Federal de Ciências da Saúde de Porto Alegre, 90050-170, Porto Alegre, RS, Brasil.

出版信息

Chem Phys Lipids. 2023 Jul;253:105304. doi: 10.1016/j.chemphyslip.2023.105304. Epub 2023 Apr 18.

Abstract

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), 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.

摘要

不同的药物输送系统在纳米尺度上被制备以改善药物配方中的性能,例如纳米粒子或纳米乳液。由于这些载体具有控制药物释放、将分子输送到特定组织、保护药物和提高药物生物利用度等特性,因此已经使用聚合物纳米粒子来包封药物。当使用纳米胶囊时,包封不同亲水性或亲脂性分子的一个重要参数是核心的特性。巴巴苏油(BBS)是一种来自巴西的天然产物,主要由短链饱和脂肪酸组成。BBS 的亲水亲脂平衡(HLB)较高,可能促进油与亲水性药物的相互作用。在这项研究中,我们开发并表征了含有巴巴苏油的粒子,仅含有或与失水山梨醇单硬脂酸酯(Span®60)或中链甘油三酯(MCT)一起作为核心,以测试不同的 HLB,并评估模型亲水分子的包封。使用不同的技术根据大小和分布对所有配方进行了表征,并通过透析技术进行了体外药物释放。还对 BBS 进行了表征,其分别含有 46.05±1.11%和 15.38±0.06%的月桂酸和肉豆蔻酸;皂化值为每克 BBS 248.87±0.64mg 的 KOH,并且通过过氧化物指数表明油没有氧化。在室温或减压下蒸发溶剂会影响粒子的大小;然而,所有粒子的 Z 均平均值均小于 220nm。水相和有机相之间的比例为 2.8 的纳米粒子被认为足以包封双氯芬酸钠。粒子的大小/ζ电位分别为 189.83±7.86nm/-10.39±2.52mV、156.80±4.77nm/-9.27±4.61mV 和 168.87±5.22nm/-12.98±4.66mV,分别对应于含有 BBS+MCT、BBS 和 BBS+Span®60 的纳米粒子。所有配方的药物含量都接近理论值(1.0mg/mL),并且在三种纳米粒子的释放曲线之间没有观察到差异。仅含有巴巴苏油的核心配方对双氯芬酸钠的包封效率为 66.78±15.62%,是所有测试配方中最高的。结果表明,含有 BBS 的创新纳米粒子能够包封模型亲水分子,并且可以评估其他成分来改变核心的亲水性和分子包封。

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