高载药固体脂质纳米颗粒、纳米结构脂质载体和纳米乳用于双重递送HIV药物达若那韦和利托那韦

Q3 Materials Science
Heba Elkateb , Helen Cauldbeck , Edyta Niezabitowska , Cameron Hogarth , Keith Arnold , Steve Rannard , Tom O. McDonald
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引用次数: 2

摘要

药物递送方法可用于提高目前用于治疗艾滋病毒的抗逆转录病毒药物的生物利用度。脂质纳米载体是很有吸引力的药物递送载体,这些系统可以根据其脂质组成分为固体脂质纳米颗粒(sln)、纳米结构脂质载体(nlc)和纳米乳液(NEs)。为了开发用于治疗HIV的高载药量纳米制剂,我们分别以Imwitor 900k和大豆油为固体和液体脂质,研究了影响sln、NLCs和NEs比较生产的因素。这些纳米制剂含有达那韦(DRV)和利托那韦(RTV)的治疗相关药物混合物。我们使用了一种简单的纳米沉淀法,不需要对脂相进行任何加热,并筛选了三个关键的配方因素(脂质浓度、表面活性剂选择和载药量),以确定它们对配方颗粒性能和稳定性的影响。使用了两种不同的表面活性剂(brij78和Tween 80),它们对形成可行的纳米分散体的能力有显著影响;使用brij78作为表面活性剂,为我们的脂质提供了更可行的配方。测定有机相中脂质浓度为4mg /mL,以在可行配方和脂质负载之间实现良好的平衡,从而产生平均直径为200-300 nm的纳米颗粒。sln的载药量为10% w/w DRV/总脂质,NLCs和NEs的载药量可能达到20% w/w,这些值是脂质纳米制剂报道的最高值之一。所有制剂的包封率均≥92.5%。总的来说,这项研究显示了纳米沉淀法生产sln、NLCs和NEs的通用性。生产具有相同成分(脂类除外)的所有三种制剂的能力可能允许将来对生物特性进行直接比较。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

High drug loading solid lipid nanoparticles, nanostructured lipid carriers and nanoemulsions for the dual drug delivery of the HIV drugs darunavir and ritonavir

High drug loading solid lipid nanoparticles, nanostructured lipid carriers and nanoemulsions for the dual drug delivery of the HIV drugs darunavir and ritonavir

Drug delivery approaches can be used to enhance the bioavailability of current antiretroviral drugs used to treat HIV. Lipid nanocarriers are attractive drug delivery vehicles and these systems can be classified based on their lipid composition into solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs) and nanoemulsions (NEs). In order to develop high drug loading nanoformulations for the treatment of HIV, we investigate the factors that influence the comparative production of SLNs, NLCs and NEs with Imwitor 900k and soybean oil as the solid and liquid lipids respectively. These nanoformulations contained a therapeutically relevant drug mixture of darunavir (DRV) and ritonavir (RTV). We used a simple nanoprecipitation method that does not require any heating of the lipid phase and screened three key formulation factors (lipid concentration, surfactant selection and drug loading) in order to determine their effect on the particle properties and stability of the formulations. Two different surfactants were used, (Brij 78 and Tween 80) which had a significant effect on the ability to form a viable nanodispersion; using Brij 78 as the surfactant resulted in more viable formulations for our lipids. A concentration of the lipid in the organic phase of 4 mg/mL was determined to achieve a good balance between viable formulations and lipid loading resulting in nanoparticles with mean diameters ∼200–300 ​nm. Drug loadings of 10% w/w DRV/total lipid was achieved for SLNs, with loadings of 20% w/w was possible for NLCs and NEs, these values are amongst the highest reported for lipid nanoformulations. All formulations had encapsulation efficiencies of ≥92.5%. Overall, this study shows the versatility of the nanoprecipitation method for producing SLNs, NLCs and NEs. The ability to produce all three formulations with identical compositions (other than the lipids) may allow direct comparison of the biological properties in the future.

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来源期刊
JCIS open
JCIS open Physical and Theoretical Chemistry, Colloid and Surface Chemistry, Surfaces, Coatings and Films
CiteScore
4.10
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