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含固体脂质纳米粒的热敏原位形成凝胶作为可控纳米颗粒递送系统的制备及其流变学、热学和侵蚀行为研究

Preparation of SLN-containing Thermoresponsive In-situ Forming Gel as a Controlled Nanoparticle Delivery System and Investigating its Rheological, Thermal and Erosion Behavior.

作者信息

Dorraj Golnar, Moghimi Hamid Reza

机构信息

Department of Pharmaceutics and Nanotechnology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

出版信息

Iran J Pharm Res. 2015 Spring;14(2):347-58.

Abstract

Various nanoparticles have been investigated as novel drug delivery systems, including solid lipid nanoparticles (SLNs). Due to their rapid clearance from systemic circulation, nanoparticles do not provide sustained action in most cases. Different strategies have been employed to overcome this problem. In this direction, the present study introduces erodible in-situ forming gel systems as potential vehicles for prolonged release of SLNs. SLNs were prepared by solidification of an oil-in-water microemulsion containing stearic acid, surfactants and co-surfactants. Nanoparticles were then dispersed in a thermosensitive Poloxamer 407 aqueous solution (sol) at 4 °C and their effects on gel forming ability, sol-gel transition and rheological behavior of the system were investigated over 5-50 °C. Thermal behavior of the system was investigated by differential scanning calorimetry too. Erosion rate of the gel in the presence and absence of SLN was measured by gravimetric method. Integrity of SLNs in the system was investigated by scanning electron microscopy (SEM) and particle size analysis. SLN showed particle size and zeta potential of 130 ± 1.39 nm and - 44 ± 2.1 mV respectively. Particle size analysis and SEM studies after gel erosion revealed presence of intact SLN in the hydrogel. SLN reduced erosion rate of Poloxamer gel and increased its sol-gel transition temperature from 26 to 29 °C. However, gelling kinetic did not change significantly after addition of SLN. Damping factor <1 indicated stability of the SLN-containing system. Present results indicate potential of sol-gel systems for controlled nanoparticle delivery and show that SLN affects properties of the system.

摘要

各种纳米颗粒已被作为新型药物递送系统进行研究,包括固体脂质纳米颗粒(SLNs)。由于纳米颗粒会从体循环中迅速清除,在大多数情况下它们无法提供持续作用。人们采用了不同策略来克服这一问题。在这个方向上,本研究引入了可蚀性原位形成凝胶系统作为延长SLNs释放的潜在载体。通过将含有硬脂酸、表面活性剂和助表面活性剂的水包油微乳液固化来制备SLNs。然后将纳米颗粒在4℃下分散于热敏性泊洛沙姆407水溶液(溶胶)中,并在5 - 50℃范围内研究它们对系统凝胶形成能力、溶胶 - 凝胶转变和流变行为的影响。还通过差示扫描量热法研究了该系统的热行为。通过重量法测量在有和没有SLN存在时凝胶的侵蚀速率。通过扫描电子显微镜(SEM)和粒度分析研究系统中SLNs的完整性。SLN的粒径和zeta电位分别为130±1.39 nm和 - 44±2.1 mV。凝胶侵蚀后的粒度分析和SEM研究表明水凝胶中存在完整的SLN。SLN降低了泊洛沙姆凝胶的侵蚀速率,并将其溶胶 - 凝胶转变温度从26℃提高到29℃。然而,添加SLN后凝胶动力学没有显著变化。阻尼因子<1表明含SLN系统的稳定性。目前的结果表明溶胶 - 凝胶系统在控制纳米颗粒递送方面具有潜力,并表明SLN会影响该系统的性质。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/07dc/4403051/8507d0726f97/ijpr-14-347-g001.jpg

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