干法吸附固体脂质纳米颗粒的配方开发、体外和体内评估：克服奥氮平缺点的一种方法

European Pharmaceutical Journal Pub Date : 2024-04-20 DOI:10.2478/afpuc-2024-0004

R. Hirlekar, Alfiha Momin, S. Bhairy

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引用次数: 0

摘要

本研究旨在制备稳定的奥氮平（OLZ）干吸附纳米颗粒（DANs），以实现固体脂质纳米颗粒（SLNs）的持续释放。在优化配方和工艺变量后，以 Precirol ATO 5 (PRE) 作为固体脂质，以 Kolliphor ELP (KELP) 和 Tween 80 (T80) 组合作为表面活性剂，通过热熔乳化和超声处理制备了 OLZ SLNs。对 SLN 系统进行了粒度、ZETA 电位、包埋效率 (EE)、体外药物释放和使用鸡肠段（空肠）进行体外肠道渗透性研究等方面的评估。此外，还采用造粒-蒸发干燥法将这些 SLNs 吸附到 Neusilin US2（NUS2）和 Avicel CL 611（ACL）载体上，将其转化为稳定的 DANs。对 DANs 的再分散特性、体外药物释放、热行为、结晶度和形态进行了表征。 SLN 和 DAN 的粒径分别为 238.0 nm [0.274 聚分散指数（PdI）] 和 302.4 [0.494 PdI]。SLN 和 DAN 的 zeta 电位分别为 -29.3 mV 和 -26.3 mV。SLN 的 EE 值为 67%，在各种介质中都能持续释放药物。在体内外渗透模型中观察到，与 OLZ 悬浮液相比，SLNs 的渗透性最高，这表明 SLNs 有可能绕过肝脏代谢。表面形态证实了 SLNs 在载体上的吸附作用。DAN 具有良好的流动性和持续释药性，与 SLN 相似。X 射线衍射（XRD）图谱和内热峰证实了脂质基质中活性物质的完全封装。将 OLZ 包封在 SLNs 中并将其转化为 DAN 显示了一种持续释放和吸附技术，可用于提高 NLC 分散体的稳定性。这种 DAN 可用于各种剂型，如装入小袋、胶囊或压制成片剂。

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Formulation development, in-vitro and ex-vivo evaluation of dry adsorbed solid lipid nanoparticles: an approach of overcoming olanzapine drawbacks

The present study was aimed at preparing stable dry adsorbed nanoparticles (DANs) of olanzapine (OLZ) loaded solid lipid nanoparticles (SLNs) for sustained release. OLZ SLNs were prepared by hot melt emulsification and ultrasonication using Precirol ATO 5 (PRE) as a solid lipid, combination of Kolliphor ELP (KELP) and Tween 80 (T80) as surfactants, after optimising formulation and process variables. The SLN system was subjected to evaluation of particle size, zeta potential, entrapment efficiency (EE), in-vitro drug release and ex-vivo intestinal permeability studies using the chicken intestinal segments (jejunum). Further, these SLNs were converted into stable DANs by adsorbing onto a Neusilin US2 (NUS2) and Avicel CL 611 (ACL) carriers using the granulation-evaporative drying method. The DANs were characterised for redispersion properties, in-vitro drug release, thermal behaviour, crystallinity, and morphology. The SLN and DAN had a particle size of 238.0 nm [0.274 polydispersity index (PdI)] and 302.4 [0.494 PdI] respectively. The zeta potentials of SLN and DAN were found to be −29.3 mV and −26.3 mV, respectively. The SLN had 67% EE, and showed a sustained drug release in various media. The highest permeability of SLNs was observed in ex-vivo permeation model compared to the OLZ suspension, indicating that SLNs have the potential to bypass hepatic metabolism. The adsorption of SLNs onto carriers was confirmed by surface morphology. The DAN had good flow properties and sustained drug release similar to that of SLNs. The X-ray diffraction (XRD) patterns and endothermic peaks confirmed the complete encapsulation of actives in lipid matrices. The encapsulating of OLZ in SLNs and converting it into DAN showed a sustained release and adsorption technique that can be used for improving the stability of NLC dispersion. The DANs can be offered in dosage forms such as filling into sachets, capsules and compressed into tablets.

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European Pharmaceutical Journal Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)

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0.60

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0.00%

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期刊介绍： European Pharmaceutical Journal publishes only original articles not previously published and articles that are not being considered or have not been submitted for publication elsewhere. If parts of the results have been published as conference abstract or elsewhere, it should be stated in references. The ethical standards of the Helsinki-Tokio Declaration should be kept. This should be mentioned in the Methods of manuscript. Reviews are published only on request. Authors, whose submitted research work was performed with the support of a company, should indicate this in Conflict of Interest.