Thymoquinone loaded lipid nanocapsule dispersion: two methods of preparation, characterization and in vitro evaluations for oral administration.

IF 2.6 4区医学 Q2 PHARMACOLOGY & PHARMACY

Pharmaceutical Development and Technology Pub Date : 2025-01-01 Epub Date: 2025-01-03 DOI:10.1080/10837450.2024.2448616

Mouna Selmi, Amine Trabelsi, Nolwenn Lautram, David Dallerac, Guillaume Lefebvre, Leila Chekir Ghedira, Emilie Roger

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引用次数: 0

Abstract

This work explores two methods to encapsulate Thymoquinone (TQ) into lipid nanocapsules (LNCs) for oral administration. TQ was added during the phase inversion temperature method (TQ-LNCs-1) or to unload LNCs dispersion (TQ-LNCs-2). LNCs were evaluated for mean diameter, polydispersity index (PDI), ζ-potential, drug loading (DL), drop tensiometer, storage stability, in vitro stability in simulated gastrointestinal fluids (SGIF), and intestinal permeability across Caco-2 cells. TQ-LNCs-1 and TQ-LNCs-2 produced NPs (58.3 ± 3.7 nm and 61.5 ± 3.5 nm, respectively), with a DL of 8.7 ± 0.2 and 7.7 ± 0.6 mg/mL of suspension, respectively. For both, less than 14% of TQ was released in SGIF, and a minor increase in TQ intestinal permeability with LNCs compared to free TQ was observed. TQ-LNCs represented a promising formulation for oral delivery of TQ. Encapsulation of TQ by adding it at LNCs dispersion can be extended for further drugs.

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百里醌载脂质纳米胶囊分散体的制备、表征及体外口服评价。

本研究探讨了两种将百里醌（TQ）包封到脂质纳米胶囊（LNCs）中用于口服的方法。在相变温度法（TQ-LNCs-1）或卸载LNCs分散（TQ-LNCs-2）时添加TQ。评估LNCs的平均直径、多分散性指数（PDI）、ζ电位、载药量（DL）、滴张力计、储存稳定性、在模拟胃肠液中的体外稳定性（SGIF）和Caco-2细胞的肠通透性。TQ-LNCs-1和TQ-LNCs-2产生的NPs分别为58.3±3.7 nm和61.5±3.5 nm， DL分别为8.7±0.2和7.7±0.6 mg/mL。在这两种情况下，SGIF中释放的TQ都不到14%，并且与游离TQ相比，LNCs中TQ肠道通透性略有增加。TQ- lncs是一种很有前途的口服TQ制剂。通过在LNCs分散体中加入TQ包封可以扩展到其他药物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Pharmaceutical Development and Technology 医学-药学

CiteScore

5.90

自引率

2.90%

发文量

审稿时长

1 months

期刊介绍： Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology. Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as: -Preformulation and pharmaceutical formulation studies -Pharmaceutical materials selection and characterization -Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation -QbD in the form a risk assessment and DoE driven approaches -Design of dosage forms and drug delivery systems -Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies -Drug delivery systems research and quality improvement -Pharmaceutical regulatory affairs This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.