一种新型拉莫三嗪纳米乳凝胶的设计、体外和体内评价。

IF 3 4区医学 Q2 CHEMISTRY, APPLIED

Journal of microencapsulation Pub Date : 2025-06-01 Epub Date: 2025-04-02 DOI:10.1080/02652048.2025.2482048

DaІia E Gaber, Alanood S Almurshedi, Basmah N Aldosari, Samiah Alhabardi, Randa M Zaki, Mahasen A Radwan, Xien Chen

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引用次数: 0

摘要

目的：通过将低溶解度抗癫痫药物拉莫三嗪（LMG）制成鼻用纳米乳（NE），提高其生物利用度和治疗效果。方法：采用32因子设计，采用自然乳化法将LMG- ne掺入鼻用纳米乳中。对LMG-NEs进行了载药量（DL）、包封效率（EE%）、粒径、显微镜检查、流变学特征、磷脂酰胆碱脂质体摄取、体外释放、抗惊痫活性和体内药动学表征。结果：最佳配方的DL为79.03±0.5 (w/w)， EE%为80.2±3.0%，平均粒径为182.78±22.76 nm， zeta电位为0.60±0.04 mV。LMG释放迅速，2 h内释放率为91.87%±4.54%。曲线下面积（AUC0-24）为标准配方的1.84倍。结论：LMG-NE是一种很有前景的癫痫治疗替代方案，可能减少外周副作用并改善治疗效果。

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Design, in vitro, and in vivo evaluation of a new nanoemulsion gel of lamotrigine for application via nasal route.

Aims: This study aimed to enhance the bioavailability and therapeutic efficacy of lamotrigine (LMG), an antiepileptic drug with low solubility, by formulating it into a nasal nanoemulsion (NE) for effective epilepsy control.

Methods: LMG was incorporated into a nasal nanoemulsion (LMG-NE) using a 3² factorial design via spontaneous emulsification method. LMG-NEs were characterised for drug loading (DL), entrapment efficiency (EE%), particle size, microscopic examination, rheological profile, phosphatidylcholine liposome uptake, in vitro release, anticonvulsant activity, and in vivo pharmacokinetics.

Results: The optimal formulation exhibited a DL of 79.03 ± 0.5 (w/w), an EE% of 80.2 ± 3.0%, a mean diameter of 182.78 ± 22.76 nm, and a zeta potential of 0.60 ± 0.04 mV. LMG was rapidly released, with 91.87% ± 4.54% of drug was released within 2 hours. The area under the curve (AUC_0-24) showed a 1.84-fold increase compared to standard formulations.

Conclusion: LMG-NE presents a promising alternative for epilepsy treatment, potentially reducing peripheral side effects and improving therapeutic outcomes.

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来源期刊

Journal of microencapsulation 工程技术-工程：化工

CiteScore

6.30

自引率

2.60%

发文量

审稿时长

3 months

期刊介绍： The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.