Exploring the potential to enhance drug distribution in the brain subregion via intranasal delivery of nanoemulsion in combination with borneol as a guider

IF 10.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Asian Journal of Pharmaceutical Sciences Pub Date : 2023-11-01 DOI:10.1016/j.ajps.2023.100778
Xin Shen, Zhixiang Cui, Yidan Wei, Yingnan Huo, Duo Yu, Xin Zhang, Shirui Mao
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引用次数: 1

Abstract

The number of people with Alzheimer's disease (AD) is increasing annually, with the nidus mainly concentrated in the cortex and hippocampus. Despite of numerous efforts, effective treatment of AD is still facing great challenges due to the blood brain barrier (BBB) and limited drug distribution in the AD nidus sites. Thus, in this study, using vinpocetine (VIN) as a model drug, the objective is to explore the feasibility of tackling the above bottleneck via intranasal drug delivery in combination with a brain guider, borneol (BOR), using nanoemulsion (NE) as the carrier. First of all, the NE were prepared and characterized. In vivo behavior of the NE after intranasal administration was investigated. Influence of BOR dose, BOR administration route on drug brain targeting behavior was evaluated, and the influence of BOR addition on drug brain subregion distribution was probed. It was demonstrated that all the NE had comparable size and similar retention behavior after intranasal delivery. Compared to intravenous injection, improved brain targeting effect was observed by intranasal route, and drug targeting index (DTI) of the VINNE group was 154.1%, with the nose-to-brain direct transport percentage (DTP) 35.1%. Especially, remarkably enhanced brain distribution was achieved after BOR addition in the NE, with the extent depending on BOR dose. VIN brain concentration was the highest in the VIN-1-BOR-NE group at BOR dose of 1 mg/kg, with the DTI reaching 596.1% and the DTP increased to 83.1%. BOR could exert better nose to brain delivery when administrated together with the drug via intranasal route. Notably, BOR can remarkably enhance drug distribution in both hippocampus and cortex, the nidus areas of AD. In conclusion, in combination with intranasal delivery and the intrinsic brain guiding effect of BOR, drug distribution not only in the brain but also in the cortex and hippocampus can be enhanced significantly, providing the perquisite for improved therapeutic efficacy of AD.

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探索纳米乳剂联合冰片作为导引剂经鼻给药增强药物在脑亚区分布的潜力
阿尔茨海默病(AD)患者数量逐年增加,病灶主要集中在皮层和海马。尽管进行了许多努力,但由于血脑屏障(BBB)和AD病灶部位药物分布有限,有效治疗AD仍面临巨大挑战。因此,本研究以长春西汀(vinpocetine, VIN)为模型药物,探讨以纳米乳(NE)为载体,联合脑导剂冰片(BOR)经鼻给药解决上述瓶颈的可行性。首先,对NE进行了制备和表征。研究了NE经鼻给药后的体内行为。评价BOR剂量、给药途径对药物脑靶向行为的影响,探讨添加BOR对药物脑亚区分布的影响。经鼻给药后,所有的NE具有相当的大小和相似的保留行为。与静脉注射相比,鼻内途径脑靶向效果明显改善,VINNE组药物靶向指数(DTI)为154.1%,鼻脑直接转运率(DTP)为35.1%。特别是在NE中添加BOR后,脑分布明显增强,其程度取决于BOR的剂量。在BOR剂量为1 mg/kg时,VIN-1-BOR- ne组脑内VIN浓度最高,DTI达到596.1%,DTP增加至83.1%。经鼻给药时,BOR能更好地发挥鼻至脑输送作用。值得注意的是,BOR可以显著增强阿尔茨海默病病灶区海马和皮层的药物分布。综上所述,结合鼻内给药和BOR固有的脑引导作用,不仅可以显著增强药物在大脑内的分布,还可以显著增强药物在皮层和海马区的分布,为提高AD的治疗效果提供了条件。
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阿拉丁 Borneol (BOR)
来源期刊
Asian Journal of Pharmaceutical Sciences
Asian Journal of Pharmaceutical Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
18.30
自引率
2.90%
发文量
11
审稿时长
14 days
期刊介绍: The Asian Journal of Pharmaceutical Sciences (AJPS) serves as the official journal of the Asian Federation for Pharmaceutical Sciences (AFPS). Recognized by the Science Citation Index Expanded (SCIE), AJPS offers a platform for the reporting of advancements, production methodologies, technologies, initiatives, and the practical application of scientific knowledge in the field of pharmaceutics. The journal covers a wide range of topics including but not limited to controlled drug release systems, drug targeting, physical pharmacy, pharmacodynamics, pharmacokinetics, pharmacogenomics, biopharmaceutics, drug and prodrug design, pharmaceutical analysis, drug stability, quality control, pharmaceutical engineering, and material sciences.
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