Intranasal Delivery of Sulpiride Nanostructured Lipid Carrier to Central Nervous System; In Vitro Characterization and In Vivo Study.

IF 2.6 4区医学 Q2 PHARMACOLOGY & PHARMACY

Pharmaceutical Development and Technology Pub Date : 2024-09-12 DOI:10.1080/10837450.2024.2404034

Hesham M Tawfeek,Aml I Mekkawy,Ahmed A H Abdelatif,Basmah N Aldosari,Waleed A Mohammed-Saeid,Marwa G Elnaggar

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引用次数: 0

Abstract

The low and erratic oral absorption of sulpiride (SUL) a dopaminergic receptor antagonist, and its P-glycoprotein efflux in the gastrointestinal tract restricted its oral route for central nervous system disorders. An intranasal formulation was formulated based on nanostructured lipid carrier to tackle these obstacles and deliver SUL directly to the brain. Sulipride-loaded nanostructured lipid carrier (SUL-NLC) was prepared using compritol®888 ATO and different types of liquid lipids and emulsifiers. SUL-NLCs were characterized for their particle size, charge, and encapsulation efficiency. Morphology and compatibility with other NLC excipients were also studied. Moreover, SUL in vitro release, nanodispersion stability, in vivo performance and SUL pharmacokinetics were investigated. Results delineates that SUL-NLC have a particle size ranging from 366.2 ± 62.1 to 640.4 ± 50.2 nm and encapsulation efficiency of 75.5 ± 1.5%. SUL showed a sustained release pattern over 24 h and maintained its physical stability for three months. Intranasal SUL-NLC showed a significantly (p < 0.01) higher SUL brain concentration than that found in plasma after oral administration of commercial SUL product with 4.47-fold increase in the relative bioavailability. SUL-NLCs as a nose to brain approach is a promising formulation for enhancing the SUL bioavailability and efficient management of neurological disorders.

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将舒必利纳米结构脂质载体鼻内递送至中枢神经系统；体外表征和体内研究

舒必利（SUL）是一种多巴胺能受体拮抗剂，其口服吸收率低且不稳定，在胃肠道的P-糖蛋白外流限制了其口服治疗中枢神经系统疾病的途径。为了解决这些障碍，我们以纳米结构脂质载体为基础配制了一种鼻内制剂，可将 SUL 直接输送到大脑。使用 compritol®888 ATO 和不同类型的液态脂质和乳化剂制备了舒利必利负载型纳米结构脂质载体（SUL-NLC）。对 SUL-NLC 的粒度、电荷和封装效率进行了表征。同时还研究了其形态以及与其他 NLC 辅料的相容性。此外，还研究了 SUL 的体外释放、纳米分散稳定性、体内性能和 SUL 的药代动力学。结果表明，SUL-NLC 的粒径范围为 366.2 ± 62.1 至 640.4 ± 50.2 nm，封装效率为 75.5 ± 1.5%。SUL 在 24 小时内呈现持续释放模式，并在三个月内保持物理稳定性。与口服商用 SUL 产品相比，鼻内 SUL-NLC 的脑内 SUL 浓度明显更高（p < 0.01），相对生物利用度增加了 4.47 倍。SUL-NLC作为一种 "鼻入脑 "的方法，是提高SUL生物利用度和有效治疗神经系统疾病的一种前景广阔的制剂。

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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.