用于脑部靶向治疗的氨磺必利鼻腔内凝胶的配制、优化和评估。

IF 3 Q2 PHARMACOLOGY & PHARMACY

Therapeutic delivery Pub Date : 2023-10-01 Epub Date: 2023-12-05 DOI:10.4155/tde-2023-0059

Vinayak S Patil, Kishori P Sutar, Rachana D Pockle, Siddarth Usulkar, Vishwanath A Jadhav

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引用次数: 0

摘要

目的：开发含有阿米舒必利（AMS）的稳定非离子表面活性剂囊泡，以改善通过鼻脑机制的脑摄取。方法采用改良的乙醇注射技术开发了 Niosomes，使用 32 因子设计进行了优化，并对囊泡大小 (VS)、封装效率 (EE)、Zeta 电位 (ZP) 和累积药物释放率 (%CDR) 进行了评估。结果优化后的 niosomes（Span-60：胆固醇比率为 0:1）显示出 191.4 nm 的 VS、84.25% 的 EE、-38.2 ZP 和 81.31% 的 CDR。使用这些 niosomes 的原位凝胶显示出 78% 的 CDR。TEM 分析表明，该药物呈球形。对大鼠进行的药代动力学和脑组织分布研究显示，血浆和脑浓度均有所提高，表明成功实现了脑靶向。结论：这种策略改善了 AMS 经鼻腔的渗透，提高了治疗精神分裂症的生物利用度。

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Formulation, optimization and evaluation of amisulpride-loaded niosomal intranasal gel for brain targeting.

Aim: To develop stable non-ionic surfactant vesicles containing amisulpride (AMS) to improve brain uptake via nose to brain mechanism. Methods: Niosomes were developed using a modified ethanol injection technique, optimized using 3² factorial design and evaluated for the vesicle size (VS), percent encapsulation efficiency (EE), zeta potential (ZP) and % cumulative drug release (%CDR). Results: Optimized niosomes (Span-60: cholesterol ratio 0:1) showed 191.4 nm VS, 84.25% EE, -38.2 ZP and 81.31% CDR. In situ gel with these niosomes displayed 78% CDR. TEM analysis revealed spherical niosomes. Pharmacokinetic and brain tissue distribution studies in rats showed enhanced plasma and brain concentrations, indicating successful brain targeting. Conclusion: This strategy demonstrates improved AMS permeation via the nasal cavity, enhancing bioavailability for treating schizophrenia.

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来源期刊

Therapeutic delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.50

自引率

0.00%

发文量

期刊介绍： Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.