含热敏鼻腔水凝胶脂质体脑给药系统的制备与优化。

IF 1.6 4区 医学 Q4 BIOCHEMICAL RESEARCH METHODS
Dyandevi Mathure, Ashish Dilip Sutar, Hemantkumar Ranpise, Atmaram Pawar, Rajendra Awasthi
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引用次数: 3

摘要

通过鼻内途径的宽表面积和避免第一次代谢,药物吸收得到改善。对于偏头痛等中枢神经系统疾病的治疗,鼻内给药可将药物输送到大脑。该研究的目的是开发一种原位鼻腔水凝胶,该水凝胶含有装载琥珀酸舒马曲坦(SS)的脂质体。采用薄膜水合法制备脂质体,并采用32因子设计对其进行优化。优化后的脂质体呈球形,粒径为171.31 nm,包封率为83.54%,8 h释药率为86.11%。为了实现原位凝胶形成,将装载ss的脂质体加入到poloxomer -407、poloxomer -188和海藻酸钠的液体凝胶体系中。测试了最终产品的粘接强度、粘度、药物含量、胶凝温度和胶凝时间。经鼻给药后,体内药代动力学研究显示,药物在脑内的治疗浓度显著,Cmax值为167±78 ng/mL,曲线下面积为502±63 ng/min·mL。对于装载ss的脂质体热敏鼻水凝胶,药物靶向指数(2.61)和药物经鼻至脑直接转运(57.01%)的鼻至脑靶向参数值显著升高,证实药物经鼻途径靶向至脑。含有热敏原位水凝胶的脂质体显示了鼻内给药SS的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation and Optimization of Liposome Containing Thermosensitive In Situ Nasal Hydrogel System for Brain Delivery of Sumatriptan Succinate.

Drug absorption is improved by the intranasal route's wide surface area and avoidance of first-pass metabolism. For the treatment of central nervous system diseases such as migraine, intranasal administration delivers the medication to the brain. The study's purpose was to develop an in situ nasal hydrogel that contained liposomes that were loaded with sumatriptan succinate (SS). A thin-film hydration approach was used to create liposomes, and a 32 factorial design was used to optimize them. The optimized liposomes had a spherical shape, a 171.31 nm particle size, a high drug encapsulation efficiency of 83.54%, and an 8-h drug release of 86.11%. To achieve in situ gel formation, SS-loaded liposomes were added to the liquid gelling system of poloxamer-407, poloxamer-188, and sodium alginate. The final product was tested for mucoadhesive strength, viscosity, drug content, gelation temperature, and gelation time. Following intranasal delivery, in vivo pharmacokinetic investigations showed a significant therapeutic concentration of the medication in the brain with a Cmax value of 167 ± 78 ng/mL and an area under the curve value of 502 ± 63 ng/min·mL. For SS-loaded liposomal thermosensitive nasal hydrogel, significantly higher values of the nose-to-brain targeting parameters, that is, drug targeting index (2.61) and nose-to-brain drug direct transport (57.01%), confirmed drug targeting to the brain through the nasal route. Liposomes containing thermosensitive in situ hydrogel demonstrated potential for intranasal administration of SS.

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来源期刊
Assay and drug development technologies
Assay and drug development technologies 医学-生化研究方法
CiteScore
3.60
自引率
0.00%
发文量
33
审稿时长
>12 weeks
期刊介绍: ASSAY and Drug Development Technologies provides access to novel techniques and robust tools that enable critical advances in early-stage screening. This research published in the Journal leads to important therapeutics and platforms for drug discovery and development. This reputable peer-reviewed journal features original papers application-oriented technology reviews, topical issues on novel and burgeoning areas of research, and reports in methodology and technology application. ASSAY and Drug Development Technologies coverage includes: -Assay design, target development, and high-throughput technologies- Hit to Lead optimization and medicinal chemistry through preclinical candidate selection- Lab automation, sample management, bioinformatics, data mining, virtual screening, and data analysis- Approaches to assays configured for gene families, inherited, and infectious diseases- Assays and strategies for adapting model organisms to drug discovery- The use of stem cells as models of disease- Translation of phenotypic outputs to target identification- Exploration and mechanistic studies of the technical basis for assay and screening artifacts
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