Preparation and Optimization of Liposome Containing Thermosensitive In Situ Nasal Hydrogel System for Brain Delivery of Sumatriptan Succinate

鼻腔给药 泊洛沙姆 脂质体 药物输送 药代动力学 药理学 泊洛沙姆407 体内 透皮 材料科学 化学 鼻粘膜 色谱法 最大值 生物医学工程 医学 纳米技术 聚合物 有机化学 生物技术 解剖 生物 共聚物
作者
Dyandevi Mathure,Ashish Dilip Sutar,Hemantkumar Ranpise,Atmaram Pawar,Rajendra Awasthi
出处
期刊:Assay and Drug Development Technologies [Mary Ann Liebert]
卷期号:21 (1): 3-16 被引量:10
标识
DOI:10.1089/adt.2022.088
摘要

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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