Mathure Dyandevi, Sutar Ashish Dilip, Ranpise Hemantkumar, Pawar Atmaram, Awasthi Rajendra
Bharati Vidyappeth's Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Pune, India.
Department of Pharmaceutics, Smt. Kashibai Navale College of Pharmacy, Savitribai Phule Pune University, Pune, India.
Assay Drug Dev Technol. 2023 Jan;21(1):3-16. doi: 10.1089/adt.2022.088. Epub 2022 Dec 22.
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 nasal hydrogel that contained liposomes that were loaded with sumatriptan succinate (SS). A thin-film hydration approach was used to create liposomes, and a 3 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 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, pharmacokinetic investigations showed a significant therapeutic concentration of the medication in the brain with a C 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 hydrogel demonstrated potential for intranasal administration of SS.
鼻内给药途径具有较大的表面积且可避免首过代谢，从而改善药物吸收。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至脑部。本研究的目的是开发一种含有载有琥珀酸舒马曲坦（SS）脂质体的鼻用水凝胶。采用薄膜水化法制备脂质体，并使用三因素设计对其进行优化。优化后的脂质体呈球形，粒径为171.31 nm，药物包封率高达83.54%，8小时药物释放率为86.11%。为形成凝胶，将载有SS的脂质体添加到泊洛沙姆-407、泊洛沙姆-188和海藻酸钠的液体胶凝体系中。对最终产品进行了粘膜粘附强度、粘度、药物含量、胶凝温度和胶凝时间的测试。鼻内给药后，药代动力学研究表明，药物在脑中具有显著的治疗浓度，C值为167±78 ng/mL，曲线下面积值为502±63 ng/min·mL。对于载有SS的脂质体热敏鼻用水凝胶，鼻脑靶向参数的值显著更高，即药物靶向指数（2.61）和鼻脑药物直接转运率（57.01%），证实了药物通过鼻腔途径靶向脑部。含有热敏水凝胶的脂质体显示出鼻内给药SS的潜力。
