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Preparation and Optimization of Liposome Containing Thermosensitive In Situ Nasal Hydrogel System for Brain Delivery of Sumatriptan Succinate
被引:10
作者:
Mathure, Dyandevi
[1
]
Sutar, Ashish Dilip
[2
]
Ranpise, Hemantkumar
[3
]
Pawar, Atmaram
[1
]
Awasthi, Rajendra
[4
]
机构:
[1] Bharati Vidyapeeth Deemed Univ, Bharati Vidyappeths Poona Coll Pharm, Pune 411038, India
[2] Savitribai Phule Pune Univ, Smt Kashibai Navale Coll Pharm, Dept Pharmaceut, Pune, India
[3] RMPs Bhalchandra Coll Pharm, Pune, India
[4] Univ Petr & Energy Studies UPES, Sch Hlth Sci & Technol, Dept Pharmaceut Sci, PO Bidholi,Via Prem Nagar, Dehra Dun 248007, India
关键词:
brain delivery;
drug delivery;
in situ nasal gel;
liposome;
thermosensitive hydrogel;
BUSPIRONE HYDROCHLORIDE;
CHITOSAN NANOPARTICLES;
INTRANASAL DELIVERY;
VITRO;
GEL;
DESIGN;
NANOEMULSION;
DISSOLUTION;
FORMULATION;
D O I:
10.1089/adt.2022.088
中图分类号:
Q5 [生物化学];
学科分类号:
071010 ;
081704 ;
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 3(2) 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 C-max 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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页码:3 / 16
页数:14
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