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A novel flunarizine hydrochloride-loaded organogel for intraocular drug delivery in situ: Design, physicochemical characteristics and inspection.

Abstract：

:We developed a safe and efficacious drug delivery system for treatment of brain diseases. A novel in-situ gel system was prepared using soybean oil, stearic acid and N-methyl-2-pyrrolidinone (NMP) (10:1:3, v/w/v). This system had low viscosity as a sol in vitro and turned into a solid or semi-solid gel in situ after administration. The poorly water-soluble drug flunarizine hydrochloride (FNZ) was incorporated into this "organogel" system. Organogel-FNZ was characterized by light microscopy, differential scanning calorimetry (DSC) and rheology. Drug release in vitro was investigated. The initial "burst" effect did not occur in organogel-FNZ, which is different from other gels formed in situ. Pharmacokinetic studies were undertaken in rats using gel administration (14 mg kg-1), intravenous administration (5 mg kg-1) and administration using drops (14 mg kg-1). Organogel-FNZ could reduce the clearance rate and prolong the duration of action, in the plasma and brain tissues of rats. The peak serum concentration, area under the curve and absolute bioavailability of the organogel-FNZ group were higher than those of the intraocular- drops group. Organogel-FNZ is a promising drug-delivery system for treatment of brain diseases by intraocular administration.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Dai M,Bai L,Zhang H,Ma Q,Luo R,Lei F,Fei Q,He N

doi

10.1016/j.ijpharm.2020.119027

subject

Has Abstract

pub_date

2020-02-25 00:00:00

pages

119027

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(20)30009-0

journal_volume

576

pub_type

杂志文章

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