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Ciprofloxacin surf-plexes in sub-micron emulsions: a novel approach to improve payload efficiency and antimicrobial efficacy.

Abstract：

:The aim of this study was to investigate antimicrobial efficacy and pharmacokinetic profile of ciprofloxacin (CFn) loaded oil-in-water (o/w) submicron emulsion (SE-CFn). This study emphasized on development of hydrophobic ion-pair complexes of CFn with sodium deoxycholate (SDC) [CFn-SDC], which was incorporated in the core of SE (SE-CFn-SDC). SE-CFn-SDC was characterized for globulet size (278±12 nm), zeta potential (-25.3±1 mV), viscosity (2.6±0.3 cP), transmission electron microscopy (TEM), drug entrapment and for in vitro release profile. The entrapment efficiency (EE) was significantly improved (≥80%; p≤0.05) on ion-pairing while it was merely 27.2±3.1% for free CFn. The cytotoxicity studies of formulations on J774 macrophage cells showed that more than 90±3% of cells were viable, even at high concentration (100 μg/ml). SE-CFn-SDC was further modified with cationic inducer chitosan (SE-CH-CFn-SDC), which showed almost twofold and fourfold enhancement in antimicrobial efficacy as compared to SE-CFn-SDC and SE-CFn, respectively when tested in vitro against E. coli, S. aureus, and P. aeruginosa. When tested in male Balb/c mice, the AUC(0-24h) of SE-CH-CFn-SDC (23.27±2.8 h μg/ml) was found to be 1.7-fold and 5-fold higher as compared to SE-CFn-SDC (13.17±0.88 h μg/ml) and CFn solution (4.70±0.77 h μg/ml), respectively. The study demonstrates that surfactant based ionic complex formation incorporated in surface modified submicron emulsion is a promising approach to improve payload efficiency of poorly water soluble drugs with improved antimicrobial efficacy and pharmacokinetic profile.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Jain V,Singodia D,Gupta GK,Garg D,Keshava GB,Shukla R,Shukla PK,Mishra PR

doi

10.1016/j.ijpharm.2011.02.020

subject

Has Abstract

pub_date

2011-05-16 00:00:00

pages

237-44

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(11)00155-4

journal_volume

409

pub_type

杂志文章

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