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AuthorImran, Muhammad
AuthorShah, Muhammad Raza
AuthorUllah, Farhat
AuthorUllah, Shafi
AuthorElhissi, Abdelbary M. A.
AuthorNawaz, Waqas
AuthorAhmad, Farid
AuthorSadiq, Abdul
AuthorAli, Imdad
Available date2021-09-01T10:03:32Z
Publication Date2016
Publication NameInternational Journal of Pharmaceutics
ResourceScopus
URIhttp://dx.doi.org/10.1016/j.ijpharm.2016.03.042
URIhttp://hdl.handle.net/10576/22496
AbstractThis study aimed to evaluate the potential of a novel glycoside non-ionic surfactant synthesized and characterized in our laboratory for increased oral bioavailability of Cefixime. The surfactant was synthesized by simple etherification of bergenin with bromoundecane and characterized by 1H NMR and mass spectroscopy (MS). Biocompatibility of the surfactant (BRM-BG) was assessed by in-vitro cytotoxicity against NIH/3T3 cells and human blood hemolysis. In-vivo acute toxicity was evaluated in mices. Cefixime loaded BRM-BG niosomes were investigated for drug entrapment efficiency using HPLC and surface morphology and vesicle size by atomic force microscopy (AFM) and dynamic light scattering (DLS). The in-vivo oral bioavailability and pharmacokinetics studies were carried out using rabbits. Cefixime loaded BRM-BG vesicles were spherical in the size range of 178.66 ± 8.17 nm with a polydipersity index (PDI) of 0.20 ± 0.01, offering an entrapment efficiency as high as 78.4 ± 0.83%. When the surfactant was applied on NIH 3T3 tissue culture, as high as 90.77 ± 3.15% and 86.86 ± 3.02%, cell viability at 1000 μg/mL concentration after 24 and 48 h respectively were observed. The surfactant also caused 5.49 ± 1.62% haemolysis and was found to be safe at a dose up to 2000 mg/kg. In-vivo drug plasma concentration (Cmax) was found to be 9.69 ± 1.22 μg/mL, much higher than that resulting from the intake of commercial suspension and capsules. BRM-BG demonstrated to be safe and effective as carrier of Cefixime following oral dosing in rabbits. The BRM-BG surfactant delivery nano-system is relatively safe and in animal models it is an appropriate carrier for Cefixime, offering enhanced bioavailability compared to commercially available formulations of the drug.
SponsorAuthors are thankful to Higher Education Commission (HEC) , Pakistan, for financial support provided for PhD scholarship of Mr. Muhammad Imran, under indigenous PhD scholarships program (PIN NO: 112-23671-2BM1-136). Authors are also thankful to Mr. Fahad Siddiqui, Manager Department of Bioanalysis, Center for Bioequivalence Studies and Clinical Research (CBSCR), International Center for Chemical and Biological Sciences (ICCBS) University of Karachi, Pakistan, for his help in-vivo studies of this research
Languageen
PublisherElsevier B.V.
Subjectbergenin
bromoundecane
cefixime
glycoside
nanocarrier
niosome
surfactant
unclassified drug
antiinfective agent
benzopyran derivative
cefixime
drug carrier
glycoside
liposome
surfactant
acute toxicity
animal cell
animal experiment
area under the curve
Article
atomic force microscopy
cell viability
controlled study
drug blood level
drug clearance
drug delivery system
drug formulation
embryo
etherification
experimental rabbit
hemolysis
high performance liquid chromatography
in vivo study
male
mass spectrometry
mouse
nonhuman
photon correlation spectroscopy
priority journal
proton nuclear magnetic resonance
suspension
tissue culture
3T3 cell line
animal
bioavailability
chemistry
comparative study
female
human
medicinal chemistry
oral drug administration
particle size
procedures
rabbit
Administration, Oral
Animals
Anti-Bacterial Agents
Benzopyrans
Biological Availability
Cefixime
Chemistry, Pharmaceutical
Drug Carriers
Dynamic Light Scattering
Female
Glycosides
Humans
Liposomes
Male
Mice
Microscopy, Atomic Force
NIH 3T3 Cells
Particle Size
Rabbits
Surface-Active Agents
TitleGlycoside-based niosomal nanocarrier for enhanced in-vivo performance of Cefixime
TypeArticle
Pagination122-132
Issue Number2-Jan
Volume Number505
dc.accessType Abstract Only


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