A novel emulsifier, Labrasol, enhances gastrointestinal absorption of gentamicin

Hu, Zhaopeng; Tawa, Riichi; Konishi, Tenji; Shibata, Nobuhito; Takada, Kanji

doi:10.1016/s0024-3205(01)01375-3

Cited by 103 publications

(66 citation statements)

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“…2 Currently, water/oil (w/o) types of microemulsions, 3 or oil/water (o/w) microemulsions separated by a two-phase region, 4,5 self-microemulsifying drug delivery system (SMEDDS), [6][7][8] and U-type phase diagrams capable of forming microemulsions at any given water dilution level (U-type preconcentrate) have been utilized to solubilize and increase the bioavailability of drugs and nutraceuticals. [9][10][11][12][13] W/o or o/w microemulsions are excellent and effective carriers that increase the solubility and improve the bioavailability of poorly water-soluble drugs.…”

Section: Introductionmentioning

confidence: 99%

In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate

Lin

Wu²,

Chen³

et al. 2011

IJN

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U of 0.9, N and Q of 0.73, T and V of 0.58, and O and R of 0.46) and water contents (1: 9.5%, 2: 5.0%, 3: 0.0%, G-V: 4.5%). Their dissolutions were conducted at different rotation speeds. Two optimal SMEDDSs containing Tween 80(B2) or a higher oil/S mix ratio(Q) and B2(solution) were selected for pharmacokinetic study. Results: FFB particles formed within the nanosize range from Group I gradually increased with time but decreased with increasing stirring rates. However, the mean size of FFB formed by B series was as low as 200 nm, which was smaller than that of A series at three stirring rates. The release rate from both groups obviously increased with increasing stirring rate. However, incomplete release was observed for S and N in Tween 20 series, whereas a faster release rate and complete release were observed for Tween 80 series with an insignificant difference among them. Results of pharmacokinetic study demonstrated that the highest-ranked area under the curve and C max values were for Q(SMEDDS) and B2(solution), respectively. The relative bioavailability of Q(SMEDDS) with respect to Tricor ® was enhanced by about 1.14-1.22-fold. Conclusion: SMEDDS, consisting of Myritol 318 and TPGS combined with Tween 80 at 4:1, was able to enhance the oral bioavailability of FFB.

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Section: Introductionmentioning

confidence: 99%

In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate

Lin

Wu²,

Chen³

et al. 2011

IJN

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“…The well known poor gastrointestinal membrane permeability and the consequent low bioavailability (class III of the biopharmaceutical classification system) are likely connected to the high polarity of this cationic compound. Various approaches have been investigated in order to increase GM oral bioavailability, including the co-administration of absorption-enhancing agents such as surfactants (Hu et al, 2001;Ito et al, 2005), bile salts and glucosteroids (Axelrod et al, 1998), and liposaccharides (Ross et al, 2004). Although good gastrointestinal absorptionenhancing effects were demonstrated, cytotoxicity and damage to the mucosa have been reported (Swenson et al, 1994;Aungst, 2000;Ross et al, 2004).…”

Section: Introductionmentioning

confidence: 99%

Microparticulate polyelectrolyte complexes for gentamicin transport across intestinal epithelia

et al. 2010

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“…Claudins and E-cadherin have been considered as key integral protein regulators responsible for the maintenance of electrical resistance and paracellular integrity (Oliveira and Morgado-Diaz, 2007). Previous findings indicate that certain solvents, like the surfactant labrasol, can disrupt tight junction integrity, and thus enhance the penetration of gentamicin across membranes (Hu et al, 2001). This phenomenon was not observed when gentamicin was supplemented with another solvent, 1% DMSO.…”

Section: Resultsmentioning

confidence: 99%

“…At higher concentrations, DMSO is known to disrupt lipid structures in epithelia (Gordeliy et al, 1998;Simons, 2008) and thus it can facilitate the penetration of certain substances. It was previously described that labrasol, a nonionic surfactant, enhanced the oral bioavailability of gentamicin (Hu et al, 2001) probably via tight junction opening mechanisms. Fig.…”

Section: Abstract: Gentamicin Dmso Ipec-j2 Permeationmentioning

confidence: 99%

Gentamicin sulphate permeation through porcine intestinal epithelial cell monolayer

Gyetvai

Jerzsele

Pászti-Gere

et al. 2015

Acta Veterinaria Hungarica

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Gentamicin is an aminoglycoside antibiotic widely used in combination with dimethyl sulphoxide (DMSO) in topical drug formulations. It is not known, however, whether DMSO can enhance the permeation of gentamicin through biological membranes, leading to oto-and nephrotoxic side effects. A simple and reliable high-performance liquid chromatographic (HPLC) method was applied for the quantitative determination of gentamicin collected from the apical and basolateral compartments of the porcine intestinal epithelial cell line IPEC-J2 cell monolayer using fluorometric derivatisation of the analyte with fluorenylmethyloxycarbonyl chloride (FMOC) prior to chromatographic run in the presence and absence of 1% DMSO. The lack of change in transepithelial electrical resistance (TER) demonstrated that gentamicin and 1% DMSO did not affect IPEC-J2 cell monolayer integrity via the disruption of cell membranes. Chromatographic data also ascertained that gentamicin penetration across the cell monolayer even in the presence of 1% DMSO was negligible at 6 h after the beginning of apical gentamicin administration. This study further indicates that the addition of this organic solvent does not increase the incidence of toxic effects related to gentamicin permeation.

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A novel emulsifier, Labrasol, enhances gastrointestinal absorption of gentamicin

Cited by 103 publications

References 0 publications

In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate

In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate

Microparticulate polyelectrolyte complexes for gentamicin transport across intestinal epithelia

Gentamicin sulphate permeation through porcine intestinal epithelial cell monolayer

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