Diethyl ether fraction of Labrasol having a stronger absorption enhancing effect on gentamicin than Labrasol itself

Hu, Zhaopeng; Yv, Rama Prasad; Tawa, Riichi; Konishi, Tenji; Ishida, M.; Shibata, Nobuhito; Takada, Kanji

doi:10.1016/s0378-5173(01)00967-x

Cited by 17 publications

(8 citation statements)

References 25 publications

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“…Labrasol, originally developed for solubilization of hydrophobic drugs (HLB 14), is a non-ionic emulsifier, useful also in oral formulations for its high tolerance and low toxicity in animals; it also displays a strong absorption enhancing effect (11). Labrasol can be easily dissolved in water; because it displays only a low interfacial tension with water, the amount of co-surfactants can be kept low.…”

Section: Resultsmentioning

confidence: 99%

Control of Transdermal Permeation of Hydrocortisone Acetate from Hydrophilic and Lipophilic Formulations

et al. 2008

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Abstract. The purpose of this research was the preparation of four formulations containing hydrocortisone acetate (HCA) for topical application, including two aqueous systems (hydrophilic microemulsion and aqueous gel) and two systems with dominant hydrophobicity (hydrophobic microemulsion and ointment). The formulations were tested for the release and permeation of HCA across an animal membrane. The release of HCA was found comparable for the four systems. The two microemulsions promote permeation across an ex-vivo membrane, examined by means of a Franz cell. Hydrophobic microemulsion guarantees the highest solubility (2,370 μg/ml) and flux (133 μg/cm 2 .h) of the drug, since it contains almost 40% Transcutol, a permeation enhancer. Gel and ointment provide lower solubility and flux, being the values, related to the ointment, the lowest ones (562 μg/ml and 0.4 μg/ cm 2 .h). Experimental results allow the conclusion that gel and ointment can be suitable when it is desirable to minimize absorption of topically applied HCA as to keep the drug restricted to the diseased area and prevent side effects of the systemic presence of HCA.

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Section: Resultsmentioning

confidence: 99%

Control of Transdermal Permeation of Hydrocortisone Acetate from Hydrophilic and Lipophilic Formulations

et al. 2008

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“…dose, drug/liposaccharide ratio) and in the design of the liposaccharide excipient itself. The potential to modulate the physicochemical properties of the system by altering the length of the Laa alkyl chain and the nature of the sugar moiety 23-25 makes this a highly adaptable synthetic drug delivery system in comparison to methods utilizing natural or semisynthetic agents. ,,,, …”

Section: Resultsmentioning

confidence: 99%

“…Banerjee et al achieved the oral delivery of tobramycin in mice by using the vehicle CRL-1605, a nonionic block copolymer synthesized from ethylene oxide and propylene oxide . Most recently, Hu et al used a product obtained from coconut oil, Labrasol, which contains saturated polyglycolysed C6−C14 glycerides, as an agent to enhance gastrointestinal absorption of gentamicin in rats. , All of the excipients in these studies are surfactants.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Evaluation of a Liposaccharide Drug Delivery Agent: Application to the Gastrointestinal Absorption of Gentamicin

et al. 2004

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The design, synthesis, and evaluation of a liposaccharide (11) for use as an agent to enhance the gastrointestinal absorption of charged, hydrophilic drugs with poor membrane permeability is reported. 11 was designed to possess both surfactant and ion-pairing properties and was conveniently synthesized from d-glucuronic acid (2) and N-Boc-lipoamino acid (5) precursors in eight steps in good yield. Isothermal titration microcalorimetry was used to determine the critical micelle concentration of 11 (in PBS) to be 2.09 +/- 0.01 mM with an enthalpy of demicellization of 4.91 +/- 0.11 kJ/mol. The ability of 11 to enhance the gastrointestinal absorption of the aminoglycoside antibiotic gentamicin (1), a hydrophilic polycation with negligible oral bioavailability, was assessed in vivo using rats. Rats dosed orally with a mixture of 11 (100 mg/kg) and 1 (60 mg/kg) had a statistically significant (P < or = 0.034) increase in Cmax, AUC120, and percent absolute bioavailability (F) compared to control 1 (60 mg/kg) alone. The highest bioavailability (F = 9.1 +/- 2.0%) was achieved by dosing with the mixture 11 (100 mg/kg) and 1 (15 mg/kg). This represents a 6-fold increase in bioavailability compared to the control (F = 1.4 +/- 0.3%). These results suggest that the molar ratio of 1:11 may be critical in optimizing the delivery system, a finding ascribed in part to the ion-pairing properties of 11. The effect of 11 on the gastrointestinal mucosa was assessed using light microscopy to examine tissue samples from rats used in the pharmacokinetic study. No morphological changes were found in either the esophagi or duodena of the rats examined. One rat dosed with 11 (100 mg/kg) and 1 (60 mg/kg) exhibited slight gastric erosion, which could be attributed to 11.

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“…Transcutol displays a strong absorption enhancing effect, used as a cosurfactant in microemulsions (24). M1 and M2 differ in their cosurfactants (Capryol 90 for M1 and Lauroglycol 90 for M2), even though of very close molecular structure (caprylate C8 vs. laurate C12; diethylene vs propylene).…”

Section: Resultsmentioning

confidence: 99%

Effect of Vehicles on Topical Application of Aloe Vera and Arnica Montana Components

et al. 2007

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Diethyl ether fraction of Labrasol having a stronger absorption enhancing effect on gentamicin than Labrasol itself

Cited by 17 publications

References 25 publications

Control of Transdermal Permeation of Hydrocortisone Acetate from Hydrophilic and Lipophilic Formulations

Control of Transdermal Permeation of Hydrocortisone Acetate from Hydrophilic and Lipophilic Formulations

Design, Synthesis, and Evaluation of a Liposaccharide Drug Delivery Agent: Application to the Gastrointestinal Absorption of Gentamicin

Effect of Vehicles on Topical Application of Aloe Vera and Arnica Montana Components

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