Preparation and evaluation of w/o/w type emulsions containing vancomycin

Okochi, Hideaki; Nakano, Masahiro

doi:10.1016/s0169-409x(00)00097-1

Cited by 142 publications

(67 citation statements)

References 70 publications

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“…34 The use of a spontaneous process of emulsification using high ratios of surfactants could explain the result in the nanoscale range, which contrasts with published data, where multiple emulsions are generally in the microscale range. [38][39][40] Moreover, the low-energy process could allow the inclusion of polar drugs sensitive to high shear stress, such as peptides. 41 …”

Section: Discussionmentioning

confidence: 99%

Formulation and cytotoxicity evaluation of new self-emulsifying multiple W/O/W nanoemulsions

Sigward¹,

Mignet²,

Rat³

et al. 2013

IJN

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Three multiple water-in-oil-in-water (W/O/W) nanoemulsions have been designed for potential inclusion of either lipophilic or hydrophilic drugs using a two-step emulsification process exclusively based on low-energy self-emulsification. The W/O primary emulsion was constituted by a blend of oil (medium chain triglyceride), a mixture (7:3) of two surfactants, and a 10% water phase. The surfactants were a mixture of Polysorbate-85/Labrasol ® , Polysorbate-85/ Cremophor ® EL or glycerol/Polysorbate-85. The final W/O/W nanoemulsions were obtained by the addition of water, with a weight ratio nanoemulsion/water of 1:2. The multiple emulsion stability was found to increase from 24 hours to 2 and 6 months with Labrasol, glycerol, and Cremophor, respectively. Cytotoxicity was found for formulations including Labrasol and Cremophor EL. The concentration of emulsion inhibiting 50% cell viability (IC 50 ) was determined using the alamarBlue ® test, giving after 24 hours of incubation, IC 50 = 10.2 mg/mL for the Labrasol formulation and IC 50 = 11.8 mg/mL for the Cremophor EL formulation. Corresponding calculated IC 50 values for surfactants were 0.51 mg/mL for Labrasol and 0.59 mg/mL for Cremophor EL. In both cases, cytotoxicity was due to an apoptotic mechanism, evidenced by chromatin condensation and P2X7 cell death receptor activation. The formulation including glycerol, investigated between 1 and 100 mg/mL concentration of nanoemulsion, did not affect cell viability. Moreover, neither chromatin condensation nor P2X7 activation was found between the 10 and 30 mg/mL final concentration of the emulsion. This last formulation would therefore be of major interest for further developments.

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Section: Discussionmentioning

confidence: 99%

Formulation and cytotoxicity evaluation of new self-emulsifying multiple W/O/W nanoemulsions

Sigward¹,

Mignet²,

Rat³

et al. 2013

IJN

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“…The pharmacokinetic parameters of DOX-loaded W/O/W emulsions were significantly different from that in the DOX solution. 46) The W/O/W emulsions gave a significantly higher AUC and hence ca. 17-fold better bioavailability compared to the DOX solution.…”

Section: Effect Of Pgpr and Tgpr On Dox-loaded W/o/w Emulsionmentioning

confidence: 97%

“…In cosmetics and pharmaceuticals, W/O/W emulsions have been used for controlled release and targeted delivery of drugs. [5][6][7][8] Food applications include the encapsulation of vitamin/minerals, 9,10) and the production of low-calorie foods. 11) W/O/W emulsions are usually created using conventional homogenization technology in a two-step procedure.…”

mentioning

confidence: 99%

Fabrication, Characterization and Pharmacokinetic Evaluation of Doxorubicin-Loaded Water-in-Oil-in-Water Microemulsions Using a Membrane Emulsification Technique

Pradhan

Kim

Jeong

et al. 2014

CHEMICAL & PHARMACEUTICAL BULLETIN

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Doxorubicin (DOX)-loaded water-in-oil-in-water (W/O/W) microemulsions were produced using a shirasu-porous-glass (SPG) membrane emulsification technique. Soybean oil was used as the oil phase; polyglycerol polyricinoleate (PGPR) or tetraglycerol polyricinoleate (TGPR) was used as the surfactant to stabilize the feed W/O emulsions, while Tween 20 was used in the external water phase to stabilize oil droplets containing water droplets. Increasing the feed pressure from 50 to 90 kPa increased the particle size of W/O/W emulsions, whereas it was decreased by increasing the agitator speed. The smallest particle sizes of multiple emulsions were obtained at the feed pressure of 50 kPa and agitator speed of 350 rpm. Under this set of conditions, the increase in the concentration of PGPR or TGPR showed a decrease in the particle size of DOX-loaded W/O/W emulsions. The optimized formulation comprising of 5% w/v PGPR and 3% w/v Tween 20 in the oil phase and external water phase, respectively, with 0.5% w/v of DOX had a particle size of 0.440 0.007 µm and polydispersity index of 0.220 0.087, which was supported by the transmission electron microscopy image. The formulations showed a sustained release profile in phosphate buffer solution (pH 7.4). The plasma concentrations of DOX after intravenous administration to rats were prolonged and gave approximately 17-fold higher area under the drug concentration-time curve (AUC) compared to free DOX solution. Thus, these results demonstrated that the SPG membrane emulsification technique could be used as a promising technique to prepare W/O/W microemulsions for delivering DOX with sustained release characteristics and better bioavailability.Key words microemulsion; shirasu-porous-glass; doxorubicin; sustained release; pharmacokinetics Over the past two decades, an increasing interest has been devoted to multiple emulsions due to their multiple compartment structure and an immense capability of encapsulating hydrophilic drug substances for sustained released characteristics. [1][2][3][4] The potential application of water-in-oil-in-water (W/O/W) multiple emulsion is not only limited to pharmaceuticals but also in the field of cosmetics and food industry. In cosmetics and pharmaceuticals, W/O/W emulsions have been used for controlled release and targeted delivery of drugs. [5][6][7][8] Food applications include the encapsulation of vitamin/minerals, 9,10) and the production of low-calorie foods. 11) W/O/W emulsions are usually created using conventional homogenization technology in a two-step procedure. 12) First, a primary water-in-oil (W/O) emulsion is prepared by homogenizing an oil phase and an aqueous phase together in the presence of a suitable oil-soluble emulsifier (low hydrophilic to lipophilic balance (HLB)<10). Second, W/O/W emulsion is prepared by homogenizing W/O emulsion with another aqueous phase in the presence of a suitable water-soluble emulsifier (high HLB>10). 1) However, the second step often results in high polydispersity or low encapsulation efficiency. Therefo...

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“…[29][30][31] Three types of solutions were prepared: a m-phenylenediamine aqueous solution, liquid paraffin containing toluene or phenol and Span 80, and a mixture of distilled water and Tween 20. The main fluids used in these solutions included distilled water for the inner aqueous phase (inner droplets), liquid paraffin for the middle oil phase (outer droplets), and distilled water for the outer aqueous phase.…”

Section: Reagents and Sample Preparationmentioning

confidence: 99%

“…When the partition coefficient (log Kow = -0.33) is taken into account, this compound should exist in the inner aqueous phase, rather than in the middle oil phase. Though a middle oil phase exists between the inner and outer phases, the miniaturization of droplets, which generally proceeds by stirring, 29 might accelerate the moving of m-phenylenediamine from an outer phase to an inner phase and/or that of water from an inner phase to an outer phase. Though further discussion is required, the same tendency was also observed in the case of a toluene-multiple emulsion, i.e., the ratio of the number of plots in C and D was slightly increased from 0.5 to 3.5%, as mentioned previously.…”

Section: Scatter Plots For the Evaluation Of Agingmentioning

confidence: 99%

Evaluating the Aging of Multiple Emulsions Using Resonance- Enhanced Multiphoton Ionization Time-of-Flight Mass Spectrometry

Tsuda

Uchimura

2016

ANAL. SCI.

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Resonance-enhanced multiphoton ionization time-of-flight mass spectrometry was applied to measurements of multiple emulsions with no pretreatment; a method for the quantitative evaluation of aging was proposed. We prepared water-inoil-in-water (W/O/W) multiple emulsions containing toluene and m-phenylenediamine. The samples were measured immediately following both preparation and after having been stirred for 24 h. Time profiles of the peak areas for each analyte species were obtained, and several intense spikes for toluene could be detected from each sample after stirring, which suggests that the concentration of toluene in the middle phase had increased during stirring. On the other hand, in the case of a W/O/W multiple emulsion containing phenol and m-phenylenediamine, spikes for m-phenylenediamine, rather than phenol, were detected after stirring. In the present study, the time-profile data were converted into a scatter plot in order to quantitatively evaluate the aging. As a result, the ratio of the plots where strong signal intensities of toluene were detected increased from 8.4% before stirring to 33.2% after stirring for 24 h. The present method could be a powerful tool for evaluating multiple emulsions, such as studies on the kinetics of the encapsulation and release of active ingredients.Keywords REMPI-TOFMS, multiple emulsion, aging

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Preparation and evaluation of w/o/w type emulsions containing vancomycin

Cited by 142 publications

References 70 publications

Formulation and cytotoxicity evaluation of new self-emulsifying multiple W/O/W nanoemulsions

Formulation and cytotoxicity evaluation of new self-emulsifying multiple W/O/W nanoemulsions

Fabrication, Characterization and Pharmacokinetic Evaluation of Doxorubicin-Loaded Water-in-Oil-in-Water Microemulsions Using a Membrane Emulsification Technique

Evaluating the Aging of Multiple Emulsions Using Resonance- Enhanced Multiphoton Ionization Time-of-Flight Mass Spectrometry

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