Propofol solubilization and structural transformations in dilutable microemulsion

Perlstein, My; Aserin, Abraham; Wachtel, Ellen; Garti, Nissim

doi:10.1016/j.colsurfb.2015.08.044

Cited by 20 publications

(6 citation statements)

References 41 publications

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“…Microemulsion (μE)-based drug-carrier systems exhibit high-performance functionality owing to their ease of formulation, biocompatibility, and structural diversity. − For completeness, microemulsions (μEs) are optically isotropic, transparent, and thermodynamically stable microfluids of two immiscible liquids (typically oil and water), homogenized by surfactants and often formulated in conjunction with co-surfactants. − As a smart drug-carrier system, μEs play an important role in local, oral, nasal, ocular, transdermal, and parenteral drug delivery and sustained release formulations of active pharmaceutical ingredients. − Drug release mechanism mainly depends on the structural type of μE, i.e., water-in-oil (w/o), oil-in-water (o/w), or bicontinuous domain. ,, Most significantly, drugs that are poorly permeable across the diffusional barriers and have low water solubility are transported with the support of μEs. The path of absorption, particle size, solubility, and distribution of drug among μE components are the prime factors that directly affect the absorption of the drug from μEs. , …”

Section: Introductionmentioning

confidence: 99%

Fourth-Generation Antibiotic Gatifloxacin Encapsulated by Microemulsions: Structural and Probing Dynamics

et al. 2018

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To overcome the increased disease rate, utilization of the versatile broad spectrum antibiotic drugs in controlled drug-delivery systems has been a challenging and complex consignment. However, with the development of microemulsion (μE)-based formulations, drugs can be effectively encapsulated and transferred to the target source. Herein, two biocompatible oil-in-water (o/w) μE formulations comprising clove oil/Tween 20/ethylene glycol/water (formulation A) and clove oil/Tween 20/1-butanol/water (formulation B) were developed for encapsulating the gatifloxacin (GTF), a fourth-generation antibiotic. The pseudoternary phase diagrams were mapped at a constant surfactant/co-surfactant (1:1) ratio to bound the existence of a monophasic isotropic region for as-formulated μEs. Multiple complementary characterization techniques, namely, conductivity (σ), viscosity (η), and optical microscopy analyses, were used to study the gradual changes that occurred in the microstructure of the as-formulated μEs, indicating the presence of a percolation transformation to a bicontinuous permeate flow. GTF showed good solubility, 3.2 wt % at pH 6.2 and 4.0 wt % at pH 6.8, in optimum μE of formulation A and formulation B, respectively. Each loaded μE formulation showed long-term stability over 8 months of storage. Moreover, no observable aggregation of GTF was found, as revealed by scanning transmission electron microscopy and peak-to-peak correlation of IR analysis, indicating the stability of GTF inside the formulation. The average particle size of each μE, measured by dynamic light scattering, increased upon loading GTF, intending the accretion of drug in the interfacial layers of microdomains. Likewise, fluorescence probing sense an interfacial hydrophobic environment to GTF molecules in any of the examined formulations, which may be of significant interest for understanding the kinetics of drug release.

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Section: Introductionmentioning

confidence: 99%

Fourth-Generation Antibiotic Gatifloxacin Encapsulated by Microemulsions: Structural and Probing Dynamics

et al. 2018

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“…SD-NMR is a very useful technique for the characterization of the ME microstructure by determination of the diffusivity of its components. ,, The self-diffusion coefficients of the components, as obtained from SD-NMR analysis of the empty and curcumin-loaded ME systems are shown in Figure A–D. In detail, Figure shows the diffusivity values of the different system components: the surfactants (A), water (B), propylene glycol (C), and curcumin (D), for empty and loaded ME systems diluted to 90 wt % water, ME 90 wt % water + gellan (1 wt %) mixture, and the dissolved film, which was previously formed from the ME–gellan mixture.…”

Section: Resultsmentioning

confidence: 99%

“…The composition of the empty-ME concentrate (simply termed “concentrate”) was based on our previous studies ,, and consisted of Tween 80 as the surfactant, propylene glycol as the solvent, and IPM as the oil phase in the weight ratio of [7:2:1]. The curcumin-loaded ME concentrate was prepared by adding curcumin (2 wt %) to the empty concentrate.…”

Section: Methodsmentioning

confidence: 99%

“…The diffusivity values provide unique information on the mobility of each component that contributes to a structural understanding of the ME organization. 4,27 By combining the results from the two magnetic-resonance techniques, useful information was obtained on the nanodomains in the film and before and after being embedded in the film. This suggests the use of this platform as a novel drug delivery system.…”

Section: Introductionmentioning

confidence: 99%

“…Self-diffusion coefficients of the main ME components were calculated from SD-NMR measurement. The diffusivity values provide unique information on the mobility of each component that contributes to a structural understanding of the ME organization. , …”

Section: Introductionmentioning

confidence: 99%

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Structural Characterization of Reconstituted Bioactive-Loaded Nanodomains after Embedding in Films Using Electron Paramagnetic Resonance and Self-Diffusion Nuclear Magnetic Resonance Techniques

et al. 2019

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Pharmaceutical applications of microemulsions (MEs) as drug delivery vehicles are recently gaining scientific and practical interests. Most MEs are able to solubilize bioactive molecules, but, at present, they cannot guarantee either controlled release of the drugs or significant advantage in the bioavailability of the bioactives. This study proposes to incorporate the modified ME structures, or nanodomains, into a natural polymeric film, to be used as a stable and capacious reservoir of drug-loaded nanodomains. These nanodomainloaded films may release the nanodroplets along with the drug molecules in a slow and controlled way. Gellan gum, an anionic polysaccharide, was used in aqueous solution as the film former, and curcumin, hydrophobic polyphenol, served as the guest molecule in the loaded systems. Films were prepared by using empty and curcumin-loaded MEs. It is imperative to verify the persistence of the ME structure upon the dissolution of the film mimicking its behavior when in contact with a human physiological aqueous environment via reaching the cell membranes. For this purpose, the films were dissolved, and the reconstituted ME structure was compared with the ME structure before film formation. Characterization of these structures, before and after dissolution, was achieved using electron paramagnetic resonance (EPR) and self-diffusion nuclear magnetic resonance (SD-NMR) techniques. Specific spin probes were inserted in the system, and a computer-aided analysis of the EPR spectra was performed to provide information on nanodomain microstructure assemblies. In addition, the SD-NMR profile of each component was analyzed to extract information on the diffusivity of the ME components before film formation and after ME reconstitution. The EPR and SD-NMR results were in good agreement to each other. The most important finding was that, after film dissolution, the ME nanodomains were reversibly and spontaneously reformed. It was also found that the film did not perturb the ME-nanodomain structure embedded in it. The film remained transparent and the bioactive curcumin was easily solubilized into the ME-droplet/water interface even after film dissolution. The combined techniques confirmed that the film constituted by bioactive-loaded MEs can serve as novel drug delivery vehicles.

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Propofol Formulation Affects Myocardial Function in Newborn Infants

et al. 2019

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Propofol solubilization and structural transformations in dilutable microemulsion

Cited by 20 publications

References 41 publications

Fourth-Generation Antibiotic Gatifloxacin Encapsulated by Microemulsions: Structural and Probing Dynamics

Fourth-Generation Antibiotic Gatifloxacin Encapsulated by Microemulsions: Structural and Probing Dynamics

Structural Characterization of Reconstituted Bioactive-Loaded Nanodomains after Embedding in Films Using Electron Paramagnetic Resonance and Self-Diffusion Nuclear Magnetic Resonance Techniques

Propofol Formulation Affects Myocardial Function in Newborn Infants

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