Effect of Lipolysis on Drug Release from Self-microemulsifying Drug Delivery Systems (SMEDDS) with Different Core/Shell Drug Location

Zhang, Jianbin; Lv, Yan; Zhao, Shan; Wang, Bing; Tan, Mingqian; Xie, Hehu; Lv, Guojun; Ma, Xiaojun

doi:10.1208/s12249-014-0096-9

Cited by 28 publications

(23 citation statements)

References 46 publications

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“…This observation suggests that LVF is protected from either of the pure bulk domain (oil and water), point towards the close confinement of LVF molecules in μE. All these results indicate that the probe associated with micro aggregates may possibly reside in the interfacial vicinity, where the propagation of the excitation is inhibited and in which rotation of LVF molecules is further restricted ,…”

Section: Resultsmentioning

confidence: 69%

Structural Insights into the Microemulsion‐Mediated Formation of Fluoroquinolone Nanoantibiotics

et al. 2018

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Microemulsions (μEs) are being exploited as a potential route for yielding an extensive range of nanoparticles of different chemical nature, shapes and sizes. Nanodrugs offer new avenues for structuring better “drug delivery systems”. In this study, an oil‐in‐water (o/w) μE formulation comprising N‐butyl acetate/polysorbate 80/ethanol/water was developed for the preparation of nanoparticles of fluoroquinolone antibiotics (FLQ‐NPs). A pseudoternary phase diagram was mapped at constant surfactant/cosurfactant (1:2), revealing improved and high loading of FLQs in an optimum μE formulation. The as‐formulated μE showed high loading of FLQs as; levofloxacin (4.20 wt.%), ciprofloxacin (3.16 wt.%), moxifloxacin (2.53 wt.%), gatifloxacin (1.36 wt.%), ofloxacin (0.70 wt.%). Fourier transform IR analysis indicated good compatibility of each FLQ drug with μE excipients. However, dynamic light scattering showed an increase in the average particle size of the μE on drug loading, indicating the accumulation of FLQ at interface layer of the micelle. Additionally, lyophilized levofloxacin (a selected antibiotic) showed long‐term stability, amorphous morphology and improved dissolution rate, inspected by scanning transmission electron microscopy, X‐ray diffraction and electronic spectroscopy, respectively. Moreover, fluorescence measurements suggested the interfacial vicinity of levofloxacin within the μE domain, which may support controlled release of drug during systemic circulation.

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Section: Resultsmentioning

confidence: 69%

Structural Insights into the Microemulsion‐Mediated Formation of Fluoroquinolone Nanoantibiotics

et al. 2018

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“…Despite the fact that the effect of particle size seemed not to be a key factor affecting the diffusion coefficients, smaller SME-2 diffused faster than larger SME-1, which both contain MCT as the oil phase. In our previous report, 19 the poorly water-soluble drug resveratrol was demonstrated to be located in the hydrophobic core (the oil phase and the palisade layer of surfactant) of microemulsions, while hymecromone was located in the hydrophilic shell (the hydrophilic headgroup layer of surfactant) of microemulsions. The diffusion of drugs with different locations in the microemulsions was also compared in this study.…”

Section: Molecular Pharmaceuticsmentioning

confidence: 90%

“…Microemulsions were obtained by the dilution of SMEDDS formulations, which were prepared following our previous report. 19 Briefly, oil phase (MCT, ethyl oleate or castor oil), surfactant (Cremophor RH40) and cosurfactant (1, 2-propanediol) were accurately weighted into sealed glass vials according to the ratios shown in Table 1. Poorly water-soluble drug (hymecromone or resveratrol) or fluorescent probe was added into the mixture.…”

Section: Introductionmentioning

confidence: 99%

Influence of Microemulsion–Mucin Interaction on the Fate of Microemulsions Diffusing through Pig Gastric Mucin Solutions

Zhang

Wang

et al. 2015

Mol. Pharmaceutics

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Mucus layer, a selective diffusion barrier, has an important effect on the fate of drug delivery systems in the gastrointestinal tract. To study the fate of microemulsions in the mucus layer, four microemulsion formulations with different particle sizes and lipid compositions were prepared. The microemulsion-mucin interaction was demonstrated by the fluorescence resonance energy transfer (FRET) method. Moreover, the microemulsions were observed aggregated into micron-sized emulsions by laser confocal microscopy. We concluded the microemulsion-mucin interaction not only led to microemulsions closely adhered to mucins but also destroyed the structure of microemulsions. At last, the diffusion of blank microemulsions and microemulsion-carried drugs (resveratrol and hymecromone) through mucin solutions was determined by the fluorescence recovery after photobleaching (FRAP) method and the Franz diffusion cell method. The results demonstrated the diffusion of microemulsions was significantly hindered by mucin solutions. The particle size of microemulsions had a negligible effect on the diffusion coefficients. However, the type of lipid played an important role, which could form hydrophobic interactions with mucins. Interestingly, microemulsion-carried drugs with different core/shell locations seemed to suffer different fates in the mucin solutions. The drug incorporated in the oil core of microemulsions, resveratrol, was transported through the mucus layer by the carriers, while the drug incorporated in the surfactant shell of microemulsions, hymecromone, was separated from the carriers and diffused toward the epithelium in the form of free molecules.

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“…The type and amount of each intermediate phase is highly associated with the types of surfactant and oil, the surfactant/oil ratio, as well as the physicochemical properties of microemulsions during digestion 23 . In our previous work, we found the dissolution rate of drug from microemulsions was affected by lipolysis, which was related to the extent of the digested oil phase 24 .…”

Section: Introductionmentioning

confidence: 97%

In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET

Zhang

et al. 2018

Acta Pharmaceutica Sinica B

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Microemulsions are promising drug delivery systems for the oral administration of poorly water-soluble drugs. However, the evolution of microemulsions in the gastrointestinal tract is still poorly characterized, especially the structural change of microemulsions under the effect of lipase and mucus. To better understand the fate of microemulsions in the gastrointestinal tract, we applied small-angle X-ray scattering (SAXS) and fluorescence resonance energy transfer (FRET) to monitor the structural change of microemulsions under the effect of lipolysis and mucus. First, the effect of lipolysis on microemulsions was studied by SAXS, which found the generation of liquid crystalline phases. Meanwhile, FRET spectra indicated micelles with smaller particle sizes were generated during lipolysis, which could be affected by CaCl2, bile salts and lecithin. Then, the effect of mucus on the structural change of lipolysed microemulsions was studied. The results of SAXS and FRET indicated that the liquid crystalline phases disappeared, and more micelles were generated. In summary, we studied the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET, and successfully monitored the appearance and disappearance of the liquid crystalline phases and micelles.

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Effect of Lipolysis on Drug Release from Self-microemulsifying Drug Delivery Systems (SMEDDS) with Different Core/Shell Drug Location

Cited by 28 publications

References 46 publications

Structural Insights into the Microemulsion‐Mediated Formation of Fluoroquinolone Nanoantibiotics

Structural Insights into the Microemulsion‐Mediated Formation of Fluoroquinolone Nanoantibiotics

Influence of Microemulsion–Mucin Interaction on the Fate of Microemulsions Diffusing through Pig Gastric Mucin Solutions

In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET

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