An investigation into the mechanism of dissolution rate enhancement of poorly water-soluble drugs from spray chilled gelucire 50/13 microspheres

Qi, Sheng; Marchaud, Delphine; Craig, Duncan Q.M.

doi:10.1002/jps.21832

Cited by 45 publications

(22 citation statements)

References 32 publications

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“…). These observations can help in explaining why in solid lipid matrix the effect of tempering on the drug release rate is ambiguous, with several works observing an increase in the drug release rate related to increased porosity and others noticing a decrease in the drug release kinetics because of increased crystallite size and tortuosity …”

Section: Discussionmentioning

confidence: 99%

“…On one hand, an undesired retarded drug release after storage that has been explained with the super water‐repellent properties of bloomed surfaces . On the other hand, several formulations have been reported showing a significant increase in their dissolution rate that has been explained with the increase in porosity . Therefore, several works have added a tempering step after production to avoid these changes during storage …”

Section: Introductionmentioning

confidence: 99%

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Role of Lipid Blooming and Crystallite Size in the Performance of Highly Soluble Drug-Loaded Microcapsules

Lopes

Becker

Stehr³

et al. 2015

Journal of Pharmaceutical Sciences

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Role of Lipid Blooming and Crystallite Size in the Performance of Highly Soluble Drug-Loaded Microcapsules

Lopes

Becker

Stehr³

et al. 2015

Journal of Pharmaceutical Sciences

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“…The unique bulk properties of Gelucire 50/13 based gels include their semi-liquid crystalline structures, which evolve from lamellar to hexagonal and cubic phases depending on the water content of the gels (Qi et al, 2010;Codoni et al, 2015). For the gels with intermediate to high water contents structural analyses suggest the possibility of the co-existence of multiple liquid crystalline phases.…”

Section: Introductionmentioning

confidence: 99%

Disc-shaped polyoxyethylene glycol glycerides gel nanoparticles as novel protein delivery vehicles

Codoni

Cowan

Bradley

et al. 2015

International Journal of Pharmaceutics

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Disc-shaped nanoparticles with high aspect ratios have been reported to show preferential cellular uptake in vitro by mammalian cells. However, engineering and producing such disc-shaped nanoparticles are often complex. This study reports for the first time the use of a single, approved pharmaceutical excipient to prepare stable disc-shaped nanoparticles with a high aspect ratio via a simple, organic solvent free process. These disc-shaped nanoparticles were formed by fragmentation of stearoyl macrogol-32 glycerides (Gelucire 50/13) hydrogels. The nanoparticles showed good physical stability as a result of their outer coating of polyethylene glycol (PEG) that is a part of Gelucire composition. Using lysozyme as a model hydrophilic protein, these nanoparticles demonstrated a good loading capacity for hydrophilic macromolecules, mainly via surface adsorption. As a result of the higher hydrophobicity of the core of the nano-discs, the loading efficiency of hydrophobic model components, such as Coumarin-6, was significantly increased in comparison to the model hydrophilic compound. These Gelucire nano-discs exhibited no cytotoxicity at the tested level of 600μg/ml for Caco-2 cells. Rapid in vitro cellular uptake of the disc-shaped nanoparticles by Caco-2 cells was observed. This rapid internalisation was attributed to the high aspect ratio of the disc-shape nanoparticles which provides a high contact surface area between the particles and cells and may lower the strain energy required for membrane deformation during uptake. The results of this study demonstrate the promising potential of Gelucire nano-discs as effective nanocarriers for drug delivery and which can be manufactured using a simple solvent-free process.

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“…[14, 25–29] Processing of these formulations may be accomplished utilizing several methodologies, including hot emulsification, extrusion, or spray chilling with the final product being in dry powder form. [30,31] Some solid and liquid formulations of mebendazole have already been studied, such as a solid dispersions with low-substituted hydroxypropylcellulose (L-HPC),[32] a tablet formulated with guar gum,[33] complexation with polyethylene glycol (PEG-6000),[34] complexation with Povidone K12 PF,[35] and various oil preparations[36]. However, to the best of our knowledge, this is the first study involving the incorporation of mebendazole in a nanostructured lipid formulation (NLF).…”

Section: Introductionmentioning

confidence: 99%

Effect of squalane on mebendazole-loaded Compritol^®nanoparticles

Graves

Ledet

Nation

et al. 2015

Journal of Biomaterials Science, Polymer Edition

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The objective of this study is to develop nanostructured lipid formulations (NLF) of Compritol for the delivery of mebendazole. The formulations were prepared with Compritol 888 ATO, squalane, and Pluronic F68. Nine batches with different amounts of modifier, squalane, and drug were prepared. The formulations were characterized by evaluating particle size, morphology, and zeta potential. The thermal properties of the formulations were analyzed by differential scanning calorimetry (DSC). The encapsulation efficiency of each formulation and the drug release rates from each formulation were quantified by UPLC. The particles were spherical and had median particle sizes between 300 and 600 nm (50th percentile). A linear relationship was observed between Compritol/squalane composition and the melting point of the mixture. The DSC scans of the formulations revealed some recrystallization of the drug from the formulations, and the amount of recrystallization correlated with the amount of squalane in the formulation. Approximately 70% efficiency of encapsulation was observed in the formulations with 30% (w/w) squalane, and these formulations also had faster dissolution rates compared to the other formulations. Overall, the formulations with 30% squalane are the preferred formulation for future testing.

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An investigation into the mechanism of dissolution rate enhancement of poorly water-soluble drugs from spray chilled gelucire 50/13 microspheres

Cited by 45 publications

References 32 publications

Role of Lipid Blooming and Crystallite Size in the Performance of Highly Soluble Drug-Loaded Microcapsules

Role of Lipid Blooming and Crystallite Size in the Performance of Highly Soluble Drug-Loaded Microcapsules

Disc-shaped polyoxyethylene glycol glycerides gel nanoparticles as novel protein delivery vehicles

Effect of squalane on mebendazole-loaded Compritol^®nanoparticles

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An investigation into the mechanism of dissolution rate enhancement of poorly water-soluble drugs from spray chilled gelucire 50/13 microspheres

Cited by 45 publications

References 32 publications

Role of Lipid Blooming and Crystallite Size in the Performance of Highly Soluble Drug-Loaded Microcapsules

Role of Lipid Blooming and Crystallite Size in the Performance of Highly Soluble Drug-Loaded Microcapsules

Disc-shaped polyoxyethylene glycol glycerides gel nanoparticles as novel protein delivery vehicles

Effect of squalane on mebendazole-loaded Compritol®nanoparticles

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Product

Resources

About

Effect of squalane on mebendazole-loaded Compritol^®nanoparticles