The influence of excipients on the diffusion of ibuprofen and paracetamol in gastric mucus

Shaw, Lance R.; Irwin, W. J.; Grattan, T. J.; Conway, Barbara R.

doi:10.1016/j.ijpharm.2004.11.028

Cited by 33 publications

(22 citation statements)

References 26 publications

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“…There are cellular models such as HT29-MTX, 20 HT29-FU, 21 HT29-GlucH, 22 and co-cultures Caco-2/ HT29-MTX, 23 Caco-2/HT29-H, 24 Caco-2/HT29-M6. 25 Various protocols have been developed to evaluate interactions between particles and mucus; for example, multiple particle tracking, 12 modified microfiltration device, 14 mucoadhesion assay, 15 in vivo experimentation 26 with radioactivity studies 27 or pharmacokinetic studies, 28 binding properties, 29 side-byside system, 30 side-on-3-compartment, 31 19 and cell association. 37 Some techniques are inconvenient to use, such as the complicated equipment used for multiple particle tracking, a fluorophore such as FRAP, or radioactive materials.…”

Section: Groo Et Almentioning

confidence: 99%

Fate of paclitaxel lipid nanocapsules in intestinal mucus in view of their oral delivery

Groo¹,

Saulnier²,

Gimel³

et al. 2013

IJN

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The bioavailability of paclitaxel (Ptx) has previously been improved via its encapsulation in lipid nanocapsules (LNCs). In this work, the interactions between LNCs and intestinal mucus are studied because they are viewed as an important barrier to successful oral delivery. The rheological properties of different batches of pig intestinal mucus were studied under different conditions (the effect of hydration and the presence of LNCs). Fluorescence resonance energy transfer (FRET) was used to study the stability of LNCs in mucus at 37°C for at least 3 hours. Diffusion through 223, 446, and 893 μm mucus layers of 8.4, 16.8, and 42 μg/mL Ptx formulated as Taxol® (Bristol-Myers Squibb, Rueil-Malmaison, France) or encapsulated in LNCs (Ptx-LNCs) were investigated. The effect of the size of the LNCs on their diffusion was also investigated (range, 25–110 nm in diameter). Mucus behaves as a non-Newtonian gel with rheofluidifying properties and a flow threshold. The viscous (G″) and elastic (G′) moduli and flow threshold of the two mucus batches varied with water content, but G′ remained below G″. LNCs had no effect on mucus viscosity and flow threshold. The FRET efficiency remained at 78% after 3 hours. Because the destruction of the LNCs would lead to a FRET efficiency below 25%, these results suggest only a slight modification of LNCs after their contact with mucus. The diffusion of Taxol® and Ptx-LNCs in mucus decreases if the mucus layer is thicker. Interestingly, the apparent permeability across mucus is higher for Ptx-LNCs than for Taxol® for drug concentrations of 16.8 and 42 μg/mL Ptx ( P <0.05). The diffusion of Ptx-LNCs through mucus is not size-dependent. This study shows that LNCs are stable in mucus, do not change mucus rheological properties, and improve Ptx diffusion at low concentrations, thus making these systems good candidates for Ptx oral delivery. The study of the physicochemical interaction between the LNC surface and its diffusion in mucus is now envisioned.

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Section: Groo Et Almentioning

confidence: 99%

Fate of paclitaxel lipid nanocapsules in intestinal mucus in view of their oral delivery

Groo¹,

Saulnier²,

Gimel³

et al. 2013

IJN

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“…For example, it is an important analgesic drug and antipyretic agent, and in combination with opioid analgesics, it can also be used in the management of more severe pain such as post surgical pain, and provide palliative care in advanced cancer patients [1][2][3][4][5][6].…”

Section: Introductionmentioning

confidence: 99%

“…Currently, diffusion coefficients of paracetamol in aqueous solutions and their dependence on media composition (e.g., pH, ionic strength and metal ions) have been poorly characterized, even though these transport parameters are necessary to obtain a satisfactory understanding of its important pharmacy function. A few diffusion coefficients of paracetamol in different systems (e.g., in hydrated alginate and alginic acid gels [3], in macroporous chitosan hydrogels using a diaphragm cell technique [4], in 1% (w/w) agarose gels at different temperatures [5], and through gastric mucus, where it was shown that mucus acts as a passive barrier in the case of paracetamol diffusion [6]) have been reported but, as far as the authors know, after careful literature search, no data are available for aqueous systems involving this drug at T = 298.15 K.…”

Section: Introductionmentioning

confidence: 99%

Diffusion coefficients of paracetamol in aqueous solutions

Ribeiro

Barros

Veríssimo

et al. 2012

The Journal of Chemical Thermodynamics

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“…In each trial, the linear relationship of concentration against time was obtained (R 2 = 0.95-0.99) what confirms that process was realized under the quasi-state conditions. Therefore, we can write Described procedure of determination of the effective diffusion coefficient is similar to the presented by other authors (Brodin et al 2010;Desai and Vadgama 1991;Shaw et al 2004). …”

Section: Determination Of the Apparent Mucus Viscositymentioning

confidence: 82%

The Influence of Functional Carrier Particles (FCPs) on the Molecular Transport Rate Through the Reconstructed Bronchial Mucus: In Vitro Studies

2014

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Mass transfer of deposited drug particles in the human lungs is an important factor in the effective drug delivery by inhalation. This study is focused on the basic research related to the possible acceleration of drug penetration toward the intended site of action through the barrier created by mucus layer. It is proposed that beneficial effect can be obtained by altering the mucus structure by inhaled functional carrier particles (FCPs) which are used to enhance pulmonary delivery of aerosolized powder drugs and simultaneously contain mucolytics (e.g., N-acetylcysteine: NAC). The FCPs were prepared by an optimized spray-drying technique and tested regarding their influence on the rheology of the reconstructed bronchial mucus and the transport rate of model drugs (Rhodamine B and Disodium Cromoglycate). The results indicate that the viscosity of mucus with high mucin concentration (i.e., reflecting a disease is reduced by up to 42 % depending on the concentration of added FCPs what is similar to the effect of pure NAC. Simultaneously, the effective diffusion coefficient D eff of the model drug through the mucus increased from 23 × 10 −7 (pure mucus) to 42 × 10 −7 cm 2 /s (mucus modified by FCPs), and it was comparable to the effect obtained with pure NAC (51 × 10 −7 cm 2 /s). The results confirm that using mucolytics incorporated into powder particles (drug carriers) may be used to enhance mass transfer of inhaled aerosol drugs across the bronchial mucus layer.

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The influence of excipients on the diffusion of ibuprofen and paracetamol in gastric mucus

Cited by 33 publications

References 26 publications

Fate of paclitaxel lipid nanocapsules in intestinal mucus in view of their oral delivery

Fate of paclitaxel lipid nanocapsules in intestinal mucus in view of their oral delivery

Diffusion coefficients of paracetamol in aqueous solutions

The Influence of Functional Carrier Particles (FCPs) on the Molecular Transport Rate Through the Reconstructed Bronchial Mucus: In Vitro Studies

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