Mucus permeating carriers: formulation and characterization of highly densely charged nanoparticles

Sousa, Irene Pereira de; Steiner, Corinna; Schmutzler, Matthias; Wilcox, Matthew; Veldhuis, Gert; Pearson, Jeffrey P.; Huck, Christian W.; Salvenmoser, Willi; Bernkop‐Schnürch, Andreas

doi:10.1016/j.ejpb.2014.12.024

Cited by 119 publications

(55 citation statements)

References 31 publications

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“…However, pre-incubation of the same formulation with IAP caused enzymatic cleavage of phosphate leading to a positive zeta potential. Combined with mucus, the surface charge of SEDDS was lower and reached -1.98  0.30 mV within 1 h. These results were in good accordance with earlier findings reported by Pereira de Sousa et al that NPs also behave in the same way (Pereira de Sousa et al, 2015). The zeta potential of positively charged NPs formed by ionic gelation of chitosan and chondroitin sulfate quickly decreased in the first hour of incubation with diluted mucus and finally became negative.…”

Section: Mucus-sedds Interaction Studiessupporting

confidence: 92%

“…The permeation of SEDDS across porcine intestinal mucus was investigated within this study using rotating tube technique as previously described (Pereira de Sousa et al, 2015). In brief, silicone tubes with a diameter of 3 mm were filled with 100 mg of mucus using a syringe without a needle and closed at one end.…”

Section: Mucus Diffusion Studiesmentioning

confidence: 99%

“…In fact, mucus contains anionic substructures, namely, sialic acid and sulfonic acid that have a negative net charge (BernkopSchnürch and Greimel, 2012). It was shown that negatively charged and uncharged NPs were capable of moving across mucus while positively charged ones were immobilized and could not permeate through mucus layer because of ionic interactions (Pereira de Sousa et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

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Development and in vitro evaluation of zeta potential changing self-emulsifying drug delivery systems for enhanced mucus permeation

Suchaoin

Sousa

Netsomboon

et al. 2016

International Journal of Pharmaceutics

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Section: Mucus-sedds Interaction Studiessupporting

confidence: 92%

Section: Mucus Diffusion Studiesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Development and in vitro evaluation of zeta potential changing self-emulsifying drug delivery systems for enhanced mucus permeation

Suchaoin

Sousa

Netsomboon

et al. 2016

International Journal of Pharmaceutics

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“…Therefore larger particles may be able to move through mucus gels depending on the surface characteristics. We have recently shown that nanoparticles made from chondroitin sulphate and chitosan (ratio 1:1) prepared by the ionic gelling method and with a diameter of 400 nm and a zeta potential of 4 mV could permeate porcine small intestinal mucus in a transwell experiment [99]. These nanoparticles mimic highly, densely charged surfaces made up of many cationic and anionic groups.…”

Section: Approaches To Overcoming the Mucus Barriermentioning

confidence: 97%

The Properties of the Mucus Barrier, a Unique Gel–How Can Nanoparticles Cross It?

2016

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The key criterion for a nanoparticle drug-delivery system is the ability to produce substantial bioavailability without damaging the physiological protective mechanisms. The main area for drug delivery is the aerodigestive tract. All epithelial surfaces have a membrane-bound layer and in the lung this layer is surmounted by a gel layer. In the gastrointestinal tract the membrane-bound mucin layer is covered by a mucus bilayer. The pore sizes of mucus gels are around 100 to 200 nm. Consequently, only nanoparticles in this size range could potentially penetrate without modification of these layers. To study nanoparticle permeation with results that pertain to in vivo conditions, native mucus mucin preparations must be used. Strategies to increase pores in mucus gels are discussed herein.

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“…The permeation ability of the prepared NPs was investigated by the rotating tube technique [27]. Plastic tube with a length of 30 mm and a diameter of 4 mm were filled in with Imucus exploiting a syringe without needle.…”

Section: Permeation Studymentioning

confidence: 99%

Nanoparticles decorated with proteolytic enzymes, a promising strategy to overcome the mucus barrier

Sousa

Cattoz

Wilcox

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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119

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Schnürch, Nanoparticles decorated with proteolytic enzymes, a promising strategy to overcome the mucus barrier, European Journal of Pharmaceutics and Biopharmaceutics (2015), doi: http://dx.doi.org/10.1016/j.ejpb. 2015.01.008 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. 3.3. Nanoparticles formulation 100 mg of PAA or enzyme-polymer conjugate were dissolved in 10 mL water to obtain a 1wt% solution and the pH was adjusted to 8. This mixture was slowly added to 7.5 mL of Lumogen aceton solution 0.07 mg/mL. After 10 min equilibration 1 mL of CaCl 2 5 mg/mL dissolved in water was added drop by drop and stirred for 30 min. The suspension was then centrifuged at 5500 rpm (4966 x g) for 25 min (MiniSpin centrifuge, Eppendorf), the supernatant discarded and the pellet washed with 50vol% aceton/water mixture for three times.Finally the washed pellet was resuspended in 1wt% trehalose/water solution by means of probe sonication for 10 sec and then lyophilized. The obtained products were referred to PAA NPs when PAA was used for the formulation, PAA-PAP NPs when PAA-PAP was used for the formulation and PAA-BRO NPs when PAA-BRO was used for the formulation. Nanoparticles characterizationNanoparticle particle size and charge characterization was carried out by using a NICOMPTM 380 ZLS PSS (Particle Sizing Systems, CA, USA). Particle size was recorded at a scattering angle of 90° for 10 min at room temperature. Zeta potential was recorded under electric field strength of 5 V/cm for 3 minutes at room temperature. Enzyme quantificationThe amount of enzyme conjugated to polymers and nanoparticles was determined by micro BCA protein assay, following the provider´s instruction. The samples were dissolved in 0.1 M NaOH solution containing 1.5wt% of sodium dodecyl sulfate to obtain a concentration of 0.1 mg/mL. The samples were incubated at 25°C in a thermomixer (Thermomixer Conform;Eppendorf, Hamburg, Germany) under constant shaking, 1000 rpm for 2 h. Thereafter, 150µL of sample were mixed with 150 µL of working reagent in a 96 well plate and incubated for 7 further 2 h at 37°C. Finally the absorbance was detected at 562 nm by using a microplate reader (TECAN Infinite M200, Austria GmbH). The amount of enzyme was extrapolated by fitting the data to a calibration curve obtained via analyzing solution with different concentration of PAP or BRO. The enzyme content of polymers and NPs was reported on a weighted base as the ratio between the amount of conjugated enzyme and the amount of polymers or NPs. The conjugation efficacy onto the polymers was calculated as weight percent of the amount of conjugated enzyme relative to...

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Mucus permeating carriers: formulation and characterization of highly densely charged nanoparticles

Cited by 119 publications

References 31 publications

Development and in vitro evaluation of zeta potential changing self-emulsifying drug delivery systems for enhanced mucus permeation

Development and in vitro evaluation of zeta potential changing self-emulsifying drug delivery systems for enhanced mucus permeation

The Properties of the Mucus Barrier, a Unique Gel–How Can Nanoparticles Cross It?

Nanoparticles decorated with proteolytic enzymes, a promising strategy to overcome the mucus barrier

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