Optimization and evaluation of zein nanoparticles to improve the oral delivery of glibenclamide. In vivo study using C. elegans

Lucio, David; Martínez-Ohárriz, María Cristina; Jaras, Gonzalo; Aranaz, Paula; González-Navarro, Carlos J.; Rădulescu, Aurel

doi:10.1016/j.ejpb.2017.09.018

Cited by 49 publications

(16 citation statements)

References 39 publications

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“…In accordance with recorded data, GBD displayed characteristic diffraction peaks at 2θ values of 10.8°, 11.5°, 19.2°, 19.6°, 21.6° and 23.7°. 42 The PXRD of anhydrous lactose showed sharp diffraction peaks at 2θ of 11.30°, 18.38°, 21.62°, and 24.02°, indicating a highly crystalline compound, 43 whereas MCC PH 101 showed a characteristic peak at diffraction angle of 2θ at 22.0°. The GBD-MCC or GBD-lactose PXRDs were very similar to their corresponding plain carriers and none of characteristic diffraction peaks of GBD can be clearly recorded.…”

Section: Crystallinity Assessmentmentioning

confidence: 98%

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

Ali

Hanafy

Alqurshi

2019

IJN

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Introduction: Presenting poorly water-soluble drugs as nanoparticles has shown to be an effective technique in enhancing drug dissolution rate, intrinsic solubility, and thus oral bioavailability. Nevertheless, working with nanoparticles introduces many challenges, one of which is their physical instability. Formulating nanoparticles into a solid dosage form may overcome such challenges and thus unlock the potential benefits of nanosizing. Methods: The current work investigates the possibility of developing a novel solid dosage form, with enhanced dissolution rate, whereby nanocrystals (~400 nm) of the class II Biopharmaceutical Classification System drug, glyburide (GBD) were fabricated through combined precipitation and homogenization procedures. Using a novel, but scalable, spraying technique, GBD nanocrystals were loaded onto commonly used tablet fillers, water-soluble lactose monohydrate (LAC), and water insoluble microcrystalline cellulose (MCC). Conventional tableting processes were then used to convert the powders generated into a tablet dosage form. Results: Studies of redispersibility showed considerable preservation of size characteristics of GBD nanocrystals during downstream processing with redispersibility indices of 105 and 118 for GBD-LAC and GBD-MCC, respectively. Characterization by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy showed that the powders generated powders contained nanosized crystals of GBD which adhered to carrier surfaces. Powder flowability was characterized using Hausner ratio (HR) and Carr's index (CI). GBD-LAC-loaded particles exhibited poor flowability with CI and HR of 37.5% and 1.60, respectively, whilst GBD-MCC particles showed a slightly improved flowability with CI and HR of 26.47% and 1.36, respectively. The novel tablet dosage form met US Pharmacopeia specifications, including drug content, hardness, and friability. Conclusion: Higher dissolution rates were observed from the nanocrystal-based tablets compared to the microsized and commercial drug formulations. Moreover, the novel nanocrystal tablet dosage forms showed enhanced in vivo performance with area under the plasma concentrationtime curve in the first 24 hours values 1.97 and 2.24 times greater than that of marketed tablets.

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Section: Crystallinity Assessmentmentioning

confidence: 98%

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

Ali

Hanafy

Alqurshi

2019

IJN

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“…The evaluation of the efficacy of insulin-loaded nanoparticles was performed by the quantification of the fat tissue inside the worm, as described previously [38]. The assays were carried out in triplicates in 6-well plates containing 4 mL glucose-supplemented NGM (0.5% w/v) per well.…”

Section: In Vivo Efficacy Of the Nanoparticles In C Elegansmentioning

confidence: 99%

Zein-Based Nanoparticles as Oral Carriers for Insulin Delivery

et al. 2021

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Zein, the major storage protein from corn, has a GRAS (Generally Regarded as Safe) status and may be easily transformed into nanoparticles, offering significant payloads for protein materials without affecting their stability. In this work, the capability of bare zein nanoparticles (mucoadhesive) and nanoparticles coated with poly(ethylene glycol) (mucus-permeating) was evaluated as oral carriers of insulin (I-NP and I-NP-PEG, respectively). Both nanocarriers displayed sizes of around 270 nm, insulin payloads close to 80 µg/mg and did not induce cytotoxic effects in Caco-2 and HT29-MTX cell lines. In Caenorhabditis elegans, where insulin decreases fat storage, I-NP-PEG induced a higher reduction in the fat content than I-NP and slightly lower than the control (Orlistat). In diabetic rats, nanoparticles induced a potent hypoglycemic effect and achieved an oral bioavailability of 4.2% for I-NP and 10.2% for I-NP-PEG. This superior effect observed for I-NP-PEG would be related to their capability to diffuse through the mucus layer and reach the surface of enterocytes (where insulin would be released), whereas the mucoadhesive I-NP would remain trapped in the mucus, far away from the absorptive epithelium. In summary, PEG-coated zein nanoparticles may be an interesting device for the effective delivery of proteins through the oral route.

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“…Zein is defined as the major storage prolamin of the corn‐grain endosperm (Xue et al., ). Zein is considered a hydrophobic protein due to its high content of amino acids, such as alanine (10%), leucine (20%), and proline (10%), it is insoluble in water (Lucio et al., ) and is generally recognized as safe by the US Food Drug Administration (Chen & Jones, ). Zein consists of three polypeptides: α ‐zein of 19 to 24 kDa (75 to 80%); β ‐zein of 17 to 18 kDa (10 to 15%), and γ ‐zein, of 27 kDa (5 to 10%) (Thapa et al., ).…”

Section: Introductionmentioning

confidence: 99%

Gallic Acid‐Loaded Zein Nanoparticles by Electrospraying Process

Tapia-Hernández

Del‐Toro‐Sánchez

Cinco-Moroyoqui

et al. 2019

Journal of Food Science

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Currently, electrospraying is a novel process for obtaining the nanoparticles from biopolymers. Zein nanoparticles have been obtained by this method and used to protect both hydrophilic and hydrophobic antioxidant molecules from environmental factors. The objective of this work was to prepare and characterize gallic acid‐loaded zein nanoparticles obtained by the electrospraying process to provide protection to gallic acid from environmental factors. Thus, it was related to the concentration of gallic acid in physicochemical and rheological properties of the electrosprayed solution, and also to equipment parameters, such as voltage, flow rate, and distance of the collector in morphology, and particle size. The physicochemical properties showed a relationship in the formation of a Taylor cone, in which at a low concentration of gallic acid (1% w/v), low viscosity (0.00464 ± 0.00001 Pa·s), and density (0.886 ± 0.00002 g/cm3), as well as high electrical conductivity (369 ± 4.3 µs/cm), forms a stable cone‐jet mode. The rheological properties and the Power Law model of the gallic acid‐zein electrosprayed solution demonstrated Newtonian behavior (n = 1). The morphology and size of the particle were dependent on the concentration of gallic acid. Electrosprayed parameters with high voltage (15 kV), low flow rate (0.1 mL/hr), and short distance (10 cm) exhibited a smaller diameter and spherical morphology. FT–IR showed interaction in the gallic acid‐loaded zein nanoparticle by hydrogen bonds. Therefore, the electrospraying process is a feasible technique for obtaining gallic acid‐loaded zein nanoparticles and providing potential protection to gallic acid from environmental factors.

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Optimization and evaluation of zein nanoparticles to improve the oral delivery of glibenclamide. In vivo study using C. elegans

Cited by 49 publications

References 39 publications

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

Zein-Based Nanoparticles as Oral Carriers for Insulin Delivery

Gallic Acid‐Loaded Zein Nanoparticles by Electrospraying Process

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