Probing the Mucoadhesive Interactions Between Porcine Gastric Mucin and Some Water‐Soluble Polymers

Albarkah, Yasser A.; Green, Rebecca; Khutoryanskiy, Vitaliy V.

doi:10.1002/mabi.201500158

Cited by 58 publications

(31 citation statements)

References 33 publications

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“…Furthermore, ITC is a versatile analytical method that has become a gold standard in characterization of molecular interactions, which allows quantitative determination of binding constants (Ka), reaction stoichiometry ( n ), enthalpy (∆H) and entropy (∆S) change, providing a complete thermodynamic profile of investigated interaction [ 31 , 32 ]. 40 μM PGM dispersions were prepared at pH 4.5 and 7.4, and the heat flow was recorded when KTN or KOS was titrated into PGM solution (Fig.…”

Section: Resultsmentioning

confidence: 99%

“…Moreover, the formation of a protein–protein rich phase gives rise to a sharp increase in turbidity of the solution, and a reduction of initial turbidity of protein–PGM mixture solution can be observed by addition of inhibitors, which was used to investigate the reactive mechanisms between protein and PGM [ 32 ]. Therefore, urea, Tween 20 and N -ethylmaleimide (NEM), acting as strong competitor for hydrogen bonding, hydrophobic interactions and disulfide bonds [ 34 ], were added into the KTN–PGM and KOS–PGM mixture solutions, respectively (Fig.…”

Section: Resultsmentioning

confidence: 99%

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Development of keratin nanoparticles for controlled gastric mucoadhesion and drug release

et al. 2018

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BackgroundNanotechnology-based drug delivery systems have been widely used for oral and systemic dosage forms delivery depending on the mucoadhesive interaction, and keratin has been applied for biomedical applications and drug delivery. However, few reports have focused on the keratin-based mucoadhesive drug delivery system and their mechanisms of mucoadhesion. Thus, the mucoadhesion controlled kerateine (reduced keratin, KTN)/keratose (oxidized keratin, KOS) composite nanoparticles were prepared via adjusting the proportion of KTN and KOS to achieve controlled gastric mucoadhesion and drug release based on their different mucoadhesive abilities and pH-sensitive properties. Furthermore, the mechanisms of mucoadhesion for KTN and KOS were also investigated in the present study.ResultsThe composite keratin nanoparticles (KNPs) with different mass ratio of KTN to KOS, including 100/0 (KNP-1), 75/25 (KNP-2), 50/50 (KNP-3), and 25/75 (KNP-4), displayed different drug release rates and gastric mucoadhesion capacities, and then altered the drug pharmacokinetic performances. The stronger mucoadhesive ability of nanoparticle could supply longer gastric retention time, indicating that KTN displayed a stronger mucoadhesion than that of KOS. Furthermore, the mechanisms of mucoadhesion for KTN and KOS at different pH conditions were also investigated. The binding between KTN and porcine gastric mucin (PGM) is dominated by electrostatic attractions and hydrogen bondings at pH 4.5, and disulfide bonds also plays a key role in the interaction at pH 7.4. While, the main mechanisms of KOS and PGM interactions are hydrogen bondings and hydrophobic interactions in pH 7.4 condition and were hydrogen bondings at pH 4.5.ConclusionsThe resulting knowledge offer an efficient strategy to control the gastric mucoadhesion and drug release of nano drug delivery systems, and the elaboration of mucoadhesive mechanism of keratins will enable the rational design of nanocarriers for specific mucoadhesive drug delivery.Electronic supplementary materialThe online version of this article (10.1186/s12951-018-0353-2) contains supplementary material, which is available to authorized users.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Development of keratin nanoparticles for controlled gastric mucoadhesion and drug release

et al. 2018

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“…Mucin solution (2 mg/mL) was mixed with chitosan glutamate coated niosome (CG-Nio) and pentamidine entrapped chitosan glutamate coated niosome (CG-NioP) suspensions (1:1 ratio), respectively, and incubated at 30 °C [ 23 , 25 ]. The concentration of mucin solution used in this study was modified to obtain optimal pH value (6.3–6.7) [ 23 , 26 ]. Particle size and ζ-potential were measured by DLS (Nano ZS90, Malvern, UK) at 0, 5, 10, and 15 min, to determine the time needed for niosome–mucin complex formation and the stability of the complex.…”

Section: Methodsmentioning

confidence: 99%

Chitosan Glutamate-Coated Niosomes: A Proposal for Nose-to-Brain Delivery

et al. 2018

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The aim of this in vitro study is to prepare and characterize drug free and pentamidine loaded chitosan glutamate coated niosomes for intranasal drug delivery to reach the brain through intranasal delivery. Mucoadhesive properties and stability testing in various environments were evaluated to examine the potential of these formulations to be effective drug delivery vehicles for intranasal delivery to the brain. Samples were prepared using thin film hydration method. Changes in size and ζ-potential of coated and uncoated niosomes with and without loading of pentamidine in various conditions were assessed by dynamic light scattering (DLS), while size and morphology were also studied by atomic force microscopy (AFM). Bilayer properties and mucoadhesive behavior were investigated by fluorescence studies and DLS analyses, respectively. Changes in vesicle size and ζ-potential values were shown after addition of chitosan glutamate to niosomes, and when in contact with mucin solution. In particular, interactions with mucin were observed in both drug free and pentamidine loaded niosomes regardless of the presence of the coating. The characteristics of the proposed systems, such as pentamidine entrapment and mucin interaction, show promising results to deliver pentamidine or other possible drugs to the brain via nasal administration.

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“…Zeta potential measurements are a common method to investigate the mucoadhesive properties of several biopolymers [31,33]. Mucin has negative charges, with zeta potential of approximately −5 mV, thus the positive surface charges of chitosan-based formulations are expected to interact strongly with mucin (Figure 3).…”

Section: Resultsmentioning

confidence: 99%

Morphological, Mechanical and Mucoadhesive Properties of Electrospun Chitosan/Phospholipid Hybrid Nanofibers

Mendes

Moreno

Hanif

et al. 2018

IJMS

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This study aimed to develop hybrid electrospun chitosan–phospholipid nanofibers and investigate the effect of phospholipid (P) content and chitosans (Ch) molecular weights (Mw) and degree of acetylation (DA), on the morphological, mechanical and mucoadhesive properties of the nanofibers. Electrospun Ch/P nanofibers exhibited a smooth and uniform surface with average diameters ranging from 300 to 1000 nm, as observed by scanning electron microscopy (SEM). The average diameter of the nanofibers was observed to increase with the increase of the Mw and degree of deacetylation of Ch, and phospholipid content. The elastic and adhesive properties of the nanofibers were determined by atomic force microscopy, and displayed higher values for higher Mw and lower DA Ch used. The elastic modulus of electrospun Ch/P hybrid fibers determined for the different conditions tested was found to be in the range of 500 and 1400 MPa. Furthermore, electrospun Ch/P nanofibers displayed mucoadhesive properties expressed by the work of adhesion calculated after the compression of the nanofibers against a section of pig small intestine. Our results showed that the increase in phospholipid content and DA of Ch decrease the work of adhesion, while the increase of Mw resulted in slightly higher work of adhesion of the nanofibers.

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Probing the Mucoadhesive Interactions Between Porcine Gastric Mucin and Some Water‐Soluble Polymers

Cited by 58 publications

References 33 publications

Development of keratin nanoparticles for controlled gastric mucoadhesion and drug release

Development of keratin nanoparticles for controlled gastric mucoadhesion and drug release

Chitosan Glutamate-Coated Niosomes: A Proposal for Nose-to-Brain Delivery

Morphological, Mechanical and Mucoadhesive Properties of Electrospun Chitosan/Phospholipid Hybrid Nanofibers

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