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Chitosan-Based Systems for Pharmaceutical and Nutraceutical Applications

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Materials Science".

Deadline for manuscript submissions: closed (20 June 2020) | Viewed by 29310

Special Issue Editors


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Guest Editor
Department of Pharmacy, University of Pisa, 56126 Pisa, Italy
Interests: controlled drug delivery systems; nanomedicine; nutraceutical products; thermosensitive hydrogels; ocular delivery; oral delivery; multifunctional chitosan derivatives; mucoadhesive nanoparticles
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Department of Pharmacy, University of Pisa, 56126 Pisa, Italy
Interests: mucoadhesive polymeric nanoparticulate systems; ocular and oral administration of drugs; nutraceutic; delivery systems of nutraceutical products; thermosensitive hydrogels; chitosan and its derivatives
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Department of Pharmacy, University of Pisa, 56126 Pisa, Italy
Interests: nanomedicine; drug delivery; pharmaceutics and pharmaceutical technology; polymeric biomaterials; biodegradable polymers
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

It is known that even slight physicochemical differences on the nanoparticle surface are reflected in significant biological differences concerning, e.g., cellular uptake, the biological processes regulating such an uptake, and nanoparticle biodistribution. Together with surface features, nanoparticle size and shape are also known to affect cellular uptake and particle biodistribution. It appears thus to be promising to more deeply investigate and correlate these aspects to be able to modulate and promote selective cellular uptake, thus targeting the site of action, resulting in strong pharmacological activity with low systemic exposure.

Much interest has been focused on nanoparticulate release systems based on chitosan and its derivatives because of their good biocompatibility and effectiveness in releasing macromolecular drugs. The physicochemical surface properties of the nanoparticles based on chitosan conjugates depend on the functional groups that have been substituted on the polymer chains. Alongside the nanoparticles, chitosan and its derivatives are also used to prepare many other innovative release systems. The use of chitosan and its derivatives for the preparation of drug delivery systems will be the focus of the present Special Issue to derive information on the structure–activity relationship.

Prof. Dr. Ylenia Zambito
Dr. Angela Fabiano
Dr. Anna Maria Piras
Guest Editors

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Published Papers (9 papers)

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Research

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16 pages, 2660 KiB  
Article
Modular Chitosan-Based Adsorbents for Tunable Uptake of Sulfate from Water
by Bernd G. K. Steiger and Lee D. Wilson
Int. J. Mol. Sci. 2020, 21(19), 7130; https://doi.org/10.3390/ijms21197130 - 27 Sep 2020
Cited by 21 | Viewed by 3161
Abstract
The context of this study responds to the need for sorbent technology development to address the controlled removal of inorganic sulfate (SO42−) from saline water and the promising potential of chitosan as a carrier system for organosulfates in pharmaceutical and [...] Read more.
The context of this study responds to the need for sorbent technology development to address the controlled removal of inorganic sulfate (SO42−) from saline water and the promising potential of chitosan as a carrier system for organosulfates in pharmaceutical and nutraceutical applications. This study aims to address the controlled removal of sulfate using chitosan as a sustainable biopolymer platform, where a modular synthetic approach was used for chitosan bead preparation that displays tunable sulfate uptake. The beads were prepared via phase-inversion synthesis, followed by cross-linking with glutaraldehyde, and impregnation of Ca2+ ions. The sulfate adsorption properties of the beads were studied at pH 5 and variable sulfate levels (50–1000 ppm), where beads with low cross-linking showed moderate sulfate uptake (35 mg/g), while cross-linked beads imbibed with Ca2+ had greater sulfate adsorption (140 mg/g). Bead stability, adsorption properties, and the point-of-zero charge (PZC) from 6.5 to 6.8 were found to depend on the cross-linking ratio and the presence of Ca2+. The beads were regenerated over multiple adsorption-desorption cycles to demonstrate the favorable uptake properties and bead stability. This study contributes to the development of chitosan-based adsorbent technology via a modular materials design strategy for the controlled removal of sulfate. The results of this study are relevant to diverse pharmaceutical and nutraceutical applications that range from the controlled removal of dextran sulfate from water to the controlled release of chondroitin sulfate. Full article
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19 pages, 3087 KiB  
Article
Development of Biodegradable Whey-Based Laminate Functionalised by Chitosan–Natural Extract Formulations
by Sanja Potrč, Lidija Fras Zemljič, Meta Sterniša, Sonja Smole Možina and Olivija Plohl
Int. J. Mol. Sci. 2020, 21(10), 3668; https://doi.org/10.3390/ijms21103668 - 22 May 2020
Cited by 11 | Viewed by 2833
Abstract
In this research, antimicrobial polysaccharide chitosan and natural extracts were used as surface coating of a plastic laminate with an integrated whey layer on the inside. The aim was to establish the biodegradable and active concept of packaging laminates. For this purpose, chitosan [...] Read more.
In this research, antimicrobial polysaccharide chitosan and natural extracts were used as surface coating of a plastic laminate with an integrated whey layer on the inside. The aim was to establish the biodegradable and active concept of packaging laminates. For this purpose, chitosan nanoparticles (CSNPs) with embedded rosemary or cinnamon extracts were synthesised and characterised. Additionally, a whey-based laminate was functionalised: i) chitosan macromolecular solution was applied as first layer and ii) cinnamon or rosemary extracts encapsulated in CSNPs were applied as upper layer (layer wise deposition). Such functionalised whey-based laminate was physicochemically characterized in terms of elemental surface composition, wettability, morphology and oxygen permeability. The antimicrobial activity was tested against Staphylococcus aureus, Escherichia coli, Aspergillus flavus and Penicillium verrucosum. The antioxidant properties were determined using the ABTS assay. It could be shown that after functionalization of the films with the above-mentioned strategy, the wettability was improved. Furthermore, such whey-based laminates still show excellent barrier properties, good antimicrobial activity and a remarkable antioxidative activity. In addition to the improved biodegradability, this type of lamination could also have a positive effect on the shelf-life of products packaged in such structured films. Full article
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23 pages, 6488 KiB  
Article
Does the Urothelium of Old Mice Regenerate after Chitosan Injury as Quickly as the Urothelium of Young Mice?
by Eva Erzar, Mojca Kerec Kos, Katja Lakota, Peter Veranič and Andreja Erman
Int. J. Mol. Sci. 2020, 21(10), 3502; https://doi.org/10.3390/ijms21103502 - 15 May 2020
Cited by 3 | Viewed by 3149
Abstract
The aging of organisms leads to a decreased ability of tissue to regenerate after injury. The regeneration of the bladder urothelium after induced desquamation with biopolymer chitosan has been studied in young mice but not in old mice. Chitosan is a suitable inducer [...] Read more.
The aging of organisms leads to a decreased ability of tissue to regenerate after injury. The regeneration of the bladder urothelium after induced desquamation with biopolymer chitosan has been studied in young mice but not in old mice. Chitosan is a suitable inducer of urothelial desquamation because it is known to be non-toxic. We used chitosan for desquamation of urothelial cells in order to compare the dynamics of urothelial regeneration after injury between young and old mice. Our aim was to determine whether the urothelial function and structure of old mice is restored as fast as in young mice, and to evaluate the inflammatory response due to chitosan treatment. We discovered that the urothelial function restored comparably fast in both age groups and that the urothelium of young and old mice recovered within 5 days after injury, although the onset of proliferation and differentiation appeared later in old mice. Acute inflammation markers showed some differences in the inflammatory response in young versus old mice, but in both age groups, chitosan caused short-term acute inflammation. In conclusion, the restoration of urothelial function is not impaired in old mice, but the regeneration of the urothelial structure in old mice slightly lags behind the regeneration in young mice. Full article
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13 pages, 1763 KiB  
Article
Nanogels of a Succinylated Glycol Chitosan-Succinyl Prednisolone Conjugate: Release Behavior, Gastrointestinal Distribution, and Systemic Absorption
by Haiyan Zhou, Yuri Ikeuchi-Takahashi, Yoshiyuki Hattori and Hiraku Onishi
Int. J. Mol. Sci. 2020, 21(7), 2376; https://doi.org/10.3390/ijms21072376 - 30 Mar 2020
Cited by 8 | Viewed by 2606
Abstract
Recently, the potential of nanoparticles (NPs) in ulcerative colitis (UC) therapy has been increasingly demonstrated. Namely, anionic NPs have been found to be accumulated efficiently to the UC damaged area due to epithelial enhanced permeability and retention (eEPR) effect. Previously, a novel anionic [...] Read more.
Recently, the potential of nanoparticles (NPs) in ulcerative colitis (UC) therapy has been increasingly demonstrated. Namely, anionic NPs have been found to be accumulated efficiently to the UC damaged area due to epithelial enhanced permeability and retention (eEPR) effect. Previously, a novel anionic nanogel system (NG(S)) was prepared, and evaluated for the efficacy and toxicity. In the present study, release behaviors and biodistribution were investigated in detail to elucidate the functional mechanisms. Rats with 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced ulcerative colitis (UC) were used as biomodels. In vitro release was examined with or without the contents of the cecum or distal colon. Gastrointestinal distribution and plasma concentrations were investigated after the intragastric administration of 10 mg prednisolone (PD) eq./kg. At pH 1.2 and 6.8, release behaviors were slow, but controlled. Overall release was not markedly different irrespective of coexistence of intestinal contents. In in vivo studies, a large amount of PD was distributed in the lower parts of the gastrointestinal tract 6 and 12 h after administration with NG(S). PD accumulated well in the colonic parts, and prolonged release was noted. The systemic absorption of PD with NG(S) was hardly found. NG(S) concentrated the drug in the colon and showed controlled release. These behaviors were considered to lead to the previously reported good results, promotion of effectiveness and suppression of toxic side effects. Full article
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22 pages, 3961 KiB  
Article
Antibacterial, Antibiofilm, and Antiadhesive Properties of Different Quaternized Chitosan Derivatives
by Anna Maria Piras, Semih Esin, Arianna Benedetti, Giuseppantonio Maisetta, Angela Fabiano, Ylenia Zambito and Giovanna Batoni
Int. J. Mol. Sci. 2019, 20(24), 6297; https://doi.org/10.3390/ijms20246297 - 13 Dec 2019
Cited by 39 | Viewed by 3947 | Correction
Abstract
In the era of antimicrobial resistance, the identification of new antimicrobials is a research priority at the global level. In this regard, the attention towards functional antimicrobial polymers, with biomedical/pharmaceutical grade, and exerting anti-infective properties has recently grown. The aim of this study [...] Read more.
In the era of antimicrobial resistance, the identification of new antimicrobials is a research priority at the global level. In this regard, the attention towards functional antimicrobial polymers, with biomedical/pharmaceutical grade, and exerting anti-infective properties has recently grown. The aim of this study was to evaluate the antibacterial, antibiofilm, and antiadhesive properties of a number of quaternized chitosan derivatives that have displayed significant muco-adhesive properties and wound healing promotion features in previous studies. Low (QAL) and high (QAH) molecular weight quaternized chitosan derivatives were synthetized and further modified with thiol moieties or pendant cyclodextrin, and their antibacterial activity evaluated as minimal inhibitory concentrations (MIC) and minimal bactericidal concentrations (MBC). The ability of the derivatives to prevent biofilm formation was assessed by crystal violet staining. Both QAL and QAH derivatives exerted a bactericidal and/or inhibitory activity on the growth of P. aeruginosa and S. epidermidis. The same compounds also showed marked dose-dependent anti-biofilm activity. Furthermore, the high molecular weight derivative (QAH) was used to functionalize titanium plates. The successful functionalization, demonstrated by electron microscopy, was able to partially inhibit the adhesion of S. epidermidis at 6 h of incubation. The shown ability of the chitosan derivatives tested to both inhibit bacterial growth and/or biofilm formation of clinically relevant bacterial species reveals their potential as multifunctional molecules against bacterial infections. Full article
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20 pages, 4668 KiB  
Article
Optimization of ZnAl/Chitosan Supra-Nano Hybrid Preparation as Efficient Antibacterial Material
by Bi Foua Claude Alain Gohi, Hong-Yan Zeng, Sheng Xu, Kai-Min Zou, Binyao Liu, Xiu Li Huang and Xiao-Ju Cao
Int. J. Mol. Sci. 2019, 20(22), 5705; https://doi.org/10.3390/ijms20225705 - 14 Nov 2019
Cited by 9 | Viewed by 2546
Abstract
The menace of antimicrobial resistance continues to increase and hence the need to discover new antibiotics, especially alternative and effective sources such as hybrid organic-inorganic, organic-organic materials, and other combinations. In this study, an antimicrobial hybrid supra-nano material was prepared by the bi-titration [...] Read more.
The menace of antimicrobial resistance continues to increase and hence the need to discover new antibiotics, especially alternative and effective sources such as hybrid organic-inorganic, organic-organic materials, and other combinations. In this study, an antimicrobial hybrid supra-nano material was prepared by the bi-titration synthesis method of chitosan (CS) and ZnAl layered double hydroxide. Fourier-transform infrared spectrometer (FTIR), thermogravimetric and differential thermal gravimetric (TGA/DTG), ultraviolet-visible (UV-Vis), X-ray diffraction (XRD), and scanning electron microscopy (SEM) analyses indicated that the ZnAl/CS hybrid exhibited low crystallinity with high thermal stability. The results of ZnAl/CS characterization showed the characteristic properties of the individual components ZnAl and CS, indicating a successful preparation of the ZnAl/CS hybrid. The antibacterial tests revealed that the ZnAl/CS hybrid possessed an enhanced antimicrobial effect against both Escherichia coli (E. coli, MTCC 739) and Penicilliumcyclopium (P. cyclopium, AS 3.4513). Under the central composite design (CCD) of the response surface methodology (RSM) tool, the parameters of the hybrid synthesis reaction were optimized and the result obtained was as follows: reaction pH was 11.3, reagent Zn/Al ratio was 3.27, and chitosan concentration was 1.07 g/L. After optimization, it was found that the antibacterial activity of ZnAl/CS was strengthened against E. coli as evidenced by a widening of the inhibition zone of about 41.6%. The antibacterial activity of ZnAl/CS was mainly due to the reactivation of the antibacterial activity of CS associated with the release of Zn2+ and Al3+ metal ions in addition to ZnO, Al2O3, and ZnAl2O4 compounds resulting from the method of preparation. Full article
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Review

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25 pages, 3445 KiB  
Review
Quaternary Ammonium Chitosans: The Importance of the Positive Fixed Charge of the Drug Delivery Systems
by Angela Fabiano, Denise Beconcini, Chiara Migone, Anna Maria Piras and Ylenia Zambito
Int. J. Mol. Sci. 2020, 21(18), 6617; https://doi.org/10.3390/ijms21186617 - 10 Sep 2020
Cited by 33 | Viewed by 3936
Abstract
As a natural polysaccharide, chitosan has good biocompatibility, biodegradability and biosecurity. The hydroxyl and amino groups present in its structure make it an extremely versatile and chemically modifiable material. In recent years, various synthetic strategies have been used to modify chitosan, mainly to [...] Read more.
As a natural polysaccharide, chitosan has good biocompatibility, biodegradability and biosecurity. The hydroxyl and amino groups present in its structure make it an extremely versatile and chemically modifiable material. In recent years, various synthetic strategies have been used to modify chitosan, mainly to solve the problem of its insolubility in neutral physiological fluids. Thus, derivatives with negative or positive fixed charge were synthesized and used to prepare innovative drug delivery systems. Positively charged conjugates showed improved properties compared to unmodified chitosan. In this review the main quaternary ammonium derivatives of chitosan will be considered, their preparation and their applications will be described to evaluate the impact of the positive fixed charge on the improvement of the properties of the drug delivery systems based on these polymers. Furthermore, the performances of the proposed systems resulting from in vitro and ex vivo experiments will be taken into consideration, with particular attention to cytotoxicity of systems, and their ability to promote drug absorption. Full article
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23 pages, 1570 KiB  
Review
New Opportunity to Formulate Intranasal Vaccines and Drug Delivery Systems Based on Chitosan
by Roxana Popescu, Mihaela Violeta Ghica, Cristina-Elena Dinu-Pîrvu, Valentina Anuța, Dumitru Lupuliasa and Lăcrămioara Popa
Int. J. Mol. Sci. 2020, 21(14), 5016; https://doi.org/10.3390/ijms21145016 - 16 Jul 2020
Cited by 33 | Viewed by 4778
Abstract
In an attempt to develop drug delivery systems that bypass the blood–brain barrier (BBB) and prevent liver and intestinal degradation, it was concluded that nasal medication meets these criteria and can be used for drugs that have these drawbacks. The aim of this [...] Read more.
In an attempt to develop drug delivery systems that bypass the blood–brain barrier (BBB) and prevent liver and intestinal degradation, it was concluded that nasal medication meets these criteria and can be used for drugs that have these drawbacks. The aim of this review is to present the influence of the properties of chitosan and its derivatives (mucoadhesion, permeability enhancement, surface tension, and zeta potential) on the development of suitable nasal drug delivery systems and on the nasal bioavailability of various active pharmaceutical ingredients. Interactions between chitosan and proteins, lipids, antigens, and other molecules lead to complexes that have their own applications or to changing characteristics of the substances involved in the bond (conformational changes, increased stability or solubility, etc.). Chitosan and its derivatives have their own actions (antibacterial, antifungal, immunostimulant, antioxidant, etc.) and can be used as such or in combination with other molecules from the same class to achieve a synergistic effect. The applicability of the properties is set out in the second part of the paper, where nasal formulations based on chitosan are described (vaccines, hydrogels, nanoparticles, nanostructured lipid carriers (NLC), powders, emulsions, etc.). Full article
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Other

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1 pages, 163 KiB  
Correction
Correction: Piras, A.M., et al. Antibacterial, Antibiofilm, and Antiadhesive Properties of Different Quaternized Chitosan Derivatives. Int. J. Mol. Sci. 2019, 20, 6297
by Anna Maria Piras, Semih Esin, Arianna Benedetti, Giuseppantonio Maisetta, Angela Fabiano, Ylenia Zambito and Giovanna Batoni
Int. J. Mol. Sci. 2021, 22(5), 2511; https://doi.org/10.3390/ijms22052511 - 3 Mar 2021
Viewed by 1630
Abstract
The authors wish to make the following corrections to this paper [...] Full article
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