Chitosan and Chitosan Derivatives in Biomedical Applications

A special issue of Polymers (ISSN 2073-4360). This special issue belongs to the section "Biomacromolecules, Biobased and Biodegradable Polymers".

Deadline for manuscript submissions: closed (30 September 2021) | Viewed by 57131

Special Issue Editor


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Guest Editor
Department of Drug Sciences, University of Pavia, Viale Taramelli, 12, 27100 Pavia PV, Italy
Interests: Rheology; electrospun fibers; in situ gelling systems; lipid and polymeric nanoparticles; wound dressings; nervous tissue repair

Special Issue Information

Dear Colleagues,

In the last few decades, chitosan and its derivatives have received considerable attention in the biomedical field.

Chitosan is a cationic polysaccharide that is obtained by the deacetylation of chitin, which represents the main component of the exoskeleton of arthropods, such as crustaceans, molluscs and insects, as well as the cell walls of bacteria and fungi. Its polycationic character determines its unique bioactive properties, which make chitosan a multifunctional excipient for the preparation of innovative drug delivery systems and scaffolds for tissue engineering purposes, comprising hydrogels, sponge-like dressings, films, and nanosystems (nanoparticles, nanocomposites, and nanofibers).

The Food and Drug Administration (FDA) approved the use of chitosan in several biomedical applications thanks to its well-known biocompatibility, nontoxicity, and biodegradability. Due to its mucoadhesive, hemostatic, and antimicrobial properties, chitosan has proven to be an effective healing enhancer, being involved in all stages of the wound-healing process. Moreover, it has been demonstrated that chitosan enhances drug penetration towards different biological membranes, such as intestinal, nasal, buccal, vaginal mucosae, and cornea, thus improving drug bioavailability.

A large family of chitosan derivatives has been produced in order to overcome some limitations of chitosan. Since chitosan is characterized by poor solubility in physiological media, the use of water-soluble derivatives, obtained through different chemical modifications, is preferable in the biomedical and pharmaceutical fields. In this perspective, chitosan chains can be modified at three reactive sites, which are two hydroxyl groups and one primary amino residue, producing CS derivatives with peculiar bulk properties. Among them, trimethyl–chitosan, carboxymethyl–chitosan, and carboxymethyl–trimethyl–chitosan have been investigated recently: They are characterized by an increased water solubility over a wide range of pH and maintain bioactive properties of pure chitosan. In an attempt to improve the antibacterial potential of chitosan, the functionalization of its backbone with chemotherapeutic agents, such as sulfonamides and derivatives, has been also proposed.

The present Special Issue on “Chitosan and Chitosan Derivatives in Biomedical Applications” serves as an overview of current research on this interesting topic, highlighting the progress in the design and development of novel drug delivery systems or tissue engineered products based on chitosan and chitosan derivatives.

Dr. Barbara Vigani
Guest Editor

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Keywords

  • chitosan
  • chitosan derivatives
  • drug delivery systems
  • scaffolds
  • tissue engineering
  • wound healing
  • mucoadhesion
  • antimicrobial properties
  • penetration enhancement

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Published Papers (17 papers)

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19 pages, 3225 KiB  
Article
Cytotoxicity Enhancement in MCF-7 Breast Cancer Cells with Depolymerized Chitosan Delivery of α-Mangostin
by Yedi Herdiana, Nasrul Wathoni, Shaharum Shamsuddin and Muchtaridi Muchtaridi
Polymers 2022, 14(15), 3139; https://doi.org/10.3390/polym14153139 - 01 Aug 2022
Cited by 9 | Viewed by 1785
Abstract
The application of α-mangostin (AMG) in breast cancer research has wide intentions. Chitosan-based nanoparticles (CSNPs) have attractive prospects for developing anticancer drugs, especially in their high flexibility for modification to enhance their anticancer action. This research aimed to study the impact of depolymerized [...] Read more.
The application of α-mangostin (AMG) in breast cancer research has wide intentions. Chitosan-based nanoparticles (CSNPs) have attractive prospects for developing anticancer drugs, especially in their high flexibility for modification to enhance their anticancer action. This research aimed to study the impact of depolymerized chitosan (CS) on the cytotoxicity enhancement of AMG in MCF-7 breast cancer cells. CSNPs effectivity depends on size, shape, crystallinity degree, and charge surface. Modifying CS molecular weight (MW) is expected to influence CSNPs’ characteristics, impacting size, shape, crystallinity degree, and charge surface. CSNPs are developed using the method of ionic gelation with sodium tripolyphosphate (TPP) as a crosslinker and spray pyrolysis procedure. Nanoparticles’ (NPs) sizes vary from 205.3 ± 81 nm to 450.9 ± 235 nm, ZP charges range from +10.56 mV to +51.56 mV, and entrapment efficiency from 85.35% to 90.45%. The morphology of NPs are all the same spherical forms. In vitro release studies confirmed that AMG–Chitosan–High Molecular Weight (AMG–CS–HMW) and AMG–Chitosan–Low Molecular Weight (AMG–CS–LMW) had a sustained-release system profile. MW has a great influence on surface, drug release, and cytotoxicity enhancement of AMG in CSNPs to MCF-7 cancer cells. The preparations AMG–CS–HMW and AMG–CS–LMW NPs considerably enhanced the cytotoxicity of MCF-7 cells with IC50 values of 5.90 ± 0.08 µg/mL and 4.90 ± 0.16 µg/mL, respectively, as compared with the non-nano particle formulation with an IC50 of 8.47 ± 0.29 µg/mL. These findings suggest that CSNPs can enhance the physicochemical characteristics and cytotoxicity of AMG in breast cancer treatment. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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18 pages, 3123 KiB  
Article
Lornoxicam-Loaded Chitosan-Decorated Nanoemulsion: Preparation and In Vitro Evaluation for Enhanced Transdermal Delivery
by Rahman Ullah Khan, Shefaat Ullah Shah, Sheikh Abdur Rashid, Faiza Naseem, Kifayat Ullah Shah, Arshad Farid, Khalid Rehman Hakeem, Majid Rasool Kamli, Eman Hillal Althubaiti and Soha A. Alamoudi
Polymers 2022, 14(9), 1922; https://doi.org/10.3390/polym14091922 - 09 May 2022
Cited by 13 | Viewed by 2239
Abstract
Nanoemulsions are promising drug delivery systems for the administration of poorly soluble drugs like lornoxicam (LRX) by oral or parenteral routes. Such formulations work perfectly for transdermal delivery of lornoxicam-type drugs. It has also been established that formulating such a delivery system is [...] Read more.
Nanoemulsions are promising drug delivery systems for the administration of poorly soluble drugs like lornoxicam (LRX) by oral or parenteral routes. Such formulations work perfectly for transdermal delivery of lornoxicam-type drugs. It has also been established that formulating such a delivery system is highly dependent on the presence, type, and concentration of excipients taking part in the formulation. The inherent characteristics of nanoemulsion (NE), i.e., smaller globule size and excipient nature, facilitate the drug’s passage through skin. The current study was aimed at the development of an NE-based formulation of LRX to improve the drug solubility in vitro as well as to enhance drug skin permeation to promote therapeutic outcome in appropriate time. Spontaneous self-emulsification technique was utilized to develop optimized LRX-encapsulated NE-based formulations. ATR-FTIR spectra of the pure drug and various formulations did not show any interaction between the drug and various formulation excipients showing compatibility. Globule size for stable formulations ranged between 63–168 nm. These formulations were characterized for viscosity, surface tension, pH, drug encapsulation efficiency, in vitro drug release, and drug skin permeation studies. Chitosan-decorated optimized NE formulation of LRX showed about 58.82% cumulative drug release, showing an anomalous non-Fickian diffusion mechanism of drug release. Drug encapsulation efficiency, in vitro drug release, and skin permeation studies exhibited promising results. An appreciable drug entrapment efficiency was exhibited by optimized NE formulations LRX-6, 71.91 ± 3.17% and C-LRX, 65.25 ± 4.89%. Permeability parameters like enhancement ratio (Er), permeability constant (Kp), and steady state flux (Jss) showed higher values and exhibited good results based on formulation type. The selected promising formulation type “LRX-6” showed significantly different results as compared to other formulations (LRX-4, 5, and 7). The skin permeation property of the LRX-6 formulation was compared to similar chitosan-based formulations and was found to have better skin permeation results than chitosan-based formulations. This study clearly exhibited that an LRX-containing NE-based formulation can be formulated to form a stable drug delivery system. Such formulations are promising in terms of physicochemical characteristics, improved solubility, and high skin permeation potential. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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22 pages, 7405 KiB  
Article
Efficacy of Chitosan Nanoparticle Loaded-Salicylic Acid and -Silver on Management of Cassava Leaf Spot Disease
by Nguyen Huy Hoang, Toan Le Thanh, Wannaporn Thepbandit, Jongjit Treekoon, Chanon Saengchan, Rungthip Sangpueak, Narendra Kumar Papathoti, Anyanee Kamkaew and Natthiya Buensanteai
Polymers 2022, 14(4), 660; https://doi.org/10.3390/polym14040660 - 09 Feb 2022
Cited by 9 | Viewed by 3087
Abstract
Leaf spot is one of the most important cassava diseases. Nanotechnology can be applied to control diseases and improve plant growth. This study was performed to prepare chitosan (CS) nanoparticle (NP)-loaded salicylic acid (SA) or silver (Ag) by the ionic gelation method, and [...] Read more.
Leaf spot is one of the most important cassava diseases. Nanotechnology can be applied to control diseases and improve plant growth. This study was performed to prepare chitosan (CS) nanoparticle (NP)-loaded salicylic acid (SA) or silver (Ag) by the ionic gelation method, and to evaluate their effectiveness on reducing leaf spot disease and enhancing the growth of cassava plants. The CS (0.4 or 0.5%) and Pentasodium triphosphate (0.2 or 0.5%) were mixed with SA varying at 0.05, 0.1, or 0.2% or silver nitrate varying at 1, 2, or 3 mM to prepare three formulations of CS-NP-loaded SA named N1, N2, and N3 or CS-NP-loaded Ag named N4, N5, and N6. The results showed that the six formulations were not toxic to cassava leaves up to 800 ppm. The CS-NP-loaded SA (N3) and CS-NP-loaded Ag (N6) were more effective than the remaining formulations in reducing the disease severity and the disease index of leaf spot. Furthermore, N3 at 400 ppm and N6 at 200, 400, and 800 ppm could reduce disease severity (68.9–73.6% or 37.0–37.7%, depending on the time of treatment and the pathogen density) and enhance plant growth more than or equal to commercial fungicide or nano-fungicide products under net-house conditions. The study indicates the potential to use CS-NP-loaded SA or Ag as elicitors to manage cassava leaf spot disease. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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15 pages, 4620 KiB  
Article
Drug Delivery from Stimuli-Responsive Poly(N-isopropylacrylamide-co-N-isopropylmethacrylamide)/Chitosan Core/Shell Nanohydrogels
by Andrés Ortega-García, Bryan Giovanny Martínez-Bernal, Israel Ceja, Eduardo Mendizábal, Jorge Emilio Puig-Arévalo and Lourdes Adriana Pérez-Carrillo
Polymers 2022, 14(3), 522; https://doi.org/10.3390/polym14030522 - 27 Jan 2022
Cited by 7 | Viewed by 2632
Abstract
The synthesis of stimulus-responsive poly(N-isopropylacrylamide-co-N-isopropylmethacrylamide)/chitosan core/shell nanohydrogels made by batch emulsion polymerization in the presence of chitosan (CS) micelles is reported. The ratio of monomers required to obtain copolymers with a volume phase transition temperature (TVPT) in the range of the [...] Read more.
The synthesis of stimulus-responsive poly(N-isopropylacrylamide-co-N-isopropylmethacrylamide)/chitosan core/shell nanohydrogels made by batch emulsion polymerization in the presence of chitosan (CS) micelles is reported. The ratio of monomers required to obtain copolymers with a volume phase transition temperature (TVPT) in the range of the temperatures observed in the human body in response to an infection (38 to 40 °C) was estimated with the Fox equation. The conversion was determined by gravimetry; mean particle size, size distribution, and thermal response were measured by quasi-elastic light scattering (QLS). The core/shell structure was confirmed by TEM, and FTIR showed the presence of N-isopropyl acrilamide (NIPA), N-isopropyl methacrylamide (NIPMA), and CS in the nanohydrogels. The nanohydrogels were loaded with the drug doxycycline hyclate, and their release kinetic profile was determined at pH = 2.0 and 7.4 at their volume phase transition temperatures (TVPT). A higher amount of drug was released at acidic pH. Some mathematical models described in the literature were used to fit the experimental drug release data. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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21 pages, 10251 KiB  
Article
Chitosan/Polyvinyl Alcohol/Tea Tree Essential Oil Composite Films for Biomedical Applications
by Jorge Iván Castro, Carlos Humberto Valencia-Llano, Mayra Eliana Valencia Zapata, Yilmar Joan Restrepo, José Herminsul Mina Hernandez, Diana Paola Navia-Porras, Yamid Valencia, Cesar Valencia and Carlos David Grande-Tovar
Polymers 2021, 13(21), 3753; https://doi.org/10.3390/polym13213753 - 29 Oct 2021
Cited by 20 | Viewed by 3283
Abstract
Tissue engineering is crucial, since its early adoption focused on designing biocompatible materials that stimulate cell adhesion and proliferation. In this sense, scaffolds made of biocompatible and resistant materials became the researchers’ focus on biomedical applications. Humans have used essential oils for a [...] Read more.
Tissue engineering is crucial, since its early adoption focused on designing biocompatible materials that stimulate cell adhesion and proliferation. In this sense, scaffolds made of biocompatible and resistant materials became the researchers’ focus on biomedical applications. Humans have used essential oils for a long time to take advantage of their antifungal, insecticide, antibacterial, and antioxidant properties. However, the literature demonstrating the use of essential oils for stimulating biocompatibility in new scaffold designs is scarce. For that reason, this work describes the synthesis of four different film composites of chitosan/polyvinyl alcohol/tea tree (Melaleuca alternifolia), essential oil (CS/PVA/TTEO), and the subdermal implantations after 90 days in Wistar rats. According to the Young modulus, DSC, TGA, mechanical studies, and thermal studies, there was a reinforcement effect with the addition of TTEO. Morphology and energy-dispersive (EDX) analysis after the immersion in simulated body fluid (SBF) exhibited a light layer of calcium chloride and sodium chloride generated on the material’s surface, which is generally related to a bioactive material. Finally, the biocompatibility of the films was comparable with porcine collagen, showing better signs of resorption as the amount of TTEO was increased. These results indicate the potential application of the films in long-term biomedical needs. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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17 pages, 2947 KiB  
Article
An Engineered Specificity of Anti-Neoplastic Agent Loaded Magnetic Nanoparticles for the Treatment of Breast Cancer
by Anroop B. Nair, Mallikarjun Telsang and Riyaz Ali Osmani
Polymers 2021, 13(21), 3623; https://doi.org/10.3390/polym13213623 - 20 Oct 2021
Cited by 3 | Viewed by 1621
Abstract
Nanoparticles have gained increased attention due to the prospection of drug delivery at target sites, thus limiting the systemic effects of the drugs. Their efficiency was further improved by adding special carriers such as magnetite (Fe3O4). It is one [...] Read more.
Nanoparticles have gained increased attention due to the prospection of drug delivery at target sites, thus limiting the systemic effects of the drugs. Their efficiency was further improved by adding special carriers such as magnetite (Fe3O4). It is one of the extensively used oxides of iron for both pharmaceutical and biomedical applications owing to its ease of preparation and biocompatibility. In this work, Gemcitabine magnetic nanoparticles were prepared using Fe3O4 and chitosan as the primary ingredients. Optimization was accomplished by Box–Behnken Design and factor interactions were evaluated. The desirability function approach was made to enhance the formulation concerning particle size, polydispersity index, and zeta potential. Based on this, optimized magnetic nanoparticles (O-MNP) were formulated with 300 mg of Fe3O4, 297.7 mg of chitosan, and a sonication time of 2.4 h, which can achieve the prerequisites of the target formulation. All other in vitro parameters were found to be following the requirement. In vitro cytotoxic studies for O-MNP were performed using cell cultures of breast cancer (MCF-7), leukemia (THP-1), prostate cancer (PC-3), and lung cancer (A549). O-MNP showed maximum inhibition growth with MCF-7 cell lines rather than other cell lines. The data observed here demonstrates the potential of magnetic nanoparticles of gemcitabine in treating breast cancers. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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17 pages, 4678 KiB  
Article
Development of pH-Sensitive Chitosan-g-poly(acrylamide-co-acrylic acid) Hydrogel for Controlled Drug Delivery of Tenofovir Disoproxil Fumarate
by Justin B. Safari, Alain M. Bapolisi and Rui W. M. Krause
Polymers 2021, 13(20), 3571; https://doi.org/10.3390/polym13203571 - 16 Oct 2021
Cited by 12 | Viewed by 3298
Abstract
The present study aimed to develop a pH-sensitive chitosan-based hydrogel for controlled delivery of an anti-hepatitis B drug, tenofovir disoproxil fumarate (TDF). Free radical polymerization was utilized to graft acrylamide and acrylic acid using N,N-methylene bisacrylamide as the crosslinker. Physicochemical [...] Read more.
The present study aimed to develop a pH-sensitive chitosan-based hydrogel for controlled delivery of an anti-hepatitis B drug, tenofovir disoproxil fumarate (TDF). Free radical polymerization was utilized to graft acrylamide and acrylic acid using N,N-methylene bisacrylamide as the crosslinker. Physicochemical characterization confirmed the synthesis of thermally stable chitosan-g-poly(acrylamide-co-acrylic acid) hydrogels with well-defined pores within a fibrous surface. The prepared hydrogels exhibited pH and ionic strength sensitivity, with the swelling significantly lower under acidic and strong ionic strength conditions but higher in neutral and basic solutions. In addition, cytotoxicity studies on HeLa cell lines proved the cytocompatibility of the drug delivery material and its readiness for physiological applications. The encapsulation of TDF in the hydrogels was optimized and an encapsulation efficiency and a drug loading percentage of 96% and 10% were achieved, respectively. More interestingly, in vitro release studies demonstrated a pH-dependent release of TDF from hydrogels. The release at pH 7.4 was found to be up to five times higher than at pH 1.2 within 96 h. This further suggested that the newly developed hydrogel-loaded TDF could be proposed as a smart delivery system for oral delivery of anti-hepatitis B drugs. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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16 pages, 5116 KiB  
Article
Chitosan-Coated Poly(lactic acid) Nanofibres Loaded with Essential Oils for Wound Healing
by Giulia Milanesi, Barbara Vigani, Silvia Rossi, Giuseppina Sandri and Elisa Mele
Polymers 2021, 13(16), 2582; https://doi.org/10.3390/polym13162582 - 04 Aug 2021
Cited by 24 | Viewed by 3382
Abstract
Chronic skin wounds are characterised by a non-healing process that makes necessary the application of wound dressings on the damaged area to promote and facilitate the recovery of skin’s physiological integrity. The aim of the present work is to develop a bioactive dressing [...] Read more.
Chronic skin wounds are characterised by a non-healing process that makes necessary the application of wound dressings on the damaged area to promote and facilitate the recovery of skin’s physiological integrity. The aim of the present work is to develop a bioactive dressing that, once applied on the injured tissue, would exert antibacterial activity and promote adhesion and proliferation of fibroblasts. Nanofibres consisting of poly(lactic acid) (PLA) and essential oils (EOs) were electrospun and coated with a medium molecular weight chitosan (CS). Black pepper essential oil (BP-EO) or limonene (L), well-known for their antibacterial properties, were added to the PLA/acetone solution before electrospinning; phase separation phenomena occurred due to the poor solubility of the EOs in the PLA solution and led to fibres having surface nano-pores. The porous electrospun fibres were coated with CS to produce hydrophilic membranes that were easy to handle, biocompatible, and suited to promote cellular proliferation. The fibrous scaffolds were tested in terms of mechanical resistance, wettability, antibacterial activity, in-vitro cytotoxicity, and ability to promote fibroblasts’ adhesion and proliferation. The results obtained proved that the CS coating improved the hydrophilicity of the fibrous mats, enhanced EO’s antibacterial potential, and promoted cell adhesion and proliferation. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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20 pages, 3839 KiB  
Article
Formulation and Antibacterial Activity Evaluation of Quaternized Aminochitosan Membrane for Wound Dressing Applications
by Ahmed M. Omer, Tamer M. Tamer, Randa E. Khalifa, Abdelazeem S. Eltaweil, Mona M. Agwa, Sally Sabra, Mahmoud S. Abd-Elmonem, Mohamed S. Mohy-Eldin and Zyta M. Ziora
Polymers 2021, 13(15), 2428; https://doi.org/10.3390/polym13152428 - 23 Jul 2021
Cited by 22 | Viewed by 2592
Abstract
Much attention has been paid to chitosan biopolymer for advanced wound dressing owing to its exceptional biological characteristics comprising biodegradability, biocompatibility and respectable antibacterial activity. This study intended to develop a new antibacterial membrane based on quaternized aminochitosan (QAMCS) derivative. Herein, aminochitosan (AMCS) [...] Read more.
Much attention has been paid to chitosan biopolymer for advanced wound dressing owing to its exceptional biological characteristics comprising biodegradability, biocompatibility and respectable antibacterial activity. This study intended to develop a new antibacterial membrane based on quaternized aminochitosan (QAMCS) derivative. Herein, aminochitosan (AMCS) derivative was quaternized by N-(2-Chloroethyl) dimethylamine hydrochloride with different ratios. The pre-fabricated membranes were characterized by several analysis tools. The results indicate that maximum surface potential of +42.2 mV was attained by QAMCS3 membrane compared with +33.6 mV for native AMCS membrane. Moreover, membranes displayed higher surface roughness (1.27 ± 0.24 μm) and higher water uptake value (237 ± 8%) for QAMCS3 compared with 0.81 ± 0.08 μm and 165 ± 6% for neat AMCS membranes. Furthermore, the antibacterial activities were evaluated against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus cereus. Superior antibacterial activities with maximum inhibition values of 80–98% were accomplished by QAMCS3 membranes compared with 57–72% for AMCS membrane. Minimum inhibition concentration (MIC) results denote that the antibacterial activities were significantly boosted with increasing of polymeric sample concentration from 25 to 250 µg/mL. Additionally, all membranes unveiled better biocompatibility and respectable biodegradability, suggesting their possible application for advanced wound dressing. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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12 pages, 2731 KiB  
Article
Hemostatic Patches Based on Crosslinked Chitosan Films Applied in Interventional Procedures
by Moon Hyun Lee, Dae Ryeong Lee, Joon Woo Chon and Dong June Chung
Polymers 2021, 13(15), 2402; https://doi.org/10.3390/polym13152402 - 22 Jul 2021
Cited by 6 | Viewed by 2100
Abstract
In this study, we manufactured biocompatible hemostatic crosslinked chitosan (CS) patches and analyzed their physicochemical and biological properties for femoral arterial puncture applications. CS is a representative hemostatic material but has some drawbacks, such as swelling, shrinkage, and brittleness. Thus, it was crosslinked [...] Read more.
In this study, we manufactured biocompatible hemostatic crosslinked chitosan (CS) patches and analyzed their physicochemical and biological properties for femoral arterial puncture applications. CS is a representative hemostatic material but has some drawbacks, such as swelling, shrinkage, and brittleness. Thus, it was crosslinked via a 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide (EDC)/N-hydroxysuccinimide (NHS) coupling reaction and a nucleophilic addition reaction with citric acid (CA), glutaraldehyde (GTA), and genipin (GP) to remedy its shortcomings. The CSCA (crosslinked CS with CA/EDC), CSGTA (crosslinked CS with GTA), and CSG (crosslinked CS with GP) films showed low swelling degrees and good mechanical properties (excluding CSCA) compared with those of neat CS films. Additionally, every crosslinked CS film coated with thrombin (TB-CS) showed enhanced hemostatic ability in the whole blood clotting and activated partial thromboplastin time tests. Furthermore, the CSCA, CSGTA, and CSGP were nontoxic in an in vitro cell cytotoxicity test (3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide assay) using L-929 mouse fibroblasts cells. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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13 pages, 2009 KiB  
Article
The Potential Cytotoxic Activity Enhancement of α-Mangostin in Chitosan-Kappa Carrageenan-Loaded Nanoparticle against MCF-7 Cell Line
by Nasrul Wathoni, Lisna Meylina, Agus Rusdin, Ahmed Fouad Abdelwahab Mohammed, Dorandani Tirtamie, Yedi Herdiana, Keiichi Motoyama, Camelia Panatarani, I Made Joni, Ronny Lesmana and Muchtaridi Muchtaridi
Polymers 2021, 13(11), 1681; https://doi.org/10.3390/polym13111681 - 21 May 2021
Cited by 17 | Viewed by 3139
Abstract
α-mangostin (αM), a xanthone derivative compound isolated from the extract of mangosteen pericarp (Garcinia mangostana L), has potential anticancer properties for breast cancer. However, it has poor solubility in water and low selectivity towards cancer cells. The polymeric nanoparticle formulation approach can [...] Read more.
α-mangostin (αM), a xanthone derivative compound isolated from the extract of mangosteen pericarp (Garcinia mangostana L), has potential anticancer properties for breast cancer. However, it has poor solubility in water and low selectivity towards cancer cells. The polymeric nanoparticle formulation approach can be used to overcome these problems. In this study, a chitosan biopolymer-based αM polymeric nanoparticle formulation was encapsulated using kappa carrageenan (αM-Ch/Cr) as a novel carrier for breast cancer therapy and evaluated for their physicochemical properties, drug release profile, and in vitro cytotoxicity against breast cancer cells (MCF-7). Polymeric nanoparticles formulated with varying concentrations of kappa carrageenan were successfully prepared by ionic gelation and spray pyrolysis techniques. αM-Ch/Cr nanoparticles formed perfectly round particles with a size of 200–400 nm and entrapment efficiency ≥ 98%. In vitro release studies confirmed that αM-Ch/Cr nanoparticles had a sustained release system profile. Interestingly, the formulation of polymeric nanoparticles significantly (p < 0.05) increased the cytotoxicity of αM against MCF-7 cell with IC50 value of 4.7 μg/mL compared to the non-nanoparticle with IC50 of 8.2 μg/mL. These results indicate that αM-Ch/Cr nanoparticles have the potential to improve the physicochemical properties and cytotoxicity effects of αM compounds as breast cancer therapy agents. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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16 pages, 3676 KiB  
Article
A Composite Nanosystem as a Potential Tool for the Local Treatment of Glioblastoma: Chitosan-Coated Solid Lipid Nanoparticles Embedded in Electrospun Nanofibers
by Barbara Vigani, Caterina Valentino, Giuseppina Sandri, Roberta Listro, Francesca Fagiani, Simona Collina, Cristina Lanni, Maria Cristina Bonferoni, Carla M. Caramella, Silvia Rossi and Franca Ferrari
Polymers 2021, 13(9), 1371; https://doi.org/10.3390/polym13091371 - 22 Apr 2021
Cited by 13 | Viewed by 2655
Abstract
Glioblastoma multiforme (GBM) is one of the most prevalent and aggressive brain tumors for which there is currently no cure. A novel composite nanosystem (CN), consisting of chitosan-coated Solid Lipid Nanoparticles (c-SLN) embedded in O-carboxymethyl chitosan (O-CMCS)-containing nanofibers (NFs), was proposed as a [...] Read more.
Glioblastoma multiforme (GBM) is one of the most prevalent and aggressive brain tumors for which there is currently no cure. A novel composite nanosystem (CN), consisting of chitosan-coated Solid Lipid Nanoparticles (c-SLN) embedded in O-carboxymethyl chitosan (O-CMCS)-containing nanofibers (NFs), was proposed as a potential tool for the local delivery of lipophilic anti-proliferative drugs. Coacervation was selected as a solvent-free method for the preparation of stearic acid (SA) and behenic acid (BA)-based SLN (SA-SLN and BA-SLN respectively). BA-SLN, containing 0.75% w/w BA sodium salt and 3% w/w poly(vinyl alcohol) (PVA), were selected for the prosecution of the work since they are characterized by the lowest size functional to their subsequent coating and incorporation in nanofibers. BA-SLN were coated with chitosan (CS) by means of a two-step coating method based on the physical absorption of positively charged CS chains on the SLN negative surface. Nile Red (NR), chosen as the hydrophobic model dye, was dissolved in a micellar solution of BA sodium salt and then added with a coacervating solution until pH ≅ 2.5 was reached. Immunocytochemistry analyses highlighted that CS-coated BA-SLN (c-BA-SLN) exhibited a higher accumulation in human glioblastoma cells (U-373) after 6 h than CS-free BA-SLN. Finally, the c-BA-SLN dispersion was blended with a solution consisting of freely soluble polymers (O-CMCS, poly(ethylene oxide) and poloxamer) and then electrospun to obtain NFs with a mean diameter equal to 850 nm. After the NFs dissolution in an aqueous media, c-BA-SLN maintained their physicochemical properties and zeta potential. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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10 pages, 6681 KiB  
Article
Magnetic Resonance Imaging of Transplanted Porcine Neonatal Pancreatic Cell Clusters Labeled with Chitosan-Coated Superparamagnetic Iron Oxide Nanoparticles in Mice
by Jyuhn-Huarng Juang, Jiun-Jie Wang, Chia-Rui Shen, Chen-Yi Chen, Chen-Wei Kao, Chen-Ling Chen, Sung-Han Lin, Shu-Ting Wu, Wan-Chun Li and Zei-Tsan Tsai
Polymers 2021, 13(8), 1238; https://doi.org/10.3390/polym13081238 - 11 Apr 2021
Cited by 6 | Viewed by 2095
Abstract
Neonatal pancreatic cell clusters (NPCCs) are potential tissues for the treatment of diabetes. Different from adult cells, they continuously proliferate and differentiate after transplantation. In this study, we utilized magnetic resonance imaging (MRI) to detect and monitor implanted NPCCs. NPCCs were isolated from [...] Read more.
Neonatal pancreatic cell clusters (NPCCs) are potential tissues for the treatment of diabetes. Different from adult cells, they continuously proliferate and differentiate after transplantation. In this study, we utilized magnetic resonance imaging (MRI) to detect and monitor implanted NPCCs. NPCCs were isolated from one-day-old neonatal pigs, cultured for three days, and then incubated overnight with the contrast agent chitosan-coated superparamagnetic iron oxide (CSPIO) nanoparticles. In vitro, Prussian blue staining and MR scans of CSPIO-labeled NPCCs were performed. In vivo, we transplanted 2000 CSPIO-labeled NPCCs under the kidney capsule of nondiabetic nude mice. Recipients were scanned with 7.0T MRI. Grafts were removed for histology with insulin and Prussian blue staining. After being incubated overnight with CSPIO, NPCCs showed positive iron staining and appeared as dark spots on MR scans. After transplantation of CSPIO-labeled NPCCs, persistent hypointense areas were observed at recipients’ implant sites for up to 54 days. Moreover, histology showed colocalization of the insulin and iron staining in 15-, 51- and 55-day NPCC grafts. Our results indicate that transplanted NPCCs survived and differentiated to β cells after transplantation, and that MRI is a useful tool for the detection and monitoring of CSPIO-labeled NPCC grafts. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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26 pages, 8572 KiB  
Article
PHB/CHIT Scaffold as a Promising Biopolymer in the Treatment of Osteochondral Defects—An Experimental Animal Study
by Eva Petrovova, Marek Tomco, Katarina Holovska, Jan Danko, Lenka Kresakova, Katarina Vdoviakova, Veronika Simaiova, Filip Kolvek, Petra Hornakova, Teodor Toth, Jozef Zivcak, Peter Gal, David Sedmera, Lenka Luptakova and Lubomir Medvecky
Polymers 2021, 13(8), 1232; https://doi.org/10.3390/polym13081232 - 11 Apr 2021
Cited by 10 | Viewed by 3080
Abstract
Biopolymer composites allow the creation of an optimal environment for the regeneration of chondral and osteochondral defects of articular cartilage, where natural regeneration potential is limited. In this experimental study, we used the sheep animal model for the creation of knee cartilage defects. [...] Read more.
Biopolymer composites allow the creation of an optimal environment for the regeneration of chondral and osteochondral defects of articular cartilage, where natural regeneration potential is limited. In this experimental study, we used the sheep animal model for the creation of knee cartilage defects. In the medial part of the trochlea and on the medial condyle of the femur, we created artificial defects (6 × 3 mm2) with microfractures. In four experimental sheep, both defects were subsequently filled with the porous acellular polyhydroxybutyrate/chitosan (PHB/CHIT)-based implant. Two sheep had untreated defects. We evaluated the quality of the newly formed tissue in the femoral trochlea defect site using imaging (X-ray, Computer Tomography (CT), Magnetic Resonance Imaging (MRI)), macroscopic, and histological methods. Macroscopically, the surface of the treated regenerate corresponded to the niveau of the surrounding cartilage. X-ray examination 6 months after the implantation confirmed the restoration of the contour in the subchondral calcified layer and the advanced rate of bone tissue integration. The CT scan revealed a low regenerative potential in the bone zone of the defect compared to the cartilage zone. The percentage change in cartilage density at the defect site was not significantly different to the reference area (0.06–6.4%). MRI examination revealed that the healing osteochondral defect was comparable to the intact cartilage signal on the surface of the defect. Hyaline-like cartilage was observed in most of the treated animals, except for one, where the defect was repaired with fibrocartilage. Thus, the acellular, chitosan-based biomaterial is a promising biopolymer composite for the treatment of chondral and osteochondral defects of traumatic character. It has potential for further clinical testing in the orthopedic field, primarily with the combination of supporting factors. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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16 pages, 1483 KiB  
Article
Chitosan Nanocarrier Entrapping Hydrophilic Drugs as Advanced Polymeric System for Dual Pharmaceutical and Cosmeceutical Application: A Comprehensive Analysis Using Box-Behnken Design
by Sara A. Abosabaa, Aliaa N. ElMeshad and Mona G. Arafa
Polymers 2021, 13(5), 677; https://doi.org/10.3390/polym13050677 - 24 Feb 2021
Cited by 23 | Viewed by 2749
Abstract
The objective of the present research is to propose chitosan as a nanocarrier for caffeine—a commonly used drug in combating cellulite. Being a hydrophilic drug, caffeine suffers from insufficient topical penetration upon application on the skin. Chitosan nanoparticles loaded with caffeine were prepared [...] Read more.
The objective of the present research is to propose chitosan as a nanocarrier for caffeine—a commonly used drug in combating cellulite. Being a hydrophilic drug, caffeine suffers from insufficient topical penetration upon application on the skin. Chitosan nanoparticles loaded with caffeine were prepared via the ionic gelation technique and optimized according to a Box–Behnken design. The effect of (A) chitosan concentration, (B) chitosan solution pH, and (C) chitosan to sodium tripolyphosphate mass ratio on (Y1) entrapment efficiency percent, (Y2) particle size, (Y3) polydispersity index, and (Y4) zeta potential were studied. Subsequently, the desired constraints on responses were applied, and validation of the optimization procedure was confirmed by the parameters exhibited by the optimal formulation. A caffeine entrapment efficiency percent of 17.25 ± 1.48%, a particle size of 173.03 ± 4.32 nm, a polydispersity index of 0.278 ± 0.01, and a surface charge of 41.7 ± 3.0 mV were attained. Microscopical evaluation using transmission electron microscope revealed a typical spherical nature of the nanoparticles arranged in a network with a further confirmation of the formation of particles in the nano range. The results proved the successful implementation of the Box–Behnken design for optimization of chitosan-based nanoparticles in the field of advanced polymeric systems for pharmaceutical and cosmeceutical applications. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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15 pages, 3635 KiB  
Article
Gelatin/Chitosan Bilayer Patches Loaded with Cortex Phellodendron amurense/Centella asiatica Extracts for Anti-Acne Application
by Chi-Wen Kuo, Yi-Fang Chiu, Min-Hua Wu, Ming-Hsien Li, Cheng-Nan Wu, Wan-Sin Chen and Chiung-Hua Huang
Polymers 2021, 13(4), 579; https://doi.org/10.3390/polym13040579 - 15 Feb 2021
Cited by 12 | Viewed by 9667
Abstract
Acne is a chronic inflammatory skin disease that often occurs with anaerobic Propionibacterium acnes (P. acnes). Anti-acne patches, made of hydrocolloid or hydrogel, have become a popular way of topical treatment. The outer water-impermeable layer of commercial patches might create hypoxic [...] Read more.
Acne is a chronic inflammatory skin disease that often occurs with anaerobic Propionibacterium acnes (P. acnes). Anti-acne patches, made of hydrocolloid or hydrogel, have become a popular way of topical treatment. The outer water-impermeable layer of commercial patches might create hypoxic conditions and promote P. acnes growth. In this study, gelatin/chitosan (GC) bilayer patches were prepared at different temperatures that included room temperature (RT), −20 °C/RT, and −80 °C/RT. The most promising GC bilayer patch (−80 °C /RT) contained a dense upper layer for protection from bacteria and infection and a porous lower layer for absorbing pus and fluids from pimples. The anti-acne bilayer patch was loaded with Cortex Phellodendri amurensis (PA) and Centella asiatica (CA) extracts. PA extract could inhibit the growth of P. acnes and CA extract was reported to improve wound healing and reduce scar formation. Moreover, the water retention rate, weight loss rate, antibacterial activity, and in vitro cytotoxicity of the patches were investigated. The porous structure of the patches promoted water retention and contributed to absorbing the exudate when used on open acne wounds. The GC bilayer patches loaded with PA/CA extracts were demonstrated to inhibit the growth of P. acnes, and accelerate the skin fibroblast cell viability. Based on their activities and characteristics, the GC bilayer patches with PA/CA extract prepared at −80 °C/RT obtain the potential for the application of acne spot treatment. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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Review

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31 pages, 4931 KiB  
Review
Biomedical Applications of Quaternized Chitosan
by Kamla Pathak, Shashi Kiran Misra, Aayush Sehgal, Sukhbir Singh, Simona Bungau, Agnieszka Najda, Robert Gruszecki and Tapan Behl
Polymers 2021, 13(15), 2514; https://doi.org/10.3390/polym13152514 - 30 Jul 2021
Cited by 53 | Viewed by 5988
Abstract
The natural polymer chitosan is the second most abundant biopolymer on earth after chitin and has been extensively explored for preparation of versatile drug delivery systems. The presence of two distinct reactive functional groups (an amino group at C2, and a primary and [...] Read more.
The natural polymer chitosan is the second most abundant biopolymer on earth after chitin and has been extensively explored for preparation of versatile drug delivery systems. The presence of two distinct reactive functional groups (an amino group at C2, and a primary and secondary hydroxyl group at C3 and C6) of chitosan are involved in the transformation of expedient derivatives such as acylated, alkylated, carboxylated, quaternized and esterified chitosan. Amongst these, quaternized chitosan is preferred in pharmaceutical industries owing to its prominent features including superior water solubility, augmented antimicrobial actions, modified wound healing, pH-sensitive targeting, biocompatibility, and biodegradability. It has been explored in a large realm of pharmaceuticals, cosmeceuticals, and the biomedical arena. Immense classy drug delivery systems containing quaternized chitosan have been intended for tissue engineering, wound healing, gene, and vaccine delivery. This review article outlines synthetic techniques, basic characteristics, inherent properties, biomedical applications, and ubiquitous challenges associated to quaternized chitosan. Full article
(This article belongs to the Special Issue Chitosan and Chitosan Derivatives in Biomedical Applications)
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