Displaying publications 1 - 20 of 23 in total

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  1. Antibacterial activity of chitosan under physiological conditions
    Mai-Ngam K, Chumningan P
    Med J Malaysia, 2004 May;59 Suppl B:137-8.
    PMID: 15468856
    Matched MeSH terms: Chitosan/pharmacology*
  2. A review on chitosan and chitosan-based bionanocomposites: Promising material for combatting global issues and its applications
    Azmana M, Mahmood S, Hilles AR, Rahman A, Arifin MAB, Ahmed S
    Int J Biol Macromol, 2021 Aug 31;185:832-848.
    PMID: 34237361 DOI: 10.1016/j.ijbiomac.2021.07.023
    Over the last few years, several attempts have been made to replace petrochemical products with renewable and biodegradable components. The most challenging part of this approach is to obtain bio-based materials with properties and functions equivalent to those of synthetic products. Various naturally occurring polymers such as starch, collagen, alginate, cellulose, and chitin represent attractive candidates as they could reduce dependence on synthetic products and consequently positively impact the environment. Chitosan is also a unique bio-based polymer with excellent intrinsic properties. It is known for its anti-bacterial and film-forming properties, has high mechanical strength and good thermal stability. Nanotechnology has also applied chitosan-based materials in its most recent achievements. Therefore, numerous chitosan-based bionanocomposites with improved physical and chemical characteristics have been developed in an eco-friendly and cost-effective approach. This review discusses various sources of chitosan, its properties and methods of modification. Also, this work focuses on diverse preparation techniques of chitosan-based bionanocomposites and their emerging application in various sectors. Additionally, this review sheds light on future research scope with some drawbacks and challenges to motivate the researchers for future outstanding research works.
    Matched MeSH terms: Chitosan/pharmacology
  3. Effect of differences in physical and chemical properties of chitosan on endothelial cell adhesion and growth
    Mai-Ngam K, Seetapan N, Sagnella S
    Med J Malaysia, 2004 May;59 Suppl B:172-3.
    PMID: 15468873
    Matched MeSH terms: Chitosan/pharmacology
  4. Effects of preharvest applications of methyl jasmonate and chitosan on postharvest decay, quality and chemical attributes of Fragaria chiloensis fruit
    Saavedra GM, Figueroa NE, Poblete LA, Cherian S, Figueroa CR
    Food Chem, 2016 Jan 1;190:448-53.
    PMID: 26212995 DOI: 10.1016/j.foodchem.2015.05.107
    Fragaria chiloensis fruit has a short postharvest life mainly due to its rapid softening. In order to improve its postharvest life, preharvest applications of methyl jasmonate (MeJA) and chitosan were evaluated during postharvest storage at room temperature. The quality and chemical parameters, and protection against decay were evaluated at 0, 24, 48 and 72 h of storage from fruits of two subsequent picks (termed as first harvest and second harvest). In general, fruits treated with MeJA and chitosan maintained higher levels of fruit firmness, anthocyanin, and showed significant delays in decay incidence compared to control fruit. MeJA-treated fruits exhibited a greater lignin content and SSC/TA ratio, and delayed decay incidences. Instead, chitosan-treated fruits presented higher antioxidant capacity and total phenol content. In short, both the elicitors were able to increase the shelf life of fruits as evidenced by the increased levels of lignin and anthocyanin, especially of the second harvest.
    Matched MeSH terms: Chitosan/pharmacology*
  5. Fulltext Residual analysis of chitosan-based agronanofungicides as a sustainable alternative in oil palm disease management
    Maluin FN, Hussein MZ, Yusof NA, Fakurazi S, Maznah Z, Idris AS, et al.
    Sci Rep, 2020 12 18;10(1):22323.
    PMID: 33339951 DOI: 10.1038/s41598-020-79335-6
    The nanoformulations of pesticides have shown great interest from many parties due to their slow release capability and site-specific delivery. Hence, in this work, a new nanoformulation of a fungicide, namely chitosan-hexaconazole nanoparticles with a mean diameter size of 18 nm was subjected to the residual analysis on oil palm tissue, leaf and palm oil (crude palm oil and crude palm kernel oil) using a quick, easy, cheap, effective, rugged and safe (QuEChERS) method coupled with the gas chromatography-micro electron capture detector (GC-µECD). The chitosan-hexaconazole nanoparticles were applied using the trunk injection method at 4.5 g a.i./palm (standard single dose) and 9.0 g a.i./palm (double dose). The fungicide residue was analyzed at 0 (6 h after application), 1, 3, 7, 14, 30, 60, 90, and 120 days after treatment. The palm oil matrices; the crude palm oil (CPO) and crude palm kernel oil (CPKO) were found to be residue-free. However, it was observed that high accumulation of the fungicide in the stem tissue and leaf after the treatment using the chitosan-hexaconazole nanoparticles, which is good for better bioavailability for the treatment of the fungi, Ganoderma boninense. The dissipation kinetic at double dose treatment in the tissue and leaf was found to govern by the second-order kinetic with half-lives (t1/2) of 383 and 515 days, respectively.
    Matched MeSH terms: Chitosan/pharmacology*
  6. Effects of chitin and chitosan from cricket and shrimp on growth and carcass performance of broiler chickens
    Lokman IH, Ibitoye EB, Hezmee MNM, Goh YM, Zuki ABZ, Jimoh AA
    Trop Anim Health Prod, 2019 Nov;51(8):2219-2225.
    PMID: 31134556 DOI: 10.1007/s11250-019-01936-9
    Majority of the studies on the effect of chitin and chitosan on growth and carcass characteristics of broiler chickens has concentrated more on shrimp chitin and shrimp chitosan, and often with contradictory results. Therefore, the objective of this present study is to evaluate and compare the effect of dietary chitin and chitosan from cricket and shrimp on growth performance, carcass, and organ characteristics of broiler chickens. One hundred fifty-day-old male Cobb500 broiler chicks of similar average weight were randomly allotted into one of the five dietary treatments with three replicates. Treatment 1 (T1) chicks were fed basal diet only (control), treatment 2 and 3 (T2 and T3) chicks were given basal diet with 0.5 g/kg diet of cricket chitin and cricket chitosan, respectively, while treatment 4 and 5 (T4 and T5) chicks were served basal diet with 0.5 g/kg diet of shrimp chitin and shrimp chitosan respectively. No significant variation occurred between cricket chitin and shrimp chitin, although data on growth performance were higher in cricket chitin, but growth performance varied significantly between cricket chitosan and shrimp chitosan. This study revealed that cricket chitin at 0.5 g/kg significantly improved growth performance, carcass quality, and organ characteristics of broilers more than chitosan. Birds fed basal diet alone, although gained more weight, also accumulated more fat having the poorest feed conversion ratio (FCR) and the highest mortality. However, carcass of birds fed cricket chitin was the leanest and thus economically beneficial as they consumed the least amount of feed with the best FCR.
    Matched MeSH terms: Chitosan/pharmacology*
  7. Effects of Gamma Irradiation on Structural, Chemical, Bioactivity and Biocompatibility Characteristics of Bioactive Glass-Polymer Composite Film
    Sujon MK, Samsurrijal SF, Baharin R, Isa NM, Zabidi MA, Mohd Noor SNF
    J Biomed Mater Res A, 2025 Jan;113(1):e37842.
    PMID: 39668803 DOI: 10.1002/jbm.a.37842
    Gamma irradiation is an effective technique for biocomposite films intended for application in tissue engineering (TE) to ensure sterility and patient safety prior to clinical applications. This study proposed a biocomposite film composed of natural polymer chitosan (CS) and synthetic polymer poly-Ɛ-caprolactone (PCL) reinforced with sol-gel-derived bioactive glass (BG) for potential application in TE. The BG/PCL/CS biocomposite film was sterilized using 25 kGy gamma rays, and subsequent changes in its characteristics were analyzed through mechanical and physical assessment, bioactivity evaluation via immersion in simulated body fluid (SBF) and biocompatibility examination using human primary dermal fibroblasts (HPDFs). Results indicated a homogeneous distribution of BG particles within the BG/PCL/CS polymer matrix which enhanced bioactivity, and the polymer blend provide a structurally stable film. Gamma irradiation induced an increase in the film's surface roughness due to photo-oxidative degradation; however, this did not adversely affect the integrity of glass particles and polymer chains. In vitro assessments demonstrated hydroxyapatite formation on the film's surface, suggesting bioactivity. Biocompatibility testing confirmed enhanced cell adhesion and proliferation. These multifunctional properties highlight the potential of the fabricated BG/PCL/CS biocomposite film for TE and regenerative medicine applications.
    Matched MeSH terms: Chitosan/pharmacology
  8. Synthesis of poly(3-hydroxybutyrate-co-4-hydroxybutyrate)/chitosan/silver nanocomposite material with enhanced antimicrobial activity
    Rennukka M, Sipaut CS, Amirul AA
    Biotechnol Prog, 2014 Nov-Dec;30(6):1469-79.
    PMID: 25181613 DOI: 10.1002/btpr.1986
    This work aims to shed light in the fabrication of poly(3-hydroxybutyrate-co-44%-4-hydroxybutyrate)[P(3HB-co-44%4HB)]/chitosan-based silver nanocomposite material using different contents of silver nanoparticle (SNP); 1-9 wt%. Two approaches were applied in the fabrication; namely solvent casting and chemical crosslinking via glutaraldehyde (GA). A detailed characterization was conducted in order to yield information regarding the nanocomposite material. X-ray diffraction analysis exhibited the nature of the three components that exist in the nanocomposite films: P(3HB-co-4HB), chitosan, and SNP. In term of mechanical properties, tensile strength, and elongation at break were significantly improved up to 125% and 22%, respectively with the impregnation of the SNP. The melting temperature of the nanocomposite materials was increased whereas their thermal stability was slightly changed. Scanning electron microscopy images revealed that incorporation of 9 wt% of SNP caused agglomeration but the surface roughness of the material was significantly improved with the loading. Staphylococcus aureus and Escherichia coli were completely inhibited by the nanocomposite films with 7 and 9 wt% of SNP, respectively. On the other hand, degradation of the nanocomposite materials outweighed the degradation of the pure copolymer. These bioactive and biodegradable materials stand a good chance to serve the vast need of biomedical applications namely management and care of wound as wound dressing.
    Matched MeSH terms: Chitosan/pharmacology
  9. In vitro capacity of different grades of chitosan derivatives to induce platelet adhesion and aggregation
    Periayah MH, Halim AS, Hussein AR, Saad AZ, Rashid AH, Noorsal K
    Int J Biol Macromol, 2013 Jan;52:244-9.
    PMID: 23063426 DOI: 10.1016/j.ijbiomac.2012.10.001
    Chitosan-derived hemostatic agents with various formulations may have distinct potential in hemostasis. This study assessed the ability of different grades and forms of chitosan derivatives as hemostatic agents to enhance platelet adhesion and aggregation in vitro. The chitosan derivatives utilized were 2% NO-CMC, 7% NO-CMC (with 0.45 mL collagen), 8% NO-CMC, O-C 52, 5% O-CMC-47, NO-CMC-35, and O-C 53. Samples of chitosan derivatives weighing 5mg were incubated at 37°C with 50 μL of phosphate buffer saline (PBS) (pH 7.4) for 60 min. The morphological features of the platelets upon adherence to the chitosan were viewed using scanning electron microscope (SEM), and the platelet count was analyzed with an Automated Hematology Analyzer. For platelet aggregation, we added an adenosine diphosphate (ADP) agonist to induce the chitosan-adhered platelets. O-C 52 bound with platelets exhibited platelet aggregates and clumps on the surface of the membrane layer with approximately 70-80% coverage. A statistically significant correlation (p<0.01) for the platelet count was identified between the baseline value and the values at 10 min and 20 min. The results indicate that O-C 53 and O-C 52 were able to promote clotting have the potential to induce the release of platelets engaged in the process of hemostasis.
    Matched MeSH terms: Chitosan/pharmacology*
  10. Fulltext Potential of chitosan-loaded nanoemulsions to control different Colletotrichum spp. and maintain quality of tropical fruits during cold storage
    Zahid N, Ali A, Manickam S, Siddiqui Y, Maqbool M
    J Appl Microbiol, 2012 Oct;113(4):925-39.
    PMID: 22805053 DOI: 10.1111/j.1365-2672.2012.05398.x
    To investigate the antifungal activity of conventional chitosan and chitosan-loaded nanoemulsions against anthracnose caused by Colletotrichum spp. isolated from different tropical fruits.
    Matched MeSH terms: Chitosan/pharmacology*
  11. Suitability of combination of calcium propionate and chitosan for preserving minimally processed banana quality
    Mirshekari A, Madani B, Golding JB
    J Sci Food Agric, 2017 Aug;97(11):3706-3711.
    PMID: 28111769 DOI: 10.1002/jsfa.8231
    BACKGROUND: The marketability of fresh-cut banana slices is limited by the rapid rate of fruit softening and browning. However, there is no scientific literature available about the role of postharvest calcium propionate and chitosan treatment on the quality attributes of fresh-cut banana. Therefore, the aim of the present study was to investigate these effects.

    RESULTS: The application of calcium propionate plus chitosan (CaP+Chit) retained higher firmness, higher ascorbic acid content, higher total antioxidant activity and higher total phenolic compounds, along with lower browning, lower polyphenol oxidase, lower peroxidase, lower polygalacturonase and lower pectin methyl esterase activities and microbial growth, compared to control banana slices after 5 days of cold storage.

    CONCLUSION: The results of the present study show that CaP+Chit could be used to slow the loss of quality at the same time as maintaining quality and inhibiting microbial loads. © 2017 Society of Chemical Industry.

    Matched MeSH terms: Chitosan/pharmacology*
  12. Recent Advances in Polymer-based Wound Dressings for the Treatment of Diabetic Foot Ulcer: An Overview of State-of-the-art
    Hussain Z, Thu HE, Shuid AN, Katas H, Hussain F
    Curr Drug Targets, 2018;19(5):527-550.
    PMID: 28676002 DOI: 10.2174/1389450118666170704132523
    BACKGROUND: Diabetic foot ulcers (DFUs) are the chronic, non-healing complications of diabetic mellitus which compels a significant burden to the patients and the healthcare system. Peripheral vascular disease, diabetic neuropathy, and abnormal cellular and cytokine/chemokine activity are among the prime players which exacerbate the severity and prevent wound repair. Unlike acute wounds, DFUs impose a substantial challenge to the conventional wound dressings and demand the development of novel and advanced wound healing modalities. In general, an ideal wound dressing should provide a moist wound environment, offer protection from secondary infections, eliminate wound exudate and stimulate tissue regeneration.

    OBJECTIVE: To date, numerous conventional wound dressings are employed for the management of DFUs but there is a lack of absolute and versatile choice. The current review was therefore aimed to summarize and critically discuss the available evidences related to pharmaceutical and therapeutic viability of polymer-based dressings for the treatment of DFUs.

    RESULTS: A versatile range of naturally-originated polymers including chitosan (CS), hyaluronic acid (HA), cellulose, alginate, dextran, collagen, gelatin, elastin, fibrin and silk fibroin have been utilized for the treatment of DFUs. These polymers have been used in the form of hydrogels, films, hydrocolloids, foams, membranes, scaffolds, microparticles, and nanoparticles. Moreover, the wound healing viability and clinical applicability of various mutually modified, semi-synthetic or synthetic polymers have also been critically discussed.

    CONCLUSION: In summary, this review enlightens the most recent developments in polymer-based wound dressings with special emphasis on advanced polymeric biomaterials, innovative therapeutic strategies and delivery approaches for the treatment of DFUs.

    Matched MeSH terms: Chitosan/pharmacology
  13. Fulltext In vitro models in biocompatibility assessment for biomedical-grade chitosan derivatives in wound management
    Keong LC, Halim AS
    Int J Mol Sci, 2009 Mar;10(3):1300-1313.
    PMID: 19399250 DOI: 10.3390/ijms10031300
    One of the ultimate goals of wound healing research is to find effective healing techniques that utilize the regeneration of similar tissues. This involves the modification of various wound dressing biomaterials for proper wound management. The biopolymer chitosan (beta-1,4-D-glucosamine) has natural biocompatibility and biodegradability that render it suitable for wound management. By definition, a biocompatible biomaterial does not have toxic or injurious effects on biological systems. Chemical and physical modifications of chitosan influence its biocompatibility and biodegradability to an uncertain degree. Hence, the modified biomedical-grade of chitosan derivatives should be pre-examined in vitro in order to produce high-quality, biocompatible dressings. In vitro toxicity examinations are more favorable than those performed in vivo, as the results are more reproducible and predictive. In this paper, basic in vitro tools were used to evaluate cellular and molecular responses with regard to the biocompatibility of biomedical-grade chitosan. Three paramount experimental parameters of biocompatibility in vitro namely cytocompatibility, genotoxicity and skin pro-inflammatory cytokine expression, were generally reviewed for biomedical-grade chitosan as wound dressing.
    Matched MeSH terms: Chitosan/pharmacology*
  14. Chitosan coated alginate-xanthan gum bead enhanced pH and thermotolerance of Lactobacillus plantarum LAB12
    Fareez IM, Lim SM, Mishra RK, Ramasamy K
    Int J Biol Macromol, 2015 Jan;72:1419-28.
    PMID: 25450046 DOI: 10.1016/j.ijbiomac.2014.10.054
    The vulnerability of probiotics at low pH and high temperature has limited their optimal use as nutraceuticals. This study addressed these issues by adopting a physicochemical driven approach of incorporating Lactobacillus plantarum LAB12 into chitosan (Ch) coated alginate-xanthan gum (Alg-XG) beads. Characterisation of Alg-XG-Ch, which elicited little effect on bead size and polydispersity, demonstrated good miscibility with improved bead surface smoothness and L. plantarum LAB12 entrapment when compared to Alg, Alg-Ch and Alg-XG. Sequential incubation of Alg-XG-Ch in simulated gastric juice and intestinal fluid yielded high survival rate of L. plantarum LAB12 (95%) at pH 1.8 which in turn facilitated sufficient release of probiotics (>7 log CFU/g) at pH 6.8 in both time- and pH-dependent manner. Whilst minimising viability loss at 75 and 90 °C, Alg-XG-Ch improved storage durability of L. plantarum LAB12 at 4 °C. The present results implied the possible use of L. plantarum LAB12 incorporated in Alg-XG-Ch as new functional food ingredient with health claims.
    Matched MeSH terms: Chitosan/pharmacology*
  15. Synergistic effects of chitosan scaffold and TGFβ1 on the proliferation and osteogenic differentiation of dental pulp stem cells derived from human exfoliated deciduous teeth
    Farea M, Husein A, Halim AS, Abdullah NA, Mokhtar KI, Lim CK, et al.
    Arch Oral Biol, 2014 Dec;59(12):1400-11.
    PMID: 25222336 DOI: 10.1016/j.archoralbio.2014.08.015
    Multipotent stem cells derived from human exfoliated deciduous teeth (SHED) represent a promising cell source for tissue regeneration. In the present study we decided to test the inductive effect of chitosan and transforming growth factor-β1 (TGFβ1) as a scaffold/factor combination on SHED proliferation and osteogenic differentiation.
    Matched MeSH terms: Chitosan/pharmacology*
  16. Fulltext Antimicrobial and controlled release studies of a novel nystatin conjugated iron oxide nanocomposite
    Hussein-Al-Ali SH, El Zowalaty ME, Kura AU, Geilich B, Fakurazi S, Webster TJ, et al.
    Biomed Res Int, 2014;2014:651831.
    PMID: 24900976 DOI: 10.1155/2014/651831
    Nystatin is a tetraene diene polyene antibiotic showing a broad spectrum of antifungal activity. In the present study, we prepared a nystatin nanocomposite (Nyst-CS-MNP) by loading nystatin (Nyst) on chitosan (CS) coated magnetic nanoparticles (MNPs). The magnetic nanocomposites were characterized by X-ray powder diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), thermogravimetry analysis (TGA), vibrating sample magnetometer (VSM), and scanning electron microscopy (SEM). The XRD results showed that the MNPs and nanocomposite are pure magnetite. The FTIR analysis confirmed the binding of CS on the surface of the MNPs and also the loading of Nyst in the nanocomposite. The Nyst drug loading was estimated using UV-Vis instrumentation and showing a 14.9% loading in the nanocomposite. The TEM size image of the MNPs, CS-MNP, and Nyst-CS-MNP was 13, 11, and 8 nm, respectively. The release profile of the Nyst drug from the nanocomposite followed a pseudo-second-order kinetic model. The antimicrobial activity of the as-synthesized Nyst and Nyst-CS-MNP nanocomposite was evaluated using an agar diffusion method and showed enhanced antifungal activity against Candida albicans. In this manner, this study introduces a novel nanocomposite that can decrease fungus activity on-demand for numerous medical applications.
    Matched MeSH terms: Chitosan/pharmacology
  17. In vitro biocompatibility of chitosan porous skin regenerating templates (PSRTs) using primary human skin keratinocytes
    Lim CK, Yaacob NS, Ismail Z, Halim AS
    Toxicol In Vitro, 2010 Apr;24(3):721-7.
    PMID: 20079826 DOI: 10.1016/j.tiv.2010.01.006
    Biopolymer chitosan (beta-1,4-d-glucosamine) comprises the copolymer mixture of N-acetylglucosamine and glucosamine. The natural biocompatibility and biodegradability of chitosan have recently highlighted its potential use for applications in wound management. Chemical and physical modifications of chitosan influence its biocompatibility and biodegradability, but it is unknown as to what degree. Hence, the biocompatibility of the chitosan porous skin regenerating templates (PSRT 82, 87 and 108) was determined using an in vitro toxicology model at the cellular and molecular level on primary normal human epidermal keratinocytes (pNHEK). Cytocompatibility was accessed by using a 3-[4,5-dimethyl-2-thiazolyl]-2,5-diphenyl tetrazolium bromide (MTT) assay from 24 to 72h. To assess the genotoxicity of the PSRTs, DNA damage to the pNHEK was evaluated by using the Comet assay following direct contact with the various PSRTs. Furthermore, the skin pro-inflammatory cytokines TNF-alpha and IL-8 were examined to evaluate the tendency of the PSRTs to provoke inflammatory responses. All PSRTs were found to be cytocompatible, but only PSRT 108 was capable of stimulating cell proliferation. While all of the PSRTs showed some DNA damage, PSRT 108 showed the least DNA damage followed by PSRT 87 and 82. PSRT 87 and 82 induced a higher secretion of TNF-alpha and IL-8 in the pNHEK cultures than did PSRT 108. Hence, based on our experiments, PSRT 108 is the most biocompatible wound dressing of the three tested.
    Matched MeSH terms: Chitosan/pharmacology*
  18. Mucoadhesive Low Molecular Chitosan Complexes to Protect rHuKGF from Proteolysis: In-vitro Characterization and FHs 74 Int Cell Proliferation Studies
    Tee YN, Kumar PV, Maki MAA, Elumalai M, Rahman SAKMEH, Cheah SC
    Curr Pharm Biotechnol, 2021;22(7):969-982.
    PMID: 33342408 DOI: 10.2174/1389201021666201218124450
    BACKGROUND: Recombinant Keratinocyte Growth Factor (rHuKGF) is a therapeutic protein used widely in oral mucositis after chemotherapy in various cancers, stimulating lung morphogenesis and gastrointestinal tract cell proliferation. In this research study, chitosan-rHuKGF polymeric complex was implemented to improve the stability of rHuKGF and used as rejuvenation therapy for the treatment of oral mucositis in cancer patients.

    OBJECTIVE: Complexation of rHuKGF with mucoadhesive low molecular weight chitosan to protect rHuKGF from proteolysis and investigate the effect of chitosan-rHuKGF complex on the proliferation rate of FHs 74 Int cells.

    METHODS: The interaction between chitosan and rHuKGF was studied by molecular docking. Malvern ZetaSizer Nano Zs and Fourier-Transform Infrared spectroscopy (FTIR) tests were carried out to characterize the chitosan-rHuKGF complex. In addition, SDS-PAGE was performed to investigate the interaction between chitosan-rHuKGF complex and pepsin. The effect of chitosan-rHuKGF complex on the proliferation rate of FHs 74 Int cells was studied by MTT assay.

    RESULTS: Chitosan-rHuKGF complex was formed through the hydrogen bonding proven by the docking studies. A stable chitosan-rHuKGF complex was formed at pH 4.5 and was protected from proteolysis and assessed by SDS PAGE. According to the MTT assay results, chitosan-rHuKGF complex increased the cell proliferation rate of FHs 74 Int cells.

    CONCLUSION: The developed complex improved the stability and the biological function of rHuKGF.

    Matched MeSH terms: Chitosan/pharmacology
  19. Antifungal and Mucoadhesive Properties of an Orally Administered Chitosan-Coated Amphotericin B Nanostructured Lipid Carrier (NLC)
    Ling JTS, Roberts CJ, Billa N
    AAPS PharmSciTech, 2019 Mar 05;20(3):136.
    PMID: 30838459 DOI: 10.1208/s12249-019-1346-7
    Surface-modified nanostructured lipid carriers (NLC) represent a promising mode of drug delivery used to enhance retention of drugs at absorption site. Formulated chitosan-coated amphotericin-B-loaded NLC (ChiAmp NLC) had a size of 394.4 ± 6.4 nm, encapsulation and loading efficiencies of 86.0 ± 3% and 11.0 ± 0.1% respectively. Amphotericin-B release from NLCs was biphasic with no changes in physical properties upon exposure to simulated gastrointestinal conditions. Antifungal properties of Amphotericin-B and ChiAmpB NLC were comparable but ChiAmpB NLC was twice less toxic to red blood cells and ten times safer on HT-29 cell lines. In vitro mucoadhesion data were observed ex vivo, where ChiAmpB NLC resulted in higher retention within the small intestine compared to the uncoated formulation. The data strongly offers the possibility of orally administering a non-toxic, yet effective Amphotericin-B nanoformulation for the treatment of systemic fungal infections.
    Matched MeSH terms: Chitosan/pharmacology*
  20. Fulltext Regioselective Sequential Modification of Chitosan via Azide-Alkyne Click Reaction: Synthesis, Characterization, and Antimicrobial Activity of Chitosan Derivatives and Nanoparticles
    Sarwar A, Katas H, Samsudin SN, Zin NM
    PLoS One, 2015;10(4):e0123084.
    PMID: 25928293 DOI: 10.1371/journal.pone.0123084
    Recently, the attention of researchers has been drawn toward the synthesis of chitosan derivatives and their nanoparticles with enhanced antimicrobial activities. In this study, chitosan derivatives with different azides and alkyne groups were synthesized using click chemistry, and these were further transformed into nanoparticles by using the ionotropic gelation method. A series of chitosan derivatives was successfully synthesized by regioselective modification of chitosan via an azide-alkyne click reaction. The amino moieties of chitosan were protected during derivatization by pthaloylation and subsequently unblocked at the end to restore their functionality. Nanoparticles of synthesized derivatives were fabricated by ionic gelation to form complexes of polyanionic penta-sodium tripolyphosphate (TPP) and cationic chitosan derivatives. Particle size analysis showed that nanoparticle size ranged from 181.03 ± 12.73 nm to 236.50 ± 14.32 nm and had narrow polydispersity index and positive surface charge. The derivatives and corresponding nanoparticles were evaluated in vitro for antibacterial and antifungal activities against three gram-positive and gram-negative bacteria and three fungal strains, respectively. The minimum inhibitory concentration (MIC) of all derivatives ranged from 31.3 to 250 µg/mL for bacteria and 188 to1500 µg/mL for fungi and was lower than that of native chitosan. The nanoparticles with MIC ranging from 1.56 to 25 µg/mLfor bacteria and 94 to 750 µg/mL for fungi exhibited higher activity than the chitosan derivatives. Chitosan O-(1-methylbenzene) triazolyl carbamate and chitosan O-(1-methyl phenyl sulfide) triazolyl carbamate were the most active against the tested bacterial and fungal strains. The hemolytic assay on erythrocytes and cell viability test on two different cell lines (Chinese hamster lung fibroblast cells V79 and Human hepatic cell line WRL68) demonstrated the safety; suggesting that these derivatives could be used in future medical applications. Chitosan derivatives with triazole functionality, synthesized by Huisgen 1,3-dipolar cycloaddition, and their nanoparticles showed significant enhancement in antibacterial and antifungal activities in comparison to those associated with native, non-altered chitosan.
    Matched MeSH terms: Chitosan/pharmacology
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