Chitosan
Scientific Name(s):Chitosan
Common Name(s): Chitosan
Clinical Overview
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Uses of Chitosan
Chitosan has been used in various drug delivery systems. It has antimicrobial and other effects and can be used for kidney failure and to lower cholesterol.
Chitosan Dosing
Chitosan has been administered at doses from 1 to 4 g daily in clinical studies of cholesterol reduction.
Contraindications
Contraindications in persons allergic to shellfish.
Pregnancy/Lactation
Information regarding safety and efficacy in pregnancy and lactation is lacking. Avoid use.
Chitosan Interactions
None well documented.
Chitosan Adverse Reactions
Those allergic to shellfish may also experience allergies to chitosan products.
Toxicology
Chitosan's toxicity profile is relatively low.
Chitin is a cellulose-like biopolymer found mainly in exoskeletons of marine invertebrates and arthropods, such as shrimp, crabs or lobsters. Chitin can also be found in fungi and yeasts. Deacylated chitin is called chitosan. 1 Chitosan is unique in that, unlike plant cellulose, it possesses positively charged amino groups. These bind to the negatively charged lipid and bile components, preventing absorption by the body. 2 “Squid pens,” a waste by-product of New Zealand squid processing, are a renewable and inexpensive source of chitosan. 3
History
Chitosan has been used in the past 30 years in water purification plants to absorb greases, oils, metals and toxic substances. It can absorb four to six times its weight, and ascorbic acid can potentiate this action even further. 4
Chemistry
Chitin consists mainly of unbranched chains of beta-(1 → 4)-2-acetamido-2-deoxy-D-glucose (=N-acetyl-d-glucosamine). It is similar to cellulose, where the C-2 hydroxyl groups are replaced by acetamido residue. Chitin is practically insoluble in water, dilute acids and alcohol. However, this varies depending on product origin. 1
Chitosan, the partially deacetylated polymer of N-acetyl-D-glucosamine, is water-soluble. 3
Rheology, flocculation and film formation testing have been performed with chitosan, demonstrating its usefulness in medical and analytical applications. 3 Biodegradable and biocompatible properties of chitosan films have been studied with good outcomes. 5 In vitro and in vivo degradation tests of chitin and chitosan have been evaluated, 6 as well as chitosan film chemistry on electrically charged metal plates. 7
N-carboxymethylchitosan solubility and structure have been reported, 8 along with its ability to chelate metal ions and to enhance binding of dyes. 9
Other chemical aspects involving chitin or chitosan include: Optical isomer separation, 10 mass-spectrometric analysis, 11 polyelectrolyte and sulfation studies, 12 adherence to liposomes 13 and properties of chitosan microspheres. 14
Chitosan Uses and Pharmacology
Chitosan is used in many areas, including the cosmetic and pharmaceutical industries, for medical use as a hyperlipidemic and in hypercholesterolemia therapy and for biomaterials. It is also used for antimicrobial and other effects.
AnticholesteremicFiber products such as bran, resins, pectins, etc. have been used in the past for cholesterol and weight reduction. Cross-linked O-carboxymethyl chitosan beads are capable of absorbing LDL-cholesterol in vitro. 15 One report relates effects on many enzymes to oral administration of chitosan but proposes that physical chitosan-lipid aggregate adsorption is the mechanism of lipid adsorption. 16
Animal dataExtensive animal studies have been reported on these topics. Chitosan decreases lipid concentrations in affected rats, decreasing VLDL and increasing HDL levels. 17 Chitosan also has hypocholesterolemic actions in rats, 18 , 19 , 20 and has been shown to lower cholesterol triglycerides. 21 , 22 Chitosan alters metabolism of bile in the intestines, affecting lipid and cholesterol levels. 23
Clinical dataHypocholesterolemic effects in humans have been reported. 24 , 25
Wound healerChitosan's characteristic as a film-forming and protective polysaccharide suggests its potential use as a biomaterial. Its applications in this area have been investigated. 26 Safety and hemostatic potential have been evaluated, concluding low toxicity and tensile strength retention in many circumstances. 27 A Russian article discusses chitosan's role in reparative skin regeneration. 28 Heparin-chitosan gel application stimulated wound healing in human skin, hypothesized to possibly be caused by stabilization and activation of growth factors that bind to heparin. 29 In burn patients, where standard of care involves application of silver sulfadiazine cream, silver toxicity is a concern because of reduced skin barriers. Membranes, including chitosan, reduce this toxicity by entrapment of silver ions in the matrix. 30 Adsorption of lead ions on chitosan has also been evaluated. 31 Chitin's involvement with human enzymatic activity seems to be activation of macrophages and stimulation of fibroblasts, promoting normal tissue production. 16
Animal dataN,O-carboxymethyl chitosan gel and solution delivered postoperatively were effective in preventing peritoneal adhesions in rats. 32
Clinical dataResearch reveals no clinical data regarding the use of chitosan as a wound healer.
Other usesOne report suggests chitosan to be an effective treatment for renal failure patients. 33
Chitosan has been reported to exert some antimicrobial actions, exhibiting bactericidal actions against several pathogens in the field of dentistry, 34 inhibiting adhesion of Candida albicans to human vaginal epithelial cells 35 and inhibiting chlamydial infection by interfering with adsorption. 36
Application of chitosan in the pharmaceutical industry is documented. Its ability to mask bitter tastes in oral pharmaceuticals has been reported. 37 There are reports employing chitosan in drug delivery systems of many types. Some of these reports include the following:
Peptide/diabetic usePeptide drug delivery enhancement using chitosan, 38 colon-specific drug delivery of insulin using chitosan capsules, 39 mucoadhesion of chitosan-coated liposomes affecting insulin absorption in rats, 40 chitosan microcapsules to control insulin release, 41 and diabetic drugs in chitosan matrix tablets. 42
Nasal route studiesFor insulin, 43 , 44 effects of chitosan on intranasal mucociliary clearance 45 and transport rates. 46 Pharmacokinetics on nasal administration on morphine-6–glucuronide in sheep. 47
Transdermal deliveryUsing chitosan composite membranes. 48
Various drug release evaluationsChitosan hydrogels for organ specific antibiotic delivery in the stomach, 49 sustained release deoxytetracycline from chitosan microspheres, 50 biophosphonate-containing chitosan microspheres, 51 chitosan-indomethacin conjugates, 52 aspirin and heparin embedded in a chitosan matrix, 53 preparation and drug-release properties of chitosan-drug microspheres, 54 suitability of chitosan as a carrier, using indomethacin papaverine 55 and lidocaine, 56 , 57 cancer drug delivery, 58 buccal and vaginal tablets containing mycotic drugs and chitosan, 59 nifedipine release with chitosan microspheres, 60 chitosan beads to deliver salmon calcitonin. 61
Chitosan to enhance absorptionFor poorly absorbable drugs 62 and across mucosal surfaces. 63
Cosmetic industryChitosan's role in the cosmetic industry has been reported. 64 , 65 , 66 Chitosan use as a natural product may substitute for the synthetic polymer elements in film-forming resins. 67
Fabric industryChitosan's use includes photographic emulsions and improving dyeability of synthetic fibers in the fabric industry. 1
Dosage
Chitosan has been administered at doses from 1 to 4 g daily in clinical studies of cholesterol reduction.
Pregnancy/Lactation
Information regarding safety and efficacy in pregnancy and lactation is lacking. Avoid use.
Interactions
None well documented.
Adverse Reactions
Consult your physician if you are allergic to shellfish or if you are pregnant or breastfeeding.
Toxicology
Chitosan's toxicity profile is relatively low. Dietary chitosan reportedly affects calcium metabolism in animals. 68 Toxic effects of chitosan are dependent mainly on their chemical composition. 62
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