The Complex World of Polysaccharides
18
Figure 6.
Staphylococcus bacteria (a), covered with chitosan (b)
18. Analgesic activity
Some investigators reported that chitin and chitosan induce analgesia. Allan in 1984 found
that chitosan provide a cool and pleasant soothing effect when applied to open wounds.
Ohshima et al in 1987, reported that chitin proved excellent pain relief in 83 out of 91 cases
who received the agent topically over open wounds such as burns, skin abrasion, skin
ulcers, skin graft areas and so on [134-135]. Minami in 1993 and Okamoto in 1993, reported
that animals did not feel pain when their wounds were covered with chitin and chitosan
[136-137].
Chitin and chitosan have been found to reduce the inflammatory pain due to intraperitoneal
administration of acetic acid in rats [138]. When the chitosan suspension was mixed with
acetic acid, the amino groups in C2 the position were protonated to NH
3
subsequently the
particles resolved in the solution. Bradykinin is one of the main substances related to pain
and the levels of this substance decrease in the presence of chitin and chitosan. Chitin
absorbs Bradykinin more extensively than chitosan and this could be one of the main
analgesic effect [138].
19. Antitumor activity
In some medical applications of chitin/chitosan, as antitumor compounds, for example, their
degradation products are preferred, as they have a lower viscosity and a better solubility in
water. The antitumor activity of chitin/chitosan is manifested by the stimulation of the
immune system (production of lymphokines, including interleukins 1 and 2, stimulation of
NK, etc.) [139-141]. Jeon and Kim in 2002, tested the antitumor activity of three kinds of
COSs (high molecular weight ranging from 6.5 to 12 kDa – HMWCOS, medium molecular
weight ranging from 1.5 to 5.5 kDa -MMWCOS, and low molecular weight ranging from 0.5
to 1.4 kDa – LMWCOS) against Sarcoma 180 solid (S180) and Uterine cervix carcinoma No.
Is Chitosan a New Panacea? Areas of Application
19
14 (U14) [140]. The efficiency of tumor growth inhibition for both types of tumor cells in
mice was best in the case of MMWCOS. There are many reports of S180 tumor cells being
used for testing the antitumor activity of chitosan [141-142].
Maeda and Kimura 2004, investigated the antitumour effect of three water-soluble low
molecular weight chitosans (21 kDa, 46 kDa, 130 kDa) and various doses of 650 kDa chitosan
in sarcoma 180-bearing mice. They found that LMWC (21 and 46 kDa) and also smaller
oligosaccharides could activate the intestinal immune system of animals, thus preventing
tumor growth. But no antitumor effect was observed after the oral administration of
chitosan samples, even of low molecular weight (46 kDa). The same authors confirmed that
high molecular weight chitosan (650 kDa) prevents the adverse reactions of some cancer
chemotherapeutic drugs [141]. Qin et al. in 2002 also tested the antitumor activity of LMWC
against sarcoma 180, but they came to the opposite conclusions [143]. They noted that oral
administration of LMW chitosan decreases the weight of the tumour [139, 142], although
administration by intraperitoneal injection led to a higher inhibitory rate [142]. It was
reported the higher the MW of LMWC, the better the tumor inhibitory effect [139]. The
introduction of acidic groups as a result of chitosan oxidation has the opposite effect, and an
increase in MW decreases antitumor activity. Qin Cai-qin et al in 2002, prepared low
molecular weight chitosans by oxidative degradation with H
2
O
2
. They found that carboxyllc
contents increased with decrease in molecular weight (M~). They also found that the
introduction of carboxylic group is advantage to water-solubility of chitosan, but more
acidic groups decrease the function of amino groups of chitosan against sarcoma 180 tumor.
There is a correlation between the activity and the molecular weights of the oxidized
chitosans, and a maximum of inhibition was found around 4 100 [143]. The influence of
LMWC and COS (including the pentamer, hexamer, and higher oligomers) on the growth
inhibition of Ehrlich ascites tumor (EAT) cells and tumor induced neovascularization was
investigated [144]. Based on experimental results concerning the inhibition of angiogenesis
and the induction of apoptosis, it was confirmed that COSs seem to be more potent angio
inhibitory and antitumor compounds. Wang et al. reported that chitin oligosaccharides (DP
1-6) also reduced the number of K562 cells (human erythromyeloblastoid leukemia cell line)
[145].
20. Chitosan applications
20.1. Biomedical
Potential applications of chitosan can only be exploited if its usable forms are properly
developed and prepared. In solution and gel, it can be used as a bacteriostatic, fungistatic
and coating agent. Gels and suspensions may play the role of carriers for slow release or
controlled action of drugs, as an immobilising medium and an encapsulation material. Film
and membranes are used in dialysis, contact lenses, dressings and the encapsulation of
mammal cells, including cell cultures. Chitosan sponges are used in dressings, and to stop
bleeding in mucous membranes. Chitosan fibres are used as resorbable sutures, non-wovens
for dressings, and as drug carriers in the form of hollow fibres.