Antibacterial composition containing water-soluble low-molecular chitosan

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents an antibacterial composition of chitosan and a gel former, containing polyvinyl alcohol, and/or glycerol, and/or polyethylene glycol and/or polyvinyl pyrrolidone, differing by the fact that the antibacterial agent is presented by low-molecular water-soluble chitosan of molecular weight 3.5 to 4.9 kDa in the amount of 0.01 to 10 wt %; the gel former is polyvinyl alcohol 2 to 15 wt %, and/or glycerol 10 to 90 wt %, and/or polyethylene glycol 1 to 20 wt %, and/or polyvinyl pyrrolidone 10 to 50 wt %; water is the rest.

EFFECT: invention provides high solubility and antibacterial activity of chitosan in the wide range of the medium acidity.

5 ex, 4 tbl, 3 dwg

 

The invention relates to the field of medical biotechnology and refers to a composition having antibacterial activity, characterized in that it contains the active substance is a water - soluble low molecular weight chitosan, and a basis.

Chitosan is a copolymer of glucosamine and acetylglucosamine - is the product of dezazetilirovanie chitin, which is found in the exoskeletons of crustaceans and insects, Paducah squid, cell walls of fungi and some algae. Chitosan is the only positively charged polymer (polycation) of natural origin, which is produced in large quantities with a high degree of chemical purity, and, importantly, with moderate cost [1]. World number chitin is estimated at the level of 1010tons, which, given the constant biosynthesis, makes it an inexhaustible source of chitosan.

In the last two decades has significantly increased the interest in biocide properties of chitosan, which along with non-toxic, biocompatible, hypoallergenic and Biodegradability, can be used in biomedical purposes as an alternative and/or auxiliary substances in antimicrobial therapy, especially in relation to a number of bacterial strains that are resistant to classical antibiotic is m [2].

However, the antibacterial properties of chitosan depend heavily on its molecular mass parameters [3]. In fact, chitosan, which is a copolymer of glucosamine and acetylglucosamine, represents a heterogeneous group of substances that differ in molecular weight, degree of deacetylation, the location of the residual acetylated units along the polymer chain, viscosity, average PKand[4]. Due to the wide variation in molecular mass parameters of the samples of the polymer, chitosan is characterized by large variations in the expression of antibacterial properties.

The antibacterial properties of chitosan depend:

- firstly, from the level of dezazetilirovanie, i.e. the share of aminosuaren residue with a free amino group. The increase in the degree of dezazetilirovanie chitosan leads to increased antibacterial properties polyaminoamide [5].

- secondly, the degree of protonation of the free amino groups of the polymer, since it is positively charged amino groups largely determine the affinity of chitosan to the cells of microorganisms. With the increase in the degree of protonation of the amino groups of chitosan enhanced the antibacterial properties of the polymer. The degree of protonation of the polymer depends on the acidity of the environment, the more acidic the environment, the more positively charged chitosane the first polymer, therefore, when increasing the pH of the medium antibacterial properties of chitosan are amplified, and when the alkalization is reduced [5].

- third, from molecular weight (polymerization degree) of chitosan. Usually with the increase of molecular weight of chitosan is its antibacterial properties are enhanced [5, 6]. This is due to its increasing ability to interact with cells of the microorganisms with increasing molecular weight. Usually this dependence is observed in the evaluation of antibacterial properties of chitosan in acidic conditions at low pH environment (below 6.5). However, there is evidence that testify to strengthening antibacterial properties of chitosan in reducing its molecular weight, which is associated with better solubility more low molecular weight forms of the polymer [7, 8]. Typically, these data are obtained in the evaluation of antibacterial properties of chitosan at neutral or slightly alkaline conditions, with an average pH of the medium (6.5 to 8.0). This contradiction based antibacterial properties of chitosan from its molecular weight (polymerization degree) determines the relevance of search for the optimum molecular-mass parameters of samples of chitosan, which would have had a sufficiently high antibacterial activity in a wide range of acidity of the environment - both in acid and in alkaline conditions, for subsequent inclusion in the antibacterial composition.

There is a method of stabilization of cosmetic products by introducing them chitosan with a molecular mass of from 3 to 700 kDa. In this case, chitosan is used as a preservative, adding it to the composition of the drug in the amount of 0.005 to 0.5 mol. [9].

Known composition containing chitosan (0,19%), ascorbic acid (0,165%) and sodium ascorbate used in dental surgery for the healing of defects in periodontal tissue [10].

Known composition containing chitosan (1-4 wt.%), glycerol (10-90 wt.%) and acetic acid (1 wt.%), used as a carrier for drugs analgesics and anti-bacterial agents [11].

A close analogue to our invention can be considered a patent for the invention "Gel for skin care and treatment of its diseases and composition to obtain" [12]. The main disadvantage of this example is that it uses chitosan with a molecular mass of from 10 to 500 kDa, which does not have sufficient solubility in neutral and alkaline conditions.

Thus, all the above examples involve the use of either chitosan with high molecular weight or molecular mass in a wide range of this parameter do not take into account the strong differences in the manifestation of Antibes is Karelenergo steps in samples with different molecular mass, that can lead to insufficient use of antimicrobial potential of this polymer. As mentioned above, samples of chitosan with higher molecular weight can lose its activity at neutral and alkaline conditions. Polydisperse samples, which contain molecules of chitosan polymer with very different molecular weight may also have a lack of efficiency in such conditions due to loss of activity they are composed of fractions of polymer molecules with a sufficiently high degree of polymerization (molecular weight).

In this regard, the purpose of the claimed invention to provide an antibacterial composition consisting of water-soluble low molecular weight chitosan with enhanced antibacterial activity in a wide range of levels of acidity (pH from 5.50 to 8.00) and giving it the property of the composition.

This object is achieved by including in the composition of chitosan with a molecular weight of from 3.5 to 4.9 kDa (degree of polymerization of from 20 to 29), which has a higher value PKand(the value of the PKandcorresponds to the pH of the medium at which exactly half of the free amino groups of a particular sample of chitosan is positively charged), compared to the more high molecular weight samples(table 1). These samples (with a molecular weight of from 3.5 to 4.9 kDa and a degree of polymerization of from 20 to 29, respectively) also have the best restorement in neutral and slightly alkaline conditions compared to the more high molecular weight samples, as judged by a slight drop in their precipitate at higher pH environment (Fig.1) the evaluation of antibacterial properties of these samples chicoasen (molecular weight from 3.5 to 4.9 kDa and a degree of polymerization of from 20 to 29, respectively) they were found to possess antibacterial activity against staphylococci in a wide range of pH environments (from 5.50 to 8.00), in contrast to the more high molecular weight samples, which were inactive at neutral and slightly alkaline conditions (Fig.2 and 3). The use of oligomers less than 3.5 kDa is not feasible due to their weak antibacterial properties (Fig.2 and 3). As a thickener may use polyvinyl alcohol, glycerin, polyethylene glycol, polyvinylpyrrolidone.

The technical result of the claimed invention to provide an antibacterial composition consisting of water-soluble low molecular weight chitosan, which is characterized by a high level PKandas well as high solubility and antibacterial activity in a wide range of levels of acidity(pH from 5.50 to 8.00).

Example 1. Antibacterial composition, consisting of: chitosan, water-soluble low molecular weight with a molecular weight of from 3.5 to 4.9 kDa (degree of polymerization of from 20 to 29) from 0.01 to 10 wt.%, polyvinyl alcohol is from 2 to 15 wt.%, the rest is water.

The composition is in the form of a gel has antibacterial activity against various species of bacteria in a wide pH range. The results of antibacterial test of the claimed composition are presented in tables 2-4.

Example 2. Antibacterial composition as in example 1, but instead of the polyvinyl alcohol include glycerin from 10 to 90 wt.%.

Example 3. Antibacterial composition as in example 1, but instead of the polyvinyl alcohol include ethylene glycol from 1 to 20 wt.%.

Example 4. Antibacterial composition as in example 1, but instead of the polyvinyl alcohol include polyvinylpyrrolidon from 10 to 50 wt.%.

Example 5. Antibacterial composition as in example 1, but in addition to polyvinyl alcohol is from 2 to 15 wt.%., including glycerin from 10 to 90 wt.%, and the polyethylene glycol is from 1 to 20 wt.%, and polyvinylpyrrolidon from 10 to 50 wt.%.

Table 1
Characterization of chitosan samples
No. sampleMolecular mass, kDaSPFEDM, mol.%PKand
10,741,41957,1
21,581,39936,7
32,213of 1.34976,6
43,5201,71956,5
54,2241,38976,5
6a 4.9292,28786,5
7 8,349the 1.44976,4
815,0871,61946,4
9to 19.91161,66986,4

JV - average degree of polymerization

PI - index polydispersity

DM - deacetylation

1. The values of the PKandchitosans are defined by using conductometric titration

Table 2
Antibacterial activity against S. aureus of the claimed composition, in comparison with compositions which include other samples of chitosan. The composition of songs: chitosan - 1 wt.%, polyvinyl alcohol and 5 wt.%, the rest is water
pHThe zone of inhibition of growth of microorganisms on a solid nutrient medium, mm
Chitosan from 3.5 to 5.5 kDaChitosan 2 to the and Chitosan 20 kDa
5,5010312
of 5.7511310
6,0011311
6,2510311
6,5010310
6,751039
7,00835
7,25833
7,50820
of 7.75700
8,005 00

Table 3
Antibacterial activity against E. coli of the claimed composition, in comparison with compositions which include other samples of chitosan. The composition of songs: chitosan - 1 wt.%, polyvinyl alcohol and 5 wt.%, the rest is water.
pHThe zone of inhibition of growth of microorganisms on a solid nutrient medium, mm
Chitosan from 3.5 to 4.9 kDaChitosan 2 kDaChitosan 20 kDa
5,5014515
of 5.7513515
6,0014514
6,2513413
6,5012412
6,7512410
7,001243
7,251120
7,501110
of 7.75800
8,00400

Chitosan 2 kDa
Table 4
Antibacterial activity against S. epidermidis claimed composition, in comparison with compositions which include other samples of chitosan. The composition of songs: chitosan - 0.01 wt.%, polyvinyl alcohol and 5 wt.%, the rest is water.
pHThe zone of inhibition of growth of microorganisms on a solid nutrient medium, mm
Chitosan from 3.5 to 4.9 kDaChitosan 20 kDa
5,50151217
of 5.75151017
6,00151116
6,25151115
6,50151015
6,75151015
7,0015314
7,251516
7,501111
of 7.751000
8,0000

LITERATURE

1. Chitin and chitosan: synthesis, properties and applications / edited KG Scriabin, GA Vikhoreva, V.P. Varlamov. - M.: Izd-vo Nauka, 2002. - 368 S.

2. Tin, S., Sakharkar K.R., Lim C.S., Sakharkar M.K.. // Int. J. Biol. Sci. 2009. V. 5. N2. P.53-60.

3. Kulikov S., Tyurin Y.A., pasahow R.S., Varlamov V.P. / Antibacterial and antifungal activity of chitosan: mechanisms of action and role structures // Journal of Microbiology Epidemiology and Immunobiology, 2009, No. 5, s-98.

4. Tharanathan R.N., Kittur F.S. Chitin - the undisputed biomolecule of great potential. Crit. Rev. Nutr. 2003. V.43. P.61-87.

5. Liu X.F., Y.L. Guan, D.Z. Yang, Z. Li, K.D. Yao Antibacterial action of chitosan and carboxymethylated chitosan. J. Appl. Polym. Sci. 2001. V.79. P.1324-1335.

6. Eaton P., Femandes J.C., Pereira E. et al. Atomic force microscopy study of the antibacterial effects of chitosans on Escherichia coli and Staphylococcus aureus. Ultramicroscopy. 2008, 108 (10): 1128 - 1134.

7. Gerasimenko D.V., Avdienko I.D., G. Bannikov and other Antibacterial activity of water-soluble low molecular weight chitosans against various microorganisms. Go active. biochem. microbiol,40 (C): 301 - 306.

8. Kumar A.B.V., Varadaraj M.C., R.N. Tharanathan Low molecular weight chitosan - preparation with the aid of pepsin, characterization, and its bactericidal activity. Biochim. Biophys. Acta. 2004, 1670 (2): 137 - 146.

9. Patent RU No. 2028138, 1995. The method of stabilization of cosmetic products

10. Muzzarelli R, Biagini G, Pugnaloni A, Filippini 0, Baldassarre V, Castaldini C, Rizzoli C./ Reconstruction of parodontal tissue with chitosan. // Biomaterials, 1989, v.10, N 9, p.598 603

11. Pat. The SHA 4659700, AG1K 31/725, 1987.

12. Patent RU No. 2085187, 1997. Gel for skin care and treatment of its diseases and composition for its receipt.

Antibacterial composition based on chitosan and a thickening agent comprising polyvinyl alcohol and/or glycerol and/or polyethylene glycol, and/or polyvinylpyrrolidone, characterized in that as an antibacterial agent used low-molecular water-soluble chitosan with a molecular weight in the range from 3.5 to 4.9 kDa in an amount of from 0.01 to 10 wt.%, the thickening agent is polyvinyl alcohol is from 2 to 15 wt.%, and/or glycerin from 10 to 90 wt.%, and/or polyethylene glycol is from 1 to 20 wt.%, and/or polyvinylpyrrolidone from 10 to 50 wt.%, the rest is water.



 

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