ENCAPSULATION OF ANTITUBERCULAR DRUGS BY BIOPOLYMERS AND POLYELECTROLYTE MULTILAYERS

The problem of drug-resistant tuberculosis treatment is complex and urgent: the standard
of treatment includes the oral administration of six names of antibiotics, i.e. up to
twenty tablets a day by the patient. This causes severe side effects, including those appeared
due to the formation of toxic products of drug interactions in the body. Therefore, it
is important that some drugs dissolve in a stomach, and others – in the intestine, which will
lead to increased bioavailability, reduced dosage and toxicity. The development of targeted
delivery systems for drugs with controlled release, targeted delivery and minimization of
side effects are of interest. One of the promising methods is polyelectrolytic multilayers
and the technology of creating such layers by a step-by-step adsorption of heterogeneously
charged polyelectrolytes.

The aim of this article is the microencapsulation of anti-tuberculous
drugs into biopolymers coated with polyelectrolytic multilayers, and the solubility
study of microcapsules at pH values simulating various parts of the gastrointestinal tract.

Materials and methods. Drugs as isoniazide, pyrazinamide, moxifloxacin, and biopolymers:
gellan, pectin and sodium alginate, chitosan and dextran sulfate, as well as Eudragit
S are used to prepare microcapsules. The obtained microcapsules are studied by a method
of scanning electron microscopy. Quantitative determination of the effectiveness of the inclusion
of drugs in microcapsules was carried out using pharmacopoeial methods.

Results and discussion. The inclusion efficiency rises with an increase of biopolymer concentration. The inclusion efficiency increases in the row isoniazide <pyrazinamide <moxifloxacin. The possibility of microencapsulation of anti-tuberculosis drugs of pyrazinamide, isoniazide and moxifloxacin by means of coating with polyelectrolytic multilayers is shown.
At pH = 7.4, the degree of release of the drugs from microcapsules without applied multilayers
for 12 hours was more than 80%, i.e. the prolongation was 12 hours. In the case
of microcapsules coated with polyelectrolytic multilayers: for 12 hours – 55/50%, for 18
hours – more than 87/80%.

Conclusion. The possibility of preparation of microcapsules of anti-tuberculosis drugs using biopolymers coated with polyelectrolytic layers, having a prolonged action is up to 18 hours, i1.5 times greater than that without coating. 

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