Chitosan-Based Hydrogel Composition with Megosine
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Pharmaceutical Chemistry Journal, Vol. 54, No. 5, August, 2020 (Russian Original Vol. 54, No. 5, May, 2020)
CHITOSAN-BASED HYDROGEL COMPOSITION WITH MEGOSINE E. M. Sultanova,1 M. Zh. Oripova,1 Yu. I. Oshchepkova,1,* and Sh. I. Salikhov1 Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 54, No. 5, pp. 43 – 46, May, 2020.
Original article submitted August 15, 2019. Chitosan hydrogels containing the antiviral drug megosine were prepared. The conditions (concentrations of polymer solution, cross-linking agent, and drug substance) were selected so that the hydrogel could be formed without separating the liquid phase. The possibility for prolonged release of megosine from the developed chitosan hydrogel was demonstrated. Megosine in the hydrogels administered vaginally did not penetrate into blood and organs. The release kinetics of megosine from the chitosan hydrogels were studied and showed 59% release of megosine from the hydrogel in 7 h. Keywords: chitosan, megosine, genital herpes.
Ordinary vaginal delivery systems, e.g., creams, foams, and gels, are held relatively briefly within the body because of the self-cleaning action of the vaginal tract. This also decreases the drug retention period and increases the dose and frequency of administration. Eventually, this becomes inconvenient for the patient. Special mucoadhesives should be added to the dosage form to increase the drug residence time on the mucosal surface and to increase the therapeutic efficacy [9]. Chitosan could be one such promising additive. Chitosan is a natural cationic aminopolysaccharide. Chitosan possesses high chemical and biological stability, excellent mechanical strength, adequate permeability, and charac-
Genital herpes is one of the most common viral diseases in the world. No known antiviral drug can eliminate herpes virus from the body [1, 2]. However, more and more viruses resistant to acyclovir (and similar drugs) have recently appeared. Interferon production in patients with recurrent herpes was found to be significantly reduced as compared to healthy individuals [2, 3]. Therefore, endogenous interferon inductors are used for herpes therapy [4, 5]. Megosine is an antiviral drug that was obtained from the Institute of Bioorganic Chemistry, Academy of Sciences of the Republic of Uzbekistan [8/118/1 from Sept. 27, 2013]. Megosine is a gossypol derivative (Fig. 1) that is produced by reacting gossypol and sodium b-aminoethanesulfonate. Megosine is used as an ointment (1%) to treat herpes infections of the skin and mucous membranes in adults (genital herpes, cervicitis, cervical erosion). It is allowed for use by Order No. 914 of the USSR Ministry of Health dated Aug. 4, 1983 [6]. Megosine can induce a,b,g-interferons in the body itself. Therefore, megosine has a direct antiviral effect that affects the interferon system [7, 8]. 1
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A. S. Sadykov Institute of Bioorganic Chemistry, Academy of Sciences of the Republic of Uzbekistan, 83 Mirzo-Ulugbeka St., Tashkent, 100125 Uzbekistan. e-mail: [email protected]
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