Chitosan Hydrogel Improves Bioavailability of Megosin

É. Sultanova, M. Salakhutdinova, Y. I. Oshchepkova, A. Asrorov, M. J. Oripova, U. J. Ishimov, S. Salikhov
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Abstract

Abstract Background The aim of this study was to obtain chitosan hydrogels containing megosin, an antiviral medicinal substance, to prolong its bioavailability. Megosin as an immunomodulating agent possesses at least twice higher virostatic and virucidal activities than gossypol, the megosin precursor, and other imine derivatives of gossypol. Materials and Methods Chitosan, used in this paper, was obtained by deacetylation of chitin; megosin was obtained on the bases of gossypol. Different concentrations of sodium tripolyphosphate (STPP) were used as the cross-linking agent. The release of megosin from hydrogel samples into blood was conducted on five white rats in four groups. Results Infrared spectral data demonstrated cross-linkage that the band responsible for NH bending of the uncross-linked chitosan reduced its intensity and moved to a lower wavelength, 1636 cm−1. It has been proven that megosin contained in gels does not penetrate into the blood and organs after vaginal administration. Release kinetics of megosin from chitosan hydrogels revealed that within 7 h, up to 52% of megosin is allowed into acidic solution (pH 4.5). Conclusion This study demonstrates the possibility to prolong bioavailability of megosin for at least 7 h, during which time it is not released into blood. The obtained results show the possibility to use the gel composition to treat vaginal herpes.
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壳聚糖水凝胶提高麦戈辛的生物利用度
摘要:本研究的目的是制备含有抗病毒药物甲去甲素的壳聚糖水凝胶,以延长其生物利用度。麦芽糖素作为一种免疫调节剂,具有比棉酚、麦芽糖素前体和棉酚的其他亚胺衍生物至少高两倍的病毒抑制和杀病毒活性。材料与方法甲壳素脱乙酰制得壳聚糖;以棉酚为原料制备了麦戈辛。采用不同浓度的三聚磷酸钠(STPP)作为交联剂。将水凝胶样品中的甲高辛释放到血液中,将5只大鼠分为4组。结果红外光谱数据显示,未交联壳聚糖的NH弯曲带强度降低,并向较低波长(1636 cm−1)移动。已经证明,凝胶中含有的甲高辛在阴道给药后不会渗透到血液和器官中。壳聚糖水凝胶中去甲素的释放动力学表明,在7小时内,高达52%的去甲素被允许进入酸性溶液(pH为4.5)。结论本研究证明了将甲高辛的生物利用度延长至少7小时的可能性,在此期间甲高辛不会释放到血液中。所获得的结果显示了使用凝胶组合物治疗阴道疱疹的可能性。
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来源期刊
European Pharmaceutical Journal
European Pharmaceutical Journal Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
0.60
自引率
0.00%
发文量
16
期刊介绍: European Pharmaceutical Journal publishes only original articles not previously published and articles that are not being considered or have not been submitted for publication elsewhere. If parts of the results have been published as conference abstract or elsewhere, it should be stated in references. The ethical standards of the Helsinki-Tokio Declaration should be kept. This should be mentioned in the Methods of manuscript. Reviews are published only on request. Authors, whose submitted research work was performed with the support of a company, should indicate this in Conflict of Interest.
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