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用于口腔递送抗菌和抗病毒剂的乙烯-醋酸乙烯酯共聚物基质。

EVA copolymer matrix for intra-oral delivery of antimicrobial and antiviral agents.

作者信息

Ramadevi A, Padmavathy T, Stigall G, Paquette D, Kalachandra S

机构信息

Department of Periodontology, School of Dentistry, University of North Carolina, Chapel Hill, NC 27599, USA.

出版信息

J Mater Sci Mater Med. 2008 Feb;19(2):721-7. doi: 10.1007/s10856-007-3109-3. Epub 2007 Jul 10.

Abstract

Biocompatible ethylene vinyl acetate copolymer (EVA) was utilized to study the release of an antiviral drug (acyclovir (ACY)) and an antimicrobial drug (doxycycline hyclate (DOH)). Release of both drugs from EVA was measured individually and in combination. The effect of drug combination of DOH and ACY is presented. Additionally, the release rate of DOH after coating of the matrix with a different copolymer, in drug-loading with increasing loads of DOH, and with increases in temperature are also presented. The drugs incorporated in EVA films were prepared from the dry sheet obtained by solvent evaporation of polymer casting solutions with drugs. Drug release from the films was examined for about 12 days in distilled water at 37 degrees C. Changes in optical density were followed spectrophotometrically. The combination of ACY and DOH resulted in an increased release of ACY by about three times (P < 0.001) while DOH showed a decrease in rate of about two times compared to the individual release rates (P = 0.008). Increases in drug levels of DOH resulted in increases in drug release rates (P = 0.001). The release rate of DOH increased with temperature (P = .001; 27, 32, 37 and 42 degrees C were studied) and the energy of activation (DeltaE ( not equal) = 56.69 kJ/mol) was calculated using the Arrhenius equation for the diffusion of DOH molecules. Thus, the release rates of drugs were influenced by many factors: drug combination, coating the device, drug-loading, and temperature variation. Therefore it is proposed that controlling these variables should make it possible to obtain therapeutic levels of drugs released from drug loaded polymer, which may be beneficial in treating oral infections.

摘要

生物相容性乙烯-醋酸乙烯酯共聚物(EVA)被用于研究抗病毒药物(阿昔洛韦(ACY))和抗菌药物(盐酸多西环素(DOH))的释放情况。分别测量了两种药物从EVA中的单独释放以及联合释放情况。展示了DOH和ACY药物组合的效果。此外,还展示了用不同共聚物包被基质后DOH的释放速率、随着DOH负载量增加时的载药情况以及温度升高时的释放速率。EVA膜中所含药物由通过溶剂蒸发含药聚合物浇铸溶液得到的干片制备而成。在37℃的蒸馏水中对膜的药物释放进行了约12天的检测。通过分光光度法跟踪光密度的变化。ACY和DOH的组合使ACY的释放增加了约三倍(P < 0.001),而与单独释放速率相比,DOH的释放速率下降了约两倍(P = 0.008)。DOH药物水平的增加导致药物释放速率增加(P = 0.001)。DOH的释放速率随温度升高而增加(研究了27、32、37和42℃;P = 0.001),并且使用阿仑尼乌斯方程计算了DOH分子扩散的活化能(ΔE≠ = 56.69 kJ/mol)。因此,药物的释放速率受多种因素影响:药物组合、包被装置、载药以及温度变化。所以建议控制这些变量应该能够获得从载药聚合物中释放的治疗水平的药物,这可能对治疗口腔感染有益。

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