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5H-indolo-[2,3-b]quinolines loaded polymeric micelles |
Katarzyna Bem 1, Magdalena Piętka-Ottlik 1, Anna Jaromin 2, Magdalena Miśkiewicz 1, Witold Musiał 3, Katarzyna Sidoryk 4, Wanda Peczyńska-Czoch 5, Łukasz S. Kaczmarek 4 |
1. Wroclaw University of Technology, Department of Organic and Pharmaceutical Technology, Wybrzeże Wyspiańskiego 27, Wrocław 50-370, Poland |
Abstract |
The purpose of this study was to optimize and characterize novel polymeric mixed micelles loaded with 2,5,9,11-tetramethyl-5H-indolo-[2,3-b]quinoline, a compound bearing the highest antitumor activity in 5H series derivatives of indoloquinolines and 5,11-dimethyl-5H-indolo-[2,3-b]quinoline which displayed a strong antibacterial, antimycotic and cytotoxic activity in vitro against leukemia P388 and L1210 and melanoma B16. Mixed polymeric micelles were prepared by thin-film hydration method in several proportions in order to confirm optimal value of variables i.e. polymers mass fraction and concentration, amount of derivative of a indoloquinoline, amount of water and level of hydration temperature. Mixed polymeric micelles proved higher sizes and lower polydispersity than micelles prepared from only one of these Pluronics. The determined drug-loading coefficients (DL%), encapsulation ratios (ER%) and Zeta potential values allow to assume that the particles have proper size and density to remain in suspension which leads to repulse. Such combination ensures that the solution or dispersion resists aggregation. This observation gives a strong ground to claim that mixed polymeric micelles may be considered as an effective nanocarrying system for 2,5,9,11-tetramethyl-5H-indolo-[2,3-b]quinoline and 5,11-dimethyl-5H-indolo-[2,3-b]quinoline. |
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Presentation: Poster at VIII Multidyscyplinarna Konferencja Nauki o Leku, by Katarzyna SidorykSee On-line Journal of VIII Multidyscyplinarna Konferencja Nauki o Leku Submitted: 2012-03-26 11:36 Revised: 2012-03-26 12:06 |