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5H-indolo-[2,3-b]quinolines loaded polymeric micelles

Katarzyna Bem 1Magdalena Piętka-Ottlik 1Anna Jaromin 2Magdalena Miśkiewicz 1Witold Musiał 3Katarzyna Sidoryk 4Wanda Peczyńska-Czoch 5Łukasz S. Kaczmarek 4

1. Wroclaw University of Technology, Department of Organic and Pharmaceutical Technology, Wybrzeże Wyspiańskiego 27, Wrocław 50-370, Poland
2. University of Wroclaw, Department of Lipids and Liposomes, Faculty of Biotechnology, Przybyszewskiego 63/77, Wrocław 51-148, Poland
3. Wroclaw Medical University, Department of Pharmaceutical Technology, Szewska 38, Wrocław 50-139, Poland
4. Pharmaceutical Research Institute, Rydygiera 8, Warsaw 01-793, Poland
5. Wrocław University of Technology, Department of Organic Chemistry, 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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Related papers

Presentation: Poster at VIII Multidyscyplinarna Konferencja Nauki o Leku, by Katarzyna Sidoryk
See On-line Journal of VIII Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2012-03-26 11:36
Revised:   2012-03-26 12:06