Indicates that the encapsulation efficiency and increased Hten with increasing drug loading ratio Ratio decreases, respectively. If the ratio Ratio gr He was 5-1, the encapsulation efficiency was above 60%, and drug loading was approx Hr 10%. With the ratio Ratio of 7:1, increases the encapsulation DPP-4 efficiency hte to 80%, but drug loading reduced to less than 10%. Fig. 2D shows the intnsity Tsgewichtete size Size distribution of micelles PazPC / DOX with a molar ratio Ratio of 5:1. Flan PazPC micelles and PazPC / IDA has a micelle Similar size Size distribution by DLS. The molar ratio Hlt ratio of 5:1 was then selected for further experiments. Characterization of PazPC / DOX and PazPC / IDA micelles produced a 5:1 molar ratio Ratio of lipid / drug summarized in Table 1. The particle E of the micelles PazPC wei, PazPC / DOX micelles and PazPC / IDA micelles was measured by DLS, was about 8 nm to 10. Table 1 also shows that the micelles PazPC / IDA a zeta potential comparable and h Here on encapsulation efficiency PazPC / DOX had micelles. IDA was more into the core of the micelles PazPC included as DOX, probably due to the h Higher hydrophobicity t of the IDA. But both contain PazPC / DOX and PazPC / IDA micellar formulations of the free Pr Parates. The data also show that interactions were both electrostatic and hydrophobic involved in the driving force behind the formation of micelles. Then, the stability of t the PazPC / drugs studied micelles with G75 size Enausschlusschromatographie. Fig. Figure 3 shows the stability of the micelles, t PazPC drug loaded under different conditions: acidic, neutral and physiological salt concentration of 10% serum. As shown in Fig.
3A and B, or IDA DOX are substantially separated from the micelles PazPC if the micelles were incubated at pH 6.0 for 30 min, which in the region of the first peak, which considerably reduced and the second peak. If the micelles in a PBS buffer for 30 min ×, the second peak of PazPC / or DOX PazPC / IDA micelles incubated slightly elevated Ht, and the encapsulation efficiency of micelles was maintained at about 60% or 80%. If the micelles f in 10% Fetal K Calf serum were incubated for 30 min Changes in the elution profiles of the micelles Similar to those × in a PBS. The profiles of the pH-dependent Independent release of DOX or IDA loaded drug from the micelles PazPC shown in FIG. 4th Absorption experimentThe contr The cell of DOX and IDA with micellar formulations was in the sensitive and resistant P388 leukemia Mie cell lines examined P388/ADR by fluorescence microscopy. After 2 h incubation, one obtains Hten absorption of PazPC / DOX micelles in Leuk Preconcentrated, purified P388/ADR resistant line was observed in comparison with free DOX. VX-770 Regarding PazPC / IDA micelles, was observed one obtains Hte absorption in the cell line of resistance of leukemia chemistry Compared to the free IDA. The absorption of DOX or IDA Leuk Mie cells was then assayed by quantitative flow cytometry by measuring the fluorescence intensity t connected cell. Fig. 5E and F shows that the cellular Re uptake of DOX or IDA significantly increased by micellar formulations compared to free drug in the resistant cells P388/ADR after a period of 2 h incubation Ht. Fig. 5G and H show the 4 h time course of drug uptake by leukemia Chemistry cells with DOX or IDA or drug-free micelles treated. DOX or IDA allm levels Hlich steps.