High-performance paclitaxel encapsulation in polymeric micelles by PLAMIC platform

SANMARCO, ELENA M.; MORETON, MARCELA; POLICASTRO, LUCIA; MARTINEZ ESPINOSA, DAILENYS; SORAIRES SANTACRUZ, M. CRISTINA; CABALEIRO, JUAN M. ; GIANNONI, FLORENCIA ; CHIAPPETA, DIEGO

Córdoba

Congreso; II Brazil-Argentine Microfluidics Congress, V Congreso de Microfluídica Argentina; 2019

Polymeric micelles (PMs) are nanoparticulates systems usually used to optimize drug delivery. PMs are generally composed by hydrophobic polymers and surfactants or amphiphilic co-polymers that form a hydrophobic core, where it is possible to include lipophilic drugs. In recent years, microfluidic technology (MT) assisted nanomedicines synthesis, where fluids are finely controlled, getting an improvement of these processes and allowing reproducibility between different batches. The objective of this project was to improve the synthesis method to obtain PM and the encapsulation of paclitaxel (PTX), a lipophilic cancer drug used as a first-line treatment of breast and ovarian cancer using PLAMIC, a Lab-on-a-Chip developing Start-up platform for drug encapsulation in nanovehicles based in our previous report1.Synthesis was performed in a zig-zag micromixer obtained by 3D printing technique. On the other hand, PMs and PTX encapsulation was performed in batch in traditional methods (TM) in order to compared. In both cases, the quantification of PTX was performed by high performance liquid chromatography (HPLC). The linearity of the last method was evaluated, not observe differences between the retention times of the peaks corresponding to the PMs containing PTX and the standard solutions. Dialysis was performed after the process. Size and polydispersity of PMs was obtained by dynamic light scattering (DLS). The co-polymer of polycaprolactorna (PCL) and polyethylene glycol (PEG) in diblock arrangement (PEG-PCL) and different PTX concentrations were evaluated. For MT at a given flow for different drug concentrations, we obtained a significant improvement in micelles sizes, polydispertion and drug encapsulation. For instance, we obtained micelles in the order of 60-70 nm and 150nm by MT versus TM respectively. PTX encapsulation also improved significantly, obtaining 44% by MT while 70-80% by MT.In summary, PLAMIC platform improved significantly the performance obtaining of paclitaxel micelles polymeric. 1-Conde AJ et al Lab Chip. 2014 14(23):4506-12, 2014.