Characterization of Docetaxel Loaded Poloxamer188 Composite PEG100k Electro-spun Fibers
Objective To investigate the morphology and material composition of Poloxamer188 composite PEG100k electro-spun fibers before and after loading docetaxel,as well as the drug solubilization and encapsulation after fibers hydration.Methods Do-cetaxel,Poloxamer188,and PEG100k were dissolved in dichloromethane to form co-solutions and be electro-spun.The composite contents of Poloxamer188 from 10%to 100%and the loading of docetaxel of 5%,10%,15%,and 20%were investigated.Scan-ning electron microscopy was used to investigate fiber morphology,and differential thermal analysis,thermogravimetric analysis,and X-ray diffraction were used to investigate materials recombination and drug loading.Under the hydration conditions of pure water/drug-loaded fiber 40/100 and 5/100(V/m,mL/mg)respectively,the former obtained liquid and the latter swelled.After centrifugation at 10 000 r/min for 3 min,solid precipitate and supernatant were obtained in the former and hydrogel precipitate and supernatant in the latter.The content of docetaxel in supernatant under two different treatment methods was determined by high performance liquid chromatography-ultraviolet spectrophotometry,and the percentage of solubilization and percentage of leakage were calculated respec-tively.Results The obtained electro-spun fibers are all less than 5μm in diameter,with uniform diameters and no bead structure.Recombination occurs between the materials,but there are diffraction peaks of PEG100k fragments on the fiber surface.In the liquid obtained after hydration,the solubilization percentage of fiber drug with 5%docetaxel load was the highest,and most samples were between 70%and80%.When the drug load increased to10%and15%,the solubilization percentage decreased to below20%,and when the drug load increased to20%,the solubilization percentage of most samples was close to0.With the increase of Poloxamer188 compound amount,the solubilization percentage of the 5%drug load series fiber first increased and then decreased,and the solubili-zation percentage of docetaxel in F-5%-40%could reach 80%.When docetaxel loading was 5%,the percentage of gel leakage obtained after hydration was greater than that of other drug loading conditions,but the percentage of leakage did not exceed 5%,and the per-centage of leakage was less than 2%when the drug loading was 10%,15%and 20%.Conclusion The PEG100k fiber containing docetaxel with ideal shape can be prepared by homogeneous solution electrospinning technology.The drug solubilization amount in the fiber after hydration can meet the pharmacopoeia standard.The loading amount of docetaxel and Poloxamer188 compound amount have obvious effects on the drug solubilization amount,and the leakage rate of the obtained hydration gel is very low.
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