Characterization And Release Behavior Of Docetaxel Loaded Poly L-lactic Acid ElectrosPun Fibers

ObjectiveA kind of surfactant with low toxicity,which can be implanted in vivo was screened out,and drug-loaded fiber which was degraded in vivo and had a sustained release effect by local implantation was prepared.The effects of different compounding ratios of surfactant and drug in fibers on fiber release were investigated.MethodElectrospun fibers were prepared by homogeneous spinning using nonyl alcohol ether,PEG 100,000,and Poloxamer188 as surfactants.The microscopic morphology of the three fibers was compared with a scanning electron microscope.The release behavior of different surfactants was analyzed and screened.The surfactant with the highest release amount and the best microscopic morphology was obtained.A solid dispersion was prepared using this surfactant as a carrier material,and its solubilization limit for the drug was investigated.The effects of docetaxel and surfactants on the microscopic morphology and release behavior of fibers under different composite ratios in the fibers were also investigated.The microscopic state was analyzed by physical characterization,and an in vitro analysis method was established to determine the content of the drug in the release medium at each sampling point,and the release curve was drawn and fitted.ResultsUsing Poloxamer188 as the surfactant can obtain continuous long fibers with uniform diameter and no bead string structure and the highest release amount.The solubilizing ability of solid dispersions prepared with this as the carrier material decreases with the increase of the drug compounding ratio.In docetaxel electrospun fibers,the release amount increases with the increase in the proportion of surfactant in the fiber.The results obtained after fitting the Korsmeyer-Pe PPas equation,found that the increase in Poloxamer188 has significant significance for increasing the porosity in the fiber and then increasing the percentage of drug release.With the increase of the compounding amount of the drug,the amount of drug release first increases and then decreases,and the compounding amount of the drug is 5%-15%.There are microcrystals in the initial release,followed by a dissolved state,and the compounding amount of 20%-25% is all crystalline status.This indicates that Poloxamer188 reached the solubilization limit for docetaxel in the specified system.ConclusionsPoloxamer188 is a non-toxic,non-hemolytic,excellent surfactant that can be injected intravenously.And using it as a surfactant can obtain long fibers with uniform diameter and continuous bead-free string structure.The release amount of docetaxel in the fiber increased with the increase of Poloxamer188 complex ratio.And reached the maximum when the drug compound ratio was 15%.The increase of Poloxamer188 is of great significance to the increase of porosity in the fiber,and then to the increase of drug release.However,as the compounding ratio of the drug increases,the combination of docetaxel and poly-L-lactic acid develops deeper,resulting in tighter binding and difficulty in solubilization.