| Objective:Isotopic carrier is poly(ethylene glycol)-poly(dl-lactide)mPEG-PLA(Mr 8000). Drug-loaded micelles were prepared using atorvastatin calcium(AC) as the model drug. In this article,we prepared AC-mPEG-PLA polymer micelles, intended to improve the solubility of drugs in water, bioavailability and clinical therapeutic effect.Methods:By the self-assembled polymer micelles are prepared by solvent evaporation method. Orthogonal L9(34)experiment design was used, with acetone and ethanol, the proportion of drug and mPEG-PLA polymer ratio.The distribution of morphology, particle size and encapsulation efficiency of quality evaluation for the optimization of preparation process of polymer micelle.Determination of AC-mPEG-PLA micelles in vitro cumulative release. DSC and XRD analysis drug of morphological changes. Pharmacokinetic and pharmacodynamic studies.Results:The best preparation for polymer micelles as:acetone and ethanol ratio was 6:l,the ratio of organic phase the aqueous phase was 1:5, drug and polymer ratio was 1:5, Spherical,polymeric micelles prepared as the rule of uniform size, no adhesion. The average particle diameter was 42.56±0.89nm, polydispersity was 0.256±0.012, Zeta potential was 52.05mV; Average encapsulation efficiency was 95.16±1.32%, drug loading was 13.256±1.84%. The best lyoprotectant was 4% of glucose; DSC and XRD analysis showed that nanoparticles formed.The solubility curve can be seen, polymeric micelles increased release in vitro. Pharmacokinetic study revealed that AC -mPEG-PLA polymeric micelles relative bioavailability is increased. |
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