Thymosin β₄-plga Microspheres Development Of Ophthalmic Preparations

Thymosinβ4 (Thymosinβ4) is an polypeptide drugs to the injury of cornea,has a good therapeutic effect, use of less, effective. However, thymosinβ4 in aqueous solution, unstable, easily biodegradable, bio-low utilization rate. In order to overcome this shortcoming, the subjects developed thymosinβ4-PLGA microspheres in ophthalmic preparations.This experiment preparation Thymosinβ4 - PLGA microspheres with complex microemulsion method, using single-factor test and L9 (34) orthogonal design optimization of microspheres, i.e.:0.1g Tween-80 to join 500 Lthymosinβ4(10mg/mL) is dissolved in A liquid, PLGA soluble in Dichloromethane (200mg/mL) for B, A liquid added to B liquid, Eddy oscillation lmin into colostrum, then drop to 6% PVA solution 4mL, Eddy oscillation 3min into complex emulsions, and then injected 6mL of 6% PVA solution and stir 3h volatile organic solvents in 1000-1200r/min speed, centrifugation, washing 4-5 times, freeze drying, thymic factorβ4 -PLGA microspheres.Using HPLC to determin Thymosinβ4 content, Thymosinβ4 in 0.5 to 4.0μg wide,linear good (r=0.9997), precision was RSD=0.48%, method of recovery was 99.86-100.66% and reproducibility was RSD=0.78%, to the determination of the Thymosinβ4-PLGA microspheres, ThymosinP4 content accurate and reliable.Using SEM, grain size tester, DSC thermal analysis on evaluation, the results indicated that the microspheres forming, the surface is smooth, uniform particle size, and has formed a total of embedding.Drops of solution recipe to settlement volume ratio, microspheres granularity, redispersible for evaluation, drops to filter solution accessories. Optimization of prescription:0.1% sodium hyaluronate, phosphate buffer (pH6.5), 1g/L NaCl. To rabbit as a model, take long-term stimulation and continuous stimulation and the results of the stimulation, as bland on the eyes.Thymosinβ4-PLGA microspheres preparation process is simple, good stability and high bio-availability, carrier materials, PLGA has good biodegradability, side effects and so on.