Preparation Of Drug-loaded Polybutylcyanoacrylate Nanoparticles

Objective:To prepare polybutylcyanoacrylate(PBCA) nanocarriers with optimized process,double-located with Tween80 and(or) polyethylene glycol(PEG)20000,to further prepare fotemustine polybutylcyanoacrylate nanoparticles(FCNU-PBCA-NP) and temozolomide polybutylcyanoacrylate nanoparticles(TMZ-PBCA-NP).Method:(1)Double-coated PBCA nanocarries was prepared by emulsion polymerization method with butylα-cyanoacrylate(BCA) as carrier materials, Tween80 and(or) PEG20000 as surfactants,and the procedure was optimized by both single factor test and uniform design test.(2) To further prepare fotemustine polybutylcyanoacrylate nanoparticles(FCNU-PBCA-NP) and temozolomide polybutylcyanoacrylate nanoparticles(TMZ-PBCA-NP),and optimize the preparing technology according to the particle size and the embedding ration(ER).Results:(1) The solution of double-coated PBAC-NP under optimum conditions was milk-white colloidal solution and the nanocarriers were circular and non-adhesion through transmission electronic microscopy.The average particle size was about 137.7nm and particle density index(PDI)was about 0.190.(2) The solution of fotemustine polybutylcyanoacrylate nanoparticles(FCNU-PBCA-NP) under optimum conditions was milk-white colloidal solution and the nanocarriers were circular and non-adhesion through transmission electronic microscopy.The average particle size was about(124.6±5.2)nm and particle density index(PDI) was about 0.07～0.16.the average embedding ration(ER) was about(64.12±2.36)%.(3)The solution of temozolomide polybutylcyanoacrylate nanoparticles(TMZ-PBCA-NP) under optimum conditions was milk-white colloidal solution and the nanocarriers were circular and non-adhesion through transmission electronic microscopy.The average particle size was about 125.1nm and particle density index(PDI) was about 0.098.the average embedding ration(ER) was about 83.02%.Conclusion:Double-coated PBCA nanocarries was prepared by emulsion polymerization method with butylα-cyanoacrylate(BCA) as carrier materials, Tween80 and(or) PEG20000 as surfactants for the first time,and the procedure was optimized by uniform design test.fotemustine polybutylcyanoacrylate nanoparticles (FCNU-PBCA-NP) and temozolomide polybutylcyanoacrylate nanoparticles (TMZ-PBCA-NP) were successfully prepared On this basis.They have provided a new direction for fotemutine and temozolomide dosage forms,and laid the foundation for Research for Sustained release and targeting of brain.They have not been reported at home and abroad at present.