Polymeric behavior evaluation of PVP K30-poloxamer binary carrier for solid dispersed nisoldipine by experimental design

摘要

Abstract Context: High melting point polymeric carrier without plasticizer is unacceptable for solid dispersion (SD) by melting method. Combined polymer-plasticizer carrier significantly affects drug solubility and tableting property of SD. Objective: To evaluate and optimize the combined effect of a binary carrier consisting PVP K30 and poloxamer 188, on nisoldipine solubility and tensile strength of amorphous SD compact (SD_(compact)) by experimental design. Materials and methods: SD of nisoldpine (SD_(nisol)) was prepared by melt mixing with different PVP K30 and poloxamer amount. A 32 factorial design was employed using nisoldipine solubility and tensile strength of SD_(compact) as response variables. Statistical optimization bydesign expert software, and SD_(nisol) characterization using ATR FTIR, DSC and microscopy were done. Results: PVP K30:poloxamer, at a ratio of 3.73:6.63, was selected as the optimized combination of binary polymeric carrier resulting nisoldipine solubility of 115 ng/mL and tensile strength of 1.19 N/m2. Discussion: PVP K30 had significant positive effect on both responses. Increase in poloxamer concentration after a certain level decreased nisoldipine solubility and tensile strength of SD_(compact) Conclusion: An optimized PVP K30-poloxamer binary composition for SD carrier was developed. Tensile strength of SD_(compact) can be considered as a response for experimental design to optimize SD.