Plasticizers and their effects on microencapsulation process by spray-drying in an aqueous system

Microencapsulated theophylline particles were prepared by an aqueous spray-drying process using hydroxypropylmethylcellulose. The effect of different plasticizers, triethylcitrate, polyethylene glycol, propylene glycol, glycerin and citric acid, was investigated. Triethylcitrate, a water-insoluble plasticizer, produced a porous honeycomb-like microcapsule wall resulting in rapid drug release. The presence of the plasticizers also influenced crystallization of the drug. The formation of a solid drug dispersion was observed with the addition of citric acid or glycerin. Changes in the pH of liquid feed caused by the plasticizer had an effect on the product dissolution profile, but this was not a major factor. Formation of pores due to leaching of plasticizers during dissolution enhanced drug release. Flow property measurements indicated that the plasticizers also affect the cohesiveness of the spray-dried products. Compared to the microcapsules formed without any plasticizers, propylene glycol, glycerin and citric acid appeared to be beneficial to the microcapsule wall formation, with microcapsules containing citric acid having the slowest drug release.