Research articlewidely in vivo without a targeting effect, thus tetrandrine in this formulation does not concentrate highly in diseased organs or tissues [6][7] and usually causes pain or phlebitis. To improve pulmonary drug concentration to maximize its effectiveness and minimize the adverse side effects, tetrandrine polylactic acid microspheres with diameters of 7-15 μm were injected intravenously to achieve lung targeting [8]. This mechanism of lung targeting by injecting more than 7 μm microspheres occurs through mechanical filtration by the pulmonary capillaries, which can damage the lung permanently. Microspheres with diameters between 0.5-5 μm used for pulmonary inhalation could overcome this shortcoming. However, the controllability and uniformity of the microsphere size are closely related to the effects of pulmonary inhalation. The particle size is difficult to control for microspheres prepared by conventional methods, such as emulsification, ultrasonic emulsifying preparation and distribution [9].Recently, a novel method, the Shirasu Porous Glass (SPG) membrane emulsification technique, has been widely applied to the preparation of uniform-sized emulsions. Uniform droplet size and high drug encapsulation efficiency have been obtained by permeating a dispersed phase into a continuous phase through an SPG membrane at an adequate pressure [10][11][12][13][14].
Optimization and Evaluation of Monodispersed
AbstractTo improve pulmonary drug concentrations and to maximize the effectiveness and minimize the adverse side effects, uniformsized tetrandrine-loaded polylactide (PLA) microspheres with a suitable particle size for pulmonary inhalation were prepared by the Shirasu Porous Glass (SPG) membrane emulsification technique. The main parameters influencing PLA microsphere properties were investigated: transmembrane pressure, circulation speed, high hydrophilic-lipophilic balance (HLB value), PLA concentration and oil-water volume ratio. Narrowly size-distributed tetrandrine-loaded PLA microspheres were obtained with a high drug encapsulation efficiency of 81.0% and an average diameter of 3.16 μm under optimized conditions. The results of Fourier transform infrared, differential scanning calorimetry and powder X-ray diffraction revealed that tetrandrine would be either molecularly dispersed in the polymer or distributed in an amorphous form. Further, the in vitro drug release experiment confirmed that the uniform-sized tetrandrine-loaded PLA microspheres showed suppressed burst release. These studies provide a basis for the use of uniformly sized 3.16 μm tetrandrine-loaded PLA microspheres for pulmonary inhalation.