The present study relates to enhancing the dosing efficiency of pharmaceutical dry powder formulations administered by pulmonary inhalation. In particular, the study relates to the provision of dry powder inhalers (DPI) by forming nanosized particles of salbutamol sulfate (SBM) in order to augment the drug penetrability and deposition in the lungs. SBM, an antiasthmatic was selected to be developed into a nanosized formulation by different techniques like solvation, high-pressure homogenization, and spray drying, which were then compared on the basis of particle shape, particle size, and particle size distribution. In case of solvation method the nanosuspension was prepared by dispersing SBM into a nonsolvent and adding Tween-80 as a surfactant to prevent the agglomeration, the particles obtained therein were in the range of 2-10 mu. The second attempt was made by passing the suspension of SBM through high-pressure homogenizer at 10,000-15,000 psi. A treatment of six cycles of homogenization in presence of a Tween-80 as surfactant was found to give a nanosuspension within a size range 50-100 nm. The only drawback seemed with this technique was the low-product yield and high-processing time (3-4 h). In order to overcome this drawback spray-drying technique was further explored; the solution of SBM containing Tween-80 was stirred on magnetic stirrer at 1,200 rpm and finally dried by using spray dryer at an inlet and outlet temperature of 75 degrees C and 56 degrees C, respectively. The feed rate for spray dryer was kept to be 91 ml/h. The sample was collected and analyzed for particle size distribution which was found to be in the range of 50-100 nm. Keeping in view the positive outcomes in terms of higher yield and lower processing time, the spray-drying technique was taken to give the optimized formulation. Nanosized particles, thus obtained were evaluated for particle size, surface topology and particles size distribution, by Transmission Electron Microscopy (TEM), Scanning Electron Microscopy (SEM), and Quasi-elastic light scattering (QELS) technique, respectively. The nanosized particles were subjected to investigate changes on the physical stability of the powder, for this different analytical method was used as: Fourier transform infrared spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC) and X-ray diffraction (XRD) analysis and thus the result indicates that there was no physical disparity when compared with the commercial SBM sample.