The effect of surfactant type and concentration on physicochemical properties of carvedilol solid dispersions prepared by wet milling method

The main objective of the present research was to apply wet milling technique to prepare solid dispersions (SDs) of a poorly water-soluble compound, carvedilol (CA), in the presence of pluronic F68 (F68) and myrj 52 in order to enhance drug dissolution. The process enabled the preparation of SDs without using any toxic organic solvents. SDs with different CA: surfactant ratios were prepared by wet milling followed by freeze-drying method and evaluated for their particle size and dissolution. They were also characterized based on X-ray diffraction (XRD), differential scanning calorimetry (DSC), fourier transform infrared (FTIR) spectroscopy, scanning electron microscope (SEM) and saturated solubility. The effect of type of cryoprotectant on the dissolution and particle size of SDs was also studied.Wet milling process resulted in reduced particle size depending on the type of surfactant. The significant drug dissolution and saturated solubility enhancement was observed for milled SD formulations. Myrj had a greater impact compared to F68, in this regard. Dissolution efficiencies (DE30) obtained for the myrj-included SDs were up to 8.2-fold higher than that of untreated CA. Type of cryoprotectant also affected the drug dissolution. Based on the results, partial amorphization occurred in wet-milled samples as confirmed by XRD and DSC analysis.Our findings showed that the use of an appropriate surfactant along with wet-milling method could be an effective approach for improving th...
Source: Iranian Journal of Pharmaceutical Research - Category: Drugs & Pharmacology Source Type: research