Preparation and Evaluation of Arthemether Ternary Solid Dispersion Formulation Using Carbopol and Poloxamer as Polymers , 2023
Background: Solubility is a physicochemical property of drugs that plays a critical role in drug ... more Background: Solubility is a physicochemical property of drugs that plays a critical role in drug effectiveness. Without it, a drug substance cannot be absorbed, leading to low bioavailability. Bioavailability is the proportion of a drug which enters the circulation when introduced into the body and so is able to have a therapeutic effect. Artemether is a drug used for the treatment of malaria, but its use is limited by poor solubility. Aim: The aim of this study is to improve the solubility of artemether by formulating it into solid dispersion using two synthetic polymers, carbopol and poloxamer in combination at different ratios. Methods: Solid dispersion of artemether was prepared by solvent evaporation method using carbopol and poloxamer. The solubility and dissolution rate were determined. The formulation with the highest solubility (optimum formulation) was characterized using scanning electron microscope (SEM), differential scanning calorimetry (DSC) and fourier transform infrared-red spectroscopy (FTIR). Dissolution studies were carried out. Results: The formulation of artemether into solid dispersion increased its solubility by two and half fold. The solid dispersion formulation C6 has the highest solubility with a value of 328ug/mL and was selected as the optimum formulation. SEM analysis showed that the solid dispersion has irregular shape with a smooth surface while DSC thermograms reveal the phase transition of the crystalline nature of artemether to amorphous nature in the solid dispersion which accounts for the improved solubility of the solid dispersion. FTIR results show that there is no formation of new bonds in the solid dispersion and physical mixture. Conclusion: The study showed that solid dispersion formulation remarkably improved the solubility and dissolution of artemether which can lead to good bioavailability and better therapeutic outcome.
Preparation and Evaluation of Arthemether Ternary Solid Dispersion Formulation Using Carbopol and Poloxamer as Polymers , 2023
Background: Solubility is a physicochemical property of drugs that plays a critical role in drug ... more Background: Solubility is a physicochemical property of drugs that plays a critical role in drug effectiveness. Without it, a drug substance cannot be absorbed, leading to low bioavailability. Bioavailability is the proportion of a drug which enters the circulation when introduced into the body and so is able to have a therapeutic effect. Artemether is a drug used for the treatment of malaria, but its use is limited by poor solubility. Aim: The aim of this study is to improve the solubility of artemether by formulating it into solid dispersion using two synthetic polymers, carbopol and poloxamer in combination at different ratios. Methods: Solid dispersion of artemether was prepared by solvent evaporation method using carbopol and poloxamer. The solubility and dissolution rate were determined. The formulation with the highest solubility (optimum formulation) was characterized using scanning electron microscope (SEM), differential scanning calorimetry (DSC) and fourier transform infrared-red spectroscopy (FTIR). Dissolution studies were carried out. Results: The formulation of artemether into solid dispersion increased its solubility by two and half fold. The solid dispersion formulation C6 has the highest solubility with a value of 328ug/mL and was selected as the optimum formulation. SEM analysis showed that the solid dispersion has irregular shape with a smooth surface while DSC thermograms reveal the phase transition of the crystalline nature of artemether to amorphous nature in the solid dispersion which accounts for the improved solubility of the solid dispersion. FTIR results show that there is no formation of new bonds in the solid dispersion and physical mixture. Conclusion: The study showed that solid dispersion formulation remarkably improved the solubility and dissolution of artemether which can lead to good bioavailability and better therapeutic outcome.
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