Influence of Drug Loading Methods on the Loading Efficiency and Dissolution Performance of Mesoporous Polymeric Carriers
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Abstract
Lower solubility of drugs like felodipine is major contributing factor towards its lower bioavailability. Mesoporous polymeric carriers can increase drug dissolution as well as promote controlled release. In this study, felodipine was loaded on mesoporous mesosol polymeric particles through two different methods: rotary evaporation and solvent impregnation method. Further, the role of choice of solvent in case of the later was evaluated by using two solvents: ethanol and isopropanol. The methods were compared through structural effect on the drug and carrier using DSC while release studies were carried out through USP 2 apparatus at pH 6.5. The DSC studies confirmed amorphous form of felodipine when loaded on mesosol in drug: carrier ratios 1:3, 1:4 and 1:5 through both loading methods. Both loading methods further confirmed no transformation of drug when in physical mixture of carrier. Highest loading efficiency was obtained for 1:3 ratio for rotary evaporation method while 1:4 ratio showed highest loading efficiency in case of formulations prepared through solvent impregnation method. Solvent impregnation methods demonstrated comparatively higher loading efficiency. The incorporation of Felodipine in the microparticles led to enhanced solubility of the drug and showed controlled release for 120 minutes. The formulations with lower drug amount (1:5 ratio drug: carrier) showed highest release in case of both methods of loading. The study establishes both rotary evaporation and solvent impregnation methods to be effective for loading Felodipine on mesosol polymeric microparticles. It further ensures complete amorphization of drug in the mesoporous carrier. While using isopropanol leads to higher loading efficiency, cumulative release rates are higher for formulations using ethanol as solvent.