Purpose. The aim of this work was the optimization of the preparation process parameters for the development of Capreomycin Sulfate (CS) liposomal formulations as potential aerosol antitubercular agents. Methods. Dipalmitoylphosphatidylcholine (DPPC), hydrogenated phosphatidylcholine (HPC) and distearoylphosphatidylcholine (DSPC) were used for liposome preparation. Freeze-thawing method was chosen for CS encapsulation. Peptide entrapment, size and morphology were evaluated by UV spectrophotometry, photocorrelation spectroscopy (PCS) and transmission electron microscopy (TEM) respectively. 23 full factorial design was employed to evaluate the optimal conditions for CS encapsulation. Results. The peptide content oscillated between 1 to 8%. Vesicles showed a narrow size distribution, with average diameters around 1 ƒÝm and a good morphology. A slight effect on size of freeze and thawing cycles was observed. A linear regression model was generated for each liposomal system. Diagnostics, ANOVA and check point analysis revealed high predictivity of the model. Response surface methodology was useful to establish the optimal conditions so as to obtain an increase in CS entrapment. DPPC liposomes were found to provide a faster increase and higher values of CS content. Conclusion. Optimal conditions for developing CS loaded liposomes were assessed and a predictive model was obtained. The 23 factorial design was a time-saving and low-cost method helpful in developing new CS liposomal formulations for a possible application in aerosol antitubercular therapies.

Development of liposomal capreomycin sulfate formulations: mathematical modeling of peptide encapsulation

GIOVAGNOLI, Stefano;RICCI, Maurizio;BLASI, PAOLO;SCHOUBBEN, Aurelie Marie Madeleine;PERIOLI, Luana;ROSSI, Carlo
2005

Abstract

Purpose. The aim of this work was the optimization of the preparation process parameters for the development of Capreomycin Sulfate (CS) liposomal formulations as potential aerosol antitubercular agents. Methods. Dipalmitoylphosphatidylcholine (DPPC), hydrogenated phosphatidylcholine (HPC) and distearoylphosphatidylcholine (DSPC) were used for liposome preparation. Freeze-thawing method was chosen for CS encapsulation. Peptide entrapment, size and morphology were evaluated by UV spectrophotometry, photocorrelation spectroscopy (PCS) and transmission electron microscopy (TEM) respectively. 23 full factorial design was employed to evaluate the optimal conditions for CS encapsulation. Results. The peptide content oscillated between 1 to 8%. Vesicles showed a narrow size distribution, with average diameters around 1 ƒÝm and a good morphology. A slight effect on size of freeze and thawing cycles was observed. A linear regression model was generated for each liposomal system. Diagnostics, ANOVA and check point analysis revealed high predictivity of the model. Response surface methodology was useful to establish the optimal conditions so as to obtain an increase in CS entrapment. DPPC liposomes were found to provide a faster increase and higher values of CS content. Conclusion. Optimal conditions for developing CS loaded liposomes were assessed and a predictive model was obtained. The 23 factorial design was a time-saving and low-cost method helpful in developing new CS liposomal formulations for a possible application in aerosol antitubercular therapies.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11391/42210
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