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• W851898560 abstract "_____________________________________________________________ Cristina Maria Franzini ABSTRACT The fungal infections treatment imposes many difficulties mainly because the intravenous therapy requires administration of solubilized or dispersed drug in particles of smaller dimension beyond the need for hospitalization. Despite its low solubility and serious adverse effects the amphotericin B (AmB) remains one of the most effective antibiotics to the treatment. Microemulsions allow circumvent these problems and provide oral administration. Therefore these lipid formulations containing AmB have been increasingly studied. Additionally, the formation of inclusion complexes with cyclodextrins (CDs) has also been promising in developing new dosage forms. In this work the formation parameters of microemulsions (MEs) containing soybean phosphatidylcholine (FS), Tween-20 (Tw) and sodium oleate (SO) as surfactant and cholesterol (CHO) as oil phase and the formation of inclusion complexes with different CDs derivatives and their incorporation into MEs were studied. The pseudo ternary phase diagram was built in order to characterize MEs. The rheological behavior and internal structure were evaluated and characterized by dynamic light scattering. The effect of the proportion of surfactant and oil phase in the diameter of the internal phase in systems with or without AmB was evaluated. Therefore the contribution of the oil phase and surfactant in the drug loading eficience was studied. The Solubility diagram of AmB in CDs was developed and its stability constants determined. The preparation of ME containing CDs in its aqueous phase, the incorporation AmB parameters and the release studies were performed followed by thermal analysis, x-ray (XRD) diffraction and nuclear magnetic resonance (NMR). The results reveal the MEs formation in regions containing up to 30% surfactant and about 11% of the oil phase. Under polarized light, the interest systems showed a dark background and lamellar structure and pseudoplastic with thixotropy predominantly behavior. The AmB maximum incorporation in MEs was dependent on the surfactant and oil phase ratio with 2.37 and 2.34 mg/mL respectively. The droplets average diameter was increased by the AmB incorporation in all samples. However, when the proportion of surfactant in MEs containing or not AmB increased, these diameters decreased. It was also observed an AmB interaction increased with CD, MECD, HPCD and SBCD, having the SBCD the predominant effect, which is in agreement with the stability constants values found of 11.82, 40.40, 919.8 and 5047 M. The AmB incorporation in binary systems containing MEs:CDs was more efficient being 2,41; 2,81; 3,24 e 4,38 mg/mL to CD, MECD, HPCD e SBCD respectively. Thermogravimetric analysis showed a strong interaction between the drug and the studied CDs respectively suggesting that the existence of inclusion complexes formation. Additionally ME:AmB provides greater protection of the drug against high temperatures reducing the possibility of degradation. The NMR and XRD also showed the presence of AmB in the obtained complexes. The release studies showed a time release prolongation in 12 hours of study for the ME systems without the CD being exacerbated by its presence following the same relation mentioned above being increased substantially relative to free drug trade and the commercial form anforicin®. It follows that so that the systems studied presents promising in the AmB transport and sustained release." @default.
• W851898560 created "2016-06-24" @default.
• W851898560 creator A5014654669 @default.
• W851898560 date "2010-08-18" @default.
• W851898560 modified "2023-09-24" @default.
• W851898560 title "Complexos de inclusão de anfotericina B com derivados de ciclodextrinas e sua incorporação em microemulsões lipídicas biocompatíveis" @default.
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