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Characterization of solid dispersions of itraconazole and vitamin E TPGS prepared by microwave technology.
Future Med Chem. 2010 Feb; 2(2):237-46.FM

Abstract

BACKGROUND

This study describes the influence of microwave irradiation (MW) on the preparation and properties of solvent-free solid dispersions (SDs) employing vitamin E D-α-tocopheryl polyethylene glycol (TPGS) 1000 succinate, with itraconazole as a model drug.

MATERIALS AND METHODS

Itraconazole is characterized by low aqueous solubility and vitamin E TPGS was chosen as the surfactant carrier for the formulation of MW solid dispersions in different ratios. Their physicochemical characteristics were investigated by means of powder x-ray diffraction (PXRD), differential scanning calorimetry (DSC), diffuse reflectance infrared Fourier transform (DRIFT) spectroscopy and hot-stage microscopy. Comparison with the corresponding physical mixtures and the drug alone allowed the relationship between influence of the technological process on physicochemical and morphological properties of the systems to be examined.

RESULTS

PXRD data confirmed the absence of phase transitions in the solid state of the drug subjected to MW alone. On the other hand, an amorphous form of the drug was obtained in the solid dispersion with the highest content of carrier investigated (1:3 w/w). All the SDs showed an improvement in the solubility and dissolution profile of the drug, with the best results obtained in the case of the 1:3 w/w SD. This was related to an interaction between the drug and the carrier with a complex that formed due to favorable H bonds, as demonstrated by DRIFT analysis.

CONCLUSION

It was demonstrated that the amorphization of the drug led to an increase in wettability and a significant improvement in bioavailability. Therefore, SDs obtained by MW technique using vitamin E TPGS as carrier provide a promising way to increase the dissolution rate and solubility of poorly bioavailable drugs.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, University of Trieste, Piazzale Europa 1, 34127 Trieste, Italy.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

21426191

Citation

Moneghini, Mariarosa, et al. "Characterization of Solid Dispersions of Itraconazole and Vitamin E TPGS Prepared By Microwave Technology." Future Medicinal Chemistry, vol. 2, no. 2, 2010, pp. 237-46.
Moneghini M, De Zordi N, Solinas D, et al. Characterization of solid dispersions of itraconazole and vitamin E TPGS prepared by microwave technology. Future Med Chem. 2010;2(2):237-46.
Moneghini, M., De Zordi, N., Solinas, D., Macchiavelli, S., & Princivalle, F. (2010). Characterization of solid dispersions of itraconazole and vitamin E TPGS prepared by microwave technology. Future Medicinal Chemistry, 2(2), 237-46. https://doi.org/10.4155/fmc.09.166
Moneghini M, et al. Characterization of Solid Dispersions of Itraconazole and Vitamin E TPGS Prepared By Microwave Technology. Future Med Chem. 2010;2(2):237-46. PubMed PMID: 21426191.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Characterization of solid dispersions of itraconazole and vitamin E TPGS prepared by microwave technology. AU - Moneghini,Mariarosa, AU - De Zordi,Nicola, AU - Solinas,Dario, AU - Macchiavelli,Stefano, AU - Princivalle,Francesco, PY - 2011/3/24/entrez PY - 2011/3/24/pubmed PY - 2011/8/31/medline SP - 237 EP - 46 JF - Future medicinal chemistry JO - Future Med Chem VL - 2 IS - 2 N2 - BACKGROUND: This study describes the influence of microwave irradiation (MW) on the preparation and properties of solvent-free solid dispersions (SDs) employing vitamin E D-α-tocopheryl polyethylene glycol (TPGS) 1000 succinate, with itraconazole as a model drug. MATERIALS AND METHODS: Itraconazole is characterized by low aqueous solubility and vitamin E TPGS was chosen as the surfactant carrier for the formulation of MW solid dispersions in different ratios. Their physicochemical characteristics were investigated by means of powder x-ray diffraction (PXRD), differential scanning calorimetry (DSC), diffuse reflectance infrared Fourier transform (DRIFT) spectroscopy and hot-stage microscopy. Comparison with the corresponding physical mixtures and the drug alone allowed the relationship between influence of the technological process on physicochemical and morphological properties of the systems to be examined. RESULTS: PXRD data confirmed the absence of phase transitions in the solid state of the drug subjected to MW alone. On the other hand, an amorphous form of the drug was obtained in the solid dispersion with the highest content of carrier investigated (1:3 w/w). All the SDs showed an improvement in the solubility and dissolution profile of the drug, with the best results obtained in the case of the 1:3 w/w SD. This was related to an interaction between the drug and the carrier with a complex that formed due to favorable H bonds, as demonstrated by DRIFT analysis. CONCLUSION: It was demonstrated that the amorphization of the drug led to an increase in wettability and a significant improvement in bioavailability. Therefore, SDs obtained by MW technique using vitamin E TPGS as carrier provide a promising way to increase the dissolution rate and solubility of poorly bioavailable drugs. SN - 1756-8927 UR - https://www.unboundmedicine.com/medline/citation/21426191/Characterization_of_solid_dispersions_of_itraconazole_and_vitamin_E_TPGS_prepared_by_microwave_technology_ L2 - https://www.future-science.com/doi/10.4155/fmc.09.166?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -