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Physical-chemical properties of furosemide nanocrystals developed using rotation revolution mixer.
Pharm Dev Technol. 2016 Nov; 21(7):812-822.PD

Abstract

Recently, several approaches have been reported to improve the dissolution rate and bioavailability of furosemide, a class IV drug. However, to the best of our knowledge, none of them proposed nanocrystals. In the last decade, nanocrystals successfully addressed solubility issues by increasing surface area and saturation solubility, both leading to an increase in the dissolution rate of poor water soluble drugs. The preparation of furosemide nanocrystals was by a rotation revolution mixer method. Size distribution and morphology were performed using laser diffraction and scanning electron microscopy, respectively. In addition, differential scanning calorimetry, thermogravimetry, X-ray powder diffraction (XRD) and low frequency shift-Raman spectroscopy allowed investigating the thermal properties and crystalline state. Solubility saturation and intrinsic dissolution rate (IDR) studies were conducted. The thermal analysis revealed lower melting range for the nanocrystals comparing to furosemide. Moreover, a slight crystalline structure change to the amorphous state was observed by XRD and confirmed by low frequency shift Raman. The particle size was reduced to 231 nm with a polydispersity index of 0.232, a 30-fold reduction from the original powder. Finally, the saturation solubility and IDR showed a significant increase. Furosemide nanocrystals showed potential for development of innovative formulations as an alternative to the commercial products.

Authors+Show Affiliations

a Faculty of Pharmaceutical Sciences , University of São Paulo , São Paulo , São Paulo , Brazil.b Thinky Corporation , Tokyo , Japan.c Course of Pharmacy, Department of Biochemistry , Institute of Biology, State University of Campinas , Campinas , São Paulo , Brazil , and.a Faculty of Pharmaceutical Sciences , University of São Paulo , São Paulo , São Paulo , Brazil.d Faculty of Pharmacy and Pharmaceutical Sciences , Katz Group-Rexall Centre for Pharmacy & Health Research, University of Alberta , Edmonton , Alberta , Canada.d Faculty of Pharmacy and Pharmaceutical Sciences , Katz Group-Rexall Centre for Pharmacy & Health Research, University of Alberta , Edmonton , Alberta , Canada.d Faculty of Pharmacy and Pharmaceutical Sciences , Katz Group-Rexall Centre for Pharmacy & Health Research, University of Alberta , Edmonton , Alberta , Canada.a Faculty of Pharmaceutical Sciences , University of São Paulo , São Paulo , São Paulo , Brazil.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27825283

Citation

Barbosa, Sávio Fujita, et al. "Physical-chemical Properties of Furosemide Nanocrystals Developed Using Rotation Revolution Mixer." Pharmaceutical Development and Technology, vol. 21, no. 7, 2016, pp. 812-822.
Barbosa SF, Takatsuka T, Tavares GD, et al. Physical-chemical properties of furosemide nanocrystals developed using rotation revolution mixer. Pharm Dev Technol. 2016;21(7):812-822.
Barbosa, S. F., Takatsuka, T., Tavares, G. D., Araújo, G. L., Wang, H., Vehring, R., Löbenberg, R., & Bou-Chacra, N. A. (2016). Physical-chemical properties of furosemide nanocrystals developed using rotation revolution mixer. Pharmaceutical Development and Technology, 21(7), 812-822.
Barbosa SF, et al. Physical-chemical Properties of Furosemide Nanocrystals Developed Using Rotation Revolution Mixer. Pharm Dev Technol. 2016;21(7):812-822. PubMed PMID: 27825283.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Physical-chemical properties of furosemide nanocrystals developed using rotation revolution mixer. AU - Barbosa,Sávio Fujita, AU - Takatsuka,Takayuki, AU - Tavares,Guilherme Diniz, AU - Araújo,Gabriel Lima Barros, AU - Wang,Hui, AU - Vehring,Reinhard, AU - Löbenberg,Raimar, AU - Bou-Chacra,Nádia Araci, Y1 - 2015/08/31/ PY - 2016/11/10/entrez PY - 2016/11/9/pubmed PY - 2017/3/16/medline KW - Dissolution rate KW - drug delivery systems KW - high-energy milling KW - nanocrystals KW - poorly water-soluble drug SP - 812 EP - 822 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 21 IS - 7 N2 - Recently, several approaches have been reported to improve the dissolution rate and bioavailability of furosemide, a class IV drug. However, to the best of our knowledge, none of them proposed nanocrystals. In the last decade, nanocrystals successfully addressed solubility issues by increasing surface area and saturation solubility, both leading to an increase in the dissolution rate of poor water soluble drugs. The preparation of furosemide nanocrystals was by a rotation revolution mixer method. Size distribution and morphology were performed using laser diffraction and scanning electron microscopy, respectively. In addition, differential scanning calorimetry, thermogravimetry, X-ray powder diffraction (XRD) and low frequency shift-Raman spectroscopy allowed investigating the thermal properties and crystalline state. Solubility saturation and intrinsic dissolution rate (IDR) studies were conducted. The thermal analysis revealed lower melting range for the nanocrystals comparing to furosemide. Moreover, a slight crystalline structure change to the amorphous state was observed by XRD and confirmed by low frequency shift Raman. The particle size was reduced to 231 nm with a polydispersity index of 0.232, a 30-fold reduction from the original powder. Finally, the saturation solubility and IDR showed a significant increase. Furosemide nanocrystals showed potential for development of innovative formulations as an alternative to the commercial products. SN - 1097-9867 UR - https://www.unboundmedicine.com/medline/citation/27825283/Physical_chemical_properties_of_furosemide_nanocrystals_developed_using_rotation_revolution_mixer_ L2 - https://www.tandfonline.com/doi/full/10.3109/10837450.2015.1063650 DB - PRIME DP - Unbound Medicine ER -