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Solubility and dissolution performances of spray-dried solid dispersion of Efavirenz in Soluplus.
Drug Dev Ind Pharm. 2017 Jan; 43(1):42-54.DD

Abstract

Efavirenz (EFV), a first-line anti-HIV drug largely used as part of antiretroviral therapies, is practically insoluble in water and belongs to BCS class II (low solubility/high permeability). The aim of this study was to improve the solubility and dissolution performances of EFV by formulating an amorphous solid dispersion of the drug in polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®) using spray-drying technique. To this purpose, spray-dried dispersions of EFV in Soluplus® at different mass ratios (1:1.25, 1:7, 1:10) were prepared and characterized using particle size measurements, SEM, XRD, DSC, FTIR and Raman microscopy mapping. Solubility and dissolution were determined in different media. Stability was studied at accelerated conditions (40 °C/75% RH) and ambient conditions for 12 months. DSC and XRD analyses confirmed the EFV amorphous state. FTIR spectroscopy analyses revealed possible drug-polymer molecular interaction. Solubility and dissolution rate of EFV was enhanced remarkably in the developed spray-dried solid dispersions, as a function of the polymer concentration. Spray-drying was concluded to be a proper technique to formulate a physically stable dispersion of amorphous EFV in Soluplus®, when protected from moisture.

Authors+Show Affiliations

a Mines Albi, CNRS , Centre RAPSODEE, Campus Jarlard, Université de Toulouse , Albi , France. b Department of Pharmaceutics Sciences, Faculty of Pharmacy , Federal University of Pernambuco , Pernambuco , PE , Brazil.b Department of Pharmaceutics Sciences, Faculty of Pharmacy , Federal University of Pernambuco , Pernambuco , PE , Brazil.a Mines Albi, CNRS , Centre RAPSODEE, Campus Jarlard, Université de Toulouse , Albi , France.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27349377

Citation

Lavra, Zênia Maria Maciel, et al. "Solubility and Dissolution Performances of Spray-dried Solid Dispersion of Efavirenz in Soluplus." Drug Development and Industrial Pharmacy, vol. 43, no. 1, 2017, pp. 42-54.
Lavra ZM, Pereira de Santana D, Ré MI. Solubility and dissolution performances of spray-dried solid dispersion of Efavirenz in Soluplus. Drug Dev Ind Pharm. 2017;43(1):42-54.
Lavra, Z. M., Pereira de Santana, D., & Ré, M. I. (2017). Solubility and dissolution performances of spray-dried solid dispersion of Efavirenz in Soluplus. Drug Development and Industrial Pharmacy, 43(1), 42-54. https://doi.org/10.1080/03639045.2016.1205598
Lavra ZM, Pereira de Santana D, Ré MI. Solubility and Dissolution Performances of Spray-dried Solid Dispersion of Efavirenz in Soluplus. Drug Dev Ind Pharm. 2017;43(1):42-54. PubMed PMID: 27349377.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Solubility and dissolution performances of spray-dried solid dispersion of Efavirenz in Soluplus. AU - Lavra,Zênia Maria Maciel, AU - Pereira de Santana,Davi, AU - Ré,Maria Inês, Y1 - 2016/07/17/ PY - 2016/6/29/pubmed PY - 2017/5/24/medline PY - 2016/6/29/entrez KW - Efavirenz KW - amorphous KW - dissolution KW - drug solubility KW - solid dispersion KW - spray drying KW - stability SP - 42 EP - 54 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 43 IS - 1 N2 - Efavirenz (EFV), a first-line anti-HIV drug largely used as part of antiretroviral therapies, is practically insoluble in water and belongs to BCS class II (low solubility/high permeability). The aim of this study was to improve the solubility and dissolution performances of EFV by formulating an amorphous solid dispersion of the drug in polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®) using spray-drying technique. To this purpose, spray-dried dispersions of EFV in Soluplus® at different mass ratios (1:1.25, 1:7, 1:10) were prepared and characterized using particle size measurements, SEM, XRD, DSC, FTIR and Raman microscopy mapping. Solubility and dissolution were determined in different media. Stability was studied at accelerated conditions (40 °C/75% RH) and ambient conditions for 12 months. DSC and XRD analyses confirmed the EFV amorphous state. FTIR spectroscopy analyses revealed possible drug-polymer molecular interaction. Solubility and dissolution rate of EFV was enhanced remarkably in the developed spray-dried solid dispersions, as a function of the polymer concentration. Spray-drying was concluded to be a proper technique to formulate a physically stable dispersion of amorphous EFV in Soluplus®, when protected from moisture. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/27349377/Solubility_and_dissolution_performances_of_spray_dried_solid_dispersion_of_Efavirenz_in_Soluplus_ L2 - https://www.tandfonline.com/doi/full/10.1080/03639045.2016.1205598 DB - PRIME DP - Unbound Medicine ER -