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Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method.
Drug Dev Ind Pharm. 2018 May; 44(5):750-756.DD

Abstract

β-lapachone (βlap) has shown potential use in various medical applications. However, its poor solubility has limited its systemic administration and clinical applications. The aim of this work is to develop solid dispersions of βlap using poly (ethylene glycol) (PEG 6000) and polyvinylpyrrolidone (PVP K30) as hydrophilic polymers and evaluate the dissolution rate in aqueous medium. Solid dispersions were prepared by solvent evaporation method using different weight ratios of βlap and hydrophilic polymer (1:1, 1:2, and 1:3). Characterization performed by differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, and scanning electron microscopy showed that βlap was molecularly dispersed within the polymer matrix. The in vitro dissolution tests showed an enhancement in the dissolution profile of βlap as solid dispersions prepared in both PVP and PEG, although the former showed better results. The drug:polymer ratio influenced βlap dissolution rate, as higher amounts of hydrophilic polymer led to enhanced drug dissolution. Thus, this study demonstrated that solid dispersions of βlap in PVP offers an effective way to overcome the poor dissolution of βlap.

Authors+Show Affiliations

a Department of Pharmacy , University of Rio Grande do Norte , Natal , Rio Grande do Norte , Brazil.a Department of Pharmacy , University of Rio Grande do Norte , Natal , Rio Grande do Norte , Brazil.a Department of Pharmacy , University of Rio Grande do Norte , Natal , Rio Grande do Norte , Brazil.b Graduate Program in Biotechnology , Laureate International Universities, Universidade Potiguar - UnP , Natal , Rio Grande do Norte , Brazil.c Department of Chemistry , Federal Rural University of Pernambuco , Recife , Pernambuco , Brazil.c Department of Chemistry , Federal Rural University of Pernambuco , Recife , Pernambuco , Brazil.a Department of Pharmacy , University of Rio Grande do Norte , Natal , Rio Grande do Norte , Brazil.a Department of Pharmacy , University of Rio Grande do Norte , Natal , Rio Grande do Norte , Brazil.a Department of Pharmacy , University of Rio Grande do Norte , Natal , Rio Grande do Norte , Brazil.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29206496

Citation

Dos Santos, Klecia M., et al. "Development of Solid Dispersions of Β-lapachone in PEG and PVP By Solvent Evaporation Method." Drug Development and Industrial Pharmacy, vol. 44, no. 5, 2018, pp. 750-756.
Dos Santos KM, Barbosa RM, Vargas FGA, et al. Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method. Drug Dev Ind Pharm. 2018;44(5):750-756.
Dos Santos, K. M., Barbosa, R. M., Vargas, F. G. A., de Azevedo, E. P., Lins, A. C. D. S., Camara, C. A., Aragão, C. F. S., Moura, T. F. L. E., & Raffin, F. N. (2018). Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method. Drug Development and Industrial Pharmacy, 44(5), 750-756. https://doi.org/10.1080/03639045.2017.1411942
Dos Santos KM, et al. Development of Solid Dispersions of Β-lapachone in PEG and PVP By Solvent Evaporation Method. Drug Dev Ind Pharm. 2018;44(5):750-756. PubMed PMID: 29206496.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method. AU - Dos Santos,Klecia M, AU - Barbosa,Raquel de Melo, AU - Vargas,Fernanda Grace A, AU - de Azevedo,Eduardo Pereira, AU - Lins,Antônio Cláudio da Silva, AU - Camara,Celso A, AU - Aragão,Cícero F S, AU - Moura,Tulio Flavio de Lima E, AU - Raffin,Fernanda Nervo, Y1 - 2017/12/19/ PY - 2017/12/6/pubmed PY - 2018/10/3/medline PY - 2017/12/6/entrez KW - PEG 6000 KW - PVP K30 KW - dissolution rate KW - solid dispersion KW - β-Lapachone SP - 750 EP - 756 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 44 IS - 5 N2 - β-lapachone (βlap) has shown potential use in various medical applications. However, its poor solubility has limited its systemic administration and clinical applications. The aim of this work is to develop solid dispersions of βlap using poly (ethylene glycol) (PEG 6000) and polyvinylpyrrolidone (PVP K30) as hydrophilic polymers and evaluate the dissolution rate in aqueous medium. Solid dispersions were prepared by solvent evaporation method using different weight ratios of βlap and hydrophilic polymer (1:1, 1:2, and 1:3). Characterization performed by differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, and scanning electron microscopy showed that βlap was molecularly dispersed within the polymer matrix. The in vitro dissolution tests showed an enhancement in the dissolution profile of βlap as solid dispersions prepared in both PVP and PEG, although the former showed better results. The drug:polymer ratio influenced βlap dissolution rate, as higher amounts of hydrophilic polymer led to enhanced drug dissolution. Thus, this study demonstrated that solid dispersions of βlap in PVP offers an effective way to overcome the poor dissolution of βlap. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/29206496/Development_of_solid_dispersions_of_β_lapachone_in_PEG_and_PVP_by_solvent_evaporation_method_ L2 - http://www.tandfonline.com/doi/full/10.1080/03639045.2017.1411942 DB - PRIME DP - Unbound Medicine ER -