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Solid Dispersion of Kaempferol: Formulation Development, Characterization, and Oral Bioavailability Assessment.
AAPS PharmSciTech. 2019 Feb 11; 20(3):106.AP

Abstract

Kaempferol (KPF), an important flavonoid, has been reported to exert antioxidant, anti-inflammatory, and anticancer activity. However, this compound has low water solubility and hence poor oral bioavailability. This work aims to prepare a solid dispersion (SD) of KPF using Poloxamer 407 in order to improve the water solubility, dissolution rate, and pharmacokinetic properties KPF. After optimization, SDs were prepared at a 1:5 weight ratio of KPF:carrier using the solvent method (SDSM) and melting method (SDMM). Formulations were characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffractometry (XRD) analysis, differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). The solubility in water of carried-KPF was about 4000-fold greater than that of free KPF. Compared with free KPF or the physical mixture, solid dispersions significantly increased the extent of drug release (approximately 100% within 120 min) and the dissolution rate. Furthermore, after oral administration of SDMM in rats, the area under the curve (AUC) and the peak plasma concentration (Cmax) of KPF from SDMM were twofold greater than those of free KPF (p < 0.05). In conclusion, SD with Poloxamer 407 is a feasible pharmacotechnical strategy to ameliorate the dissolution and bioavailability of KPF.

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Authors+Show Affiliations

Colombo M
Laboratório de Desenvolvimento Galênico, Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752-607, Porto Alegre, RS, 90610-000, Brazil.
de Lima Melchiades G
Laboratório de Desenvolvimento Galênico, Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752-607, Porto Alegre, RS, 90610-000, Brazil.
Michels LR
Laboratório de Desenvolvimento Galênico, Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752-607, Porto Alegre, RS, 90610-000, Brazil.
Figueiró F
Programa de Pós-Graduação em Ciências Biológicas: Bioquímica, Instituto de Ciências Básicas da Saúde, Universidade Federal do Rio Grande do Sul, Avenida Ramiro Barcelos, 2600 Anexo, Porto Alegre, RS, 90035-003, Brazil. Departamento de Bioquímica, Instituto de Ciências Básicas da Saúde, Universidade Federal do Rio Grande do Sul, Avenida Ramiro Barcelos, 2600 Anexo, Porto Alegre, RS, 90035-003, Brazil.
Bassani VL
Laboratório de Desenvolvimento Galênico, Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752-607, Porto Alegre, RS, 90610-000, Brazil.
Teixeira HF
Laboratório de Desenvolvimento Galênico, Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752-607, Porto Alegre, RS, 90610-000, Brazil.
Koester LS
Laboratório de Desenvolvimento Galênico, Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752-607, Porto Alegre, RS, 90610-000, Brazil. leticia.koester@ufrgs.br.

MeSH

Administration, OralAnimalsArea Under CurveBiological AvailabilityCalorimetry, Differential ScanningKaempferolsMaleMicroscopy, Electron, ScanningPoloxamerRatsSolubilitySpectroscopy, Fourier Transform Infrared

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30746582

Citation

Colombo, Mariana, et al. "Solid Dispersion of Kaempferol: Formulation Development, Characterization, and Oral Bioavailability Assessment." AAPS PharmSciTech, vol. 20, no. 3, 2019, p. 106.
Colombo M, de Lima Melchiades G, Michels LR, et al. Solid Dispersion of Kaempferol: Formulation Development, Characterization, and Oral Bioavailability Assessment. AAPS PharmSciTech. 2019;20(3):106.
Colombo, M., de Lima Melchiades, G., Michels, L. R., Figueiró, F., Bassani, V. L., Teixeira, H. F., & Koester, L. S. (2019). Solid Dispersion of Kaempferol: Formulation Development, Characterization, and Oral Bioavailability Assessment. AAPS PharmSciTech, 20(3), 106. https://doi.org/10.1208/s12249-019-1318-y
Colombo M, et al. Solid Dispersion of Kaempferol: Formulation Development, Characterization, and Oral Bioavailability Assessment. AAPS PharmSciTech. 2019 Feb 11;20(3):106. PubMed PMID: 30746582.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Solid Dispersion of Kaempferol: Formulation Development, Characterization, and Oral Bioavailability Assessment. AU - Colombo,Mariana, AU - de Lima Melchiades,Gabriela, AU - Michels,Luana Roberta, AU - Figueiró,Fabrício, AU - Bassani,Valquiria Linck, AU - Teixeira,Helder Ferreira, AU - Koester,Letícia Scherer, Y1 - 2019/02/11/ PY - 2018/11/29/received PY - 2019/01/22/accepted PY - 2019/2/13/entrez PY - 2019/2/13/pubmed PY - 2019/4/6/medline KW - Poloxamer 407 KW - bioavailability KW - dissolution KW - kaempferol KW - solid dispersion SP - 106 EP - 106 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 20 IS - 3 N2 - Kaempferol (KPF), an important flavonoid, has been reported to exert antioxidant, anti-inflammatory, and anticancer activity. However, this compound has low water solubility and hence poor oral bioavailability. This work aims to prepare a solid dispersion (SD) of KPF using Poloxamer 407 in order to improve the water solubility, dissolution rate, and pharmacokinetic properties KPF. After optimization, SDs were prepared at a 1:5 weight ratio of KPF:carrier using the solvent method (SDSM) and melting method (SDMM). Formulations were characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffractometry (XRD) analysis, differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). The solubility in water of carried-KPF was about 4000-fold greater than that of free KPF. Compared with free KPF or the physical mixture, solid dispersions significantly increased the extent of drug release (approximately 100% within 120 min) and the dissolution rate. Furthermore, after oral administration of SDMM in rats, the area under the curve (AUC) and the peak plasma concentration (Cmax) of KPF from SDMM were twofold greater than those of free KPF (p < 0.05). In conclusion, SD with Poloxamer 407 is a feasible pharmacotechnical strategy to ameliorate the dissolution and bioavailability of KPF. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/30746582/Solid_Dispersion_of_Kaempferol:_Formulation_Development_Characterization_and_Oral_Bioavailability_Assessment_ L2 - https://dx.doi.org/10.1208/s12249-019-1318-y DB - PRIME DP - Unbound Medicine ER -