Enhanced oral bioavailability of levormeloxifene and raloxifene by nanoemulsion: simultaneous bioanalysis using liquid chromatography-tandem mass spectrometry.
Nanomedicine (Lond)
; 19(12): 1051-1068, 2024.
Article
en En
| MEDLINE
| ID: mdl-38639565
ABSTRACT
Aim & objective:
Levormeloxifene (L-ORM) and raloxifene (RAL) are selective estrogen receptor modulators used in the treatment of postmenopausal osteoporosis and breast cancer. Here, we developed and validated a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the simultaneous estimation of both drugs. Materials &methods:
A quality-by-design (QbD) approach was used for the optimization of the nanoemulsion, and US FDA guidelines were followed for method validation.Results:
Multiple reaction monitoring transitions were used for L-ORM (459.05â98.50), RAL (475.00â112.02) and internal standard (180.10â110.2). Analytes were resolved in a C18 column with 8020 v/v% acetonitrile (ACN), 0.1% formic acid in triple-distilled water as a mobile phase. The developed method was linear over a concentration range of 1-600 ng/ml. Pharmacokinetic results of free L-ORM-RAL and the L-ORM-RAL nanoemulsion showed Cmax of free L-ORM - 70.65 ± 16.64, free RAL 13.53 ± 2.72, L-ORM nanoemulsion 65.07 ± 14.0 and RAL-nanoemulsion 59.27 ± 17.44 ng/ml.Conclusion:
Future findings will contribute to the treatment of postmenopausal osteoporosis and breast cancer using L-ORM and RAL.
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Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Disponibilidad Biológica
/
Clorhidrato de Raloxifeno
/
Moduladores Selectivos de los Receptores de Estrógeno
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Emulsiones
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Espectrometría de Masas en Tándem
Límite:
Animals
/
Female
/
Humans
Idioma:
En
Revista:
Nanomedicine (Lond)
Año:
2024
Tipo del documento:
Article
País de afiliación:
India