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Attenuation of lipid levels in triton induced hyperlipidemia rats through rosuvastatin calcium nanoparticles: Pharmacokinetic and pharmacodynamic studies.
Dudhipala, N R; Ettireddy, S R; Puchakayala, G R.
Afiliación
  • Dudhipala NR; Department of Pharmaceutics, Vaagdevi Pharmacy College, Warangal, Telangana, 506 001, India. Electronic address: dnrku14@gmail.com.
  • Ettireddy SR; University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Telangana, 506 009, India. Electronic address: swethareddy532@gmail.com.
  • Puchakayala GR; Department of Pharmacology, Vaagdevi Pharmacy College, Warangal, Telangana, 506 001, India; Synapse Life Sciences, Warangal, Telangana, 506 005, India. Electronic address: goverdhanucpsc@gmail.com.
Chem Phys Lipids ; 237: 105081, 2021 07.
Article en En | MEDLINE | ID: mdl-33811848
ABSTRACT
The aim of this research was to study the effect of marketed tablet (Crestor®) powder suspension (MTPS) and nanoparticle formulation of rosuvastatin calcium (RC) on the pharmacokinetic (PK) and pharmacodynamic (PD) parameters in hyperlipidemia rats. The hyperlipidemia is induced by intraperitoneal injection of Triton-X-100 in 0.9 %w/v saline solution. The marketed tablet was dispersed into suspension. The RC loaded nanoparticles (RC-NPs) are prepared by homogenization method. The prepared RC-NP formulation was characterized for size, drug excipient compatibility and crystallization by differential scanning calorimeter (DSC), morphology by SEM, stability at room temperature, in-vitro dissolution and in-situ absorption in rats. Further, the pharmacokinetic and pharmacodynamic studies were conducted in hyperlipidemia rats. The size of the RC-NP formulation was found to be 183.4 ± 4.5 nm and to be nearly spherical by SEM. DSC studies revealed that no interaction and RC converted to amorphous form in RC-NP formulation. RC-NP formulation was physically and chemically stable over two months at room temperature. The drug release was found to be 25.8 ± 2.5 and 89.96 ± 2.8 % in five mins, respectively from MTPS and RC-NP formulations. The Peff of MTPS and NP of RC was 1.8 ± 0.2 × 10-5 and 2.7 ± 0.3 × 10-5 cm/s, respectively. From the PK studies, the enhancement in the oral bioavailability was found to be 2.4-folds when compared to MTPS formulation and statistically significant (p < 0.05). PD study of RC-NP formulation in hyperlipidemic rats exhibited decrease in lipid profile for 24 h, while MTPS exhibited a decrease in lipid profile for 12 h. Therefore, the results conclusively demonstrate the nanoparticles of RC showed significant enhancement in the PK and PD parameters.
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Nanopartículas / Rosuvastatina Cálcica / Lípidos Límite: Animals Idioma: En Revista: Chem Phys Lipids Año: 2021 Tipo del documento: Article

Texto completo: 1 Base de datos: MEDLINE Asunto principal: Nanopartículas / Rosuvastatina Cálcica / Lípidos Límite: Animals Idioma: En Revista: Chem Phys Lipids Año: 2021 Tipo del documento: Article