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Improved anti-hyperlipidemic activity of Rosuvastatin Calcium via lipid nanoparticles: Pharmacokinetic and pharmacodynamic evaluation.
Eur J Pharm Biopharm. 2017 Jan; 110:47-57.EJ

Abstract

The intent of this investigation was to improve pharmacokinetic (PK) and pharmacodynamic (PD) effects of Rosuvastatin calcium (RC) by solid lipid nanoparticles (SLNs). RC is anti-hyperlipidemic drug with low oral bioavailability (20%) due to first-pass metabolism. Hot homogenization followed by ultrasonication method was used to prepare RC-SLNs with stearic acid, glyceryl behenate and glyceryl trilaurate as lipid matrices, egg lecithin and poloxamer 188 as surfactants. The prepared SLNs were tested for particle size, PDI, zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro release. Further, PK and PD studies were conducted on selected SLNs. No changes in physical stability of the optimized SLN were observed at refrigerated and room temperature for 90days. SLNs prepared with glyceryl trilaurate having average size of 67.21±1.71nm, PDI of 0.25±0.01, ZP of -28.93±0.84mV with 93.51±0.34% EE was considered as optimized. DSC and XRD studies revealed that no interaction occurred between the drug and lipid. SEM and TEM studies revealed that SLNs were nearly spherical in shape. PK studies showed improvement in the oral bioavailability (extent of absorption) of SLNs by 4.6-fold when compared to that of suspension. PD study of SLNs in hyperlipidemic rats exhibited a decrease in lipid profile for 36h, while a suspension exhibited for 24h.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, Laboratory of Nanotechnology, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Telangana State 506009, India.Department of Pharmaceutical Sciences, Laboratory of Nanotechnology, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Telangana State 506009, India. Electronic address: vbkishan@yahoo.com.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27810472

Citation

Dudhipala, Narendar, and Kishan Veerabrahma. "Improved Anti-hyperlipidemic Activity of Rosuvastatin Calcium Via Lipid Nanoparticles: Pharmacokinetic and Pharmacodynamic Evaluation." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 110, 2017, pp. 47-57.
Dudhipala N, Veerabrahma K. Improved anti-hyperlipidemic activity of Rosuvastatin Calcium via lipid nanoparticles: Pharmacokinetic and pharmacodynamic evaluation. Eur J Pharm Biopharm. 2017;110:47-57.
Dudhipala, N., & Veerabrahma, K. (2017). Improved anti-hyperlipidemic activity of Rosuvastatin Calcium via lipid nanoparticles: Pharmacokinetic and pharmacodynamic evaluation. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 110, 47-57. https://doi.org/10.1016/j.ejpb.2016.10.022
Dudhipala N, Veerabrahma K. Improved Anti-hyperlipidemic Activity of Rosuvastatin Calcium Via Lipid Nanoparticles: Pharmacokinetic and Pharmacodynamic Evaluation. Eur J Pharm Biopharm. 2017;110:47-57. PubMed PMID: 27810472.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Improved anti-hyperlipidemic activity of Rosuvastatin Calcium via lipid nanoparticles: Pharmacokinetic and pharmacodynamic evaluation. AU - Dudhipala,Narendar, AU - Veerabrahma,Kishan, Y1 - 2016/10/31/ PY - 2016/01/19/received PY - 2016/09/03/revised PY - 2016/10/29/accepted PY - 2016/11/5/pubmed PY - 2017/3/21/medline PY - 2016/11/5/entrez KW - Extent of absorption KW - Pharmacodynamics KW - Pharmacokinetics KW - Rosuvastatin calcium KW - SEM KW - Solid lipid nanoparticles SP - 47 EP - 57 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 110 N2 - The intent of this investigation was to improve pharmacokinetic (PK) and pharmacodynamic (PD) effects of Rosuvastatin calcium (RC) by solid lipid nanoparticles (SLNs). RC is anti-hyperlipidemic drug with low oral bioavailability (20%) due to first-pass metabolism. Hot homogenization followed by ultrasonication method was used to prepare RC-SLNs with stearic acid, glyceryl behenate and glyceryl trilaurate as lipid matrices, egg lecithin and poloxamer 188 as surfactants. The prepared SLNs were tested for particle size, PDI, zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro release. Further, PK and PD studies were conducted on selected SLNs. No changes in physical stability of the optimized SLN were observed at refrigerated and room temperature for 90days. SLNs prepared with glyceryl trilaurate having average size of 67.21±1.71nm, PDI of 0.25±0.01, ZP of -28.93±0.84mV with 93.51±0.34% EE was considered as optimized. DSC and XRD studies revealed that no interaction occurred between the drug and lipid. SEM and TEM studies revealed that SLNs were nearly spherical in shape. PK studies showed improvement in the oral bioavailability (extent of absorption) of SLNs by 4.6-fold when compared to that of suspension. PD study of SLNs in hyperlipidemic rats exhibited a decrease in lipid profile for 36h, while a suspension exhibited for 24h. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/27810472/Improved_anti_hyperlipidemic_activity_of_Rosuvastatin_Calcium_via_lipid_nanoparticles:_Pharmacokinetic_and_pharmacodynamic_evaluation_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(16)30759-7 DB - PRIME DP - Unbound Medicine ER -