2014Journal of Drug Delivery and TherapeuticsOpen access

ENHANCED ORAL BIOAVAILABILITY IN ALBINO RABBITS OF LOVASTATIN NANOPARTICLES

Anilkumar Jalindar Shinde

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Abstract

The aim of the study was to compare the single dose oral bioavailability of lovastatin (LV) nanoparticles in albino rabbits. Plasma was analyzed for lovastatin using a sensitive, reproducible, accurate and validated RP-HPLC method. Pharmacokinetic parameters including AUC, Cmax, Tmax, t1/2, MRT and Kel were determined from plasma concentration of the formulations. The randomly divided into three treatment groups with six animals in each group, as standard I, Standard II and Test. Lovastatin pure drug and lovastatin lovastatin marketed formulation were administered to standard group. Lovastatin loaded nanoparticles suspension was administered to test group. The Cmax of LV nanoparticles was found to be 72.28 ±0.158 ng/ml, whereas Cmax value for the drug suspension and marketed tablet formulation was found to be 33.10 ± 0.176ng/ml and 40.96 ± 0.244ng/ml respectively. (P < 0.001) indicating facilitated absorption of LV by nanoparticles. Tmax of lovastatin nanoparticles was 2 hrs, whereas for the drug suspension and marketed tablet formulation were 1 h respectively. (P < 0.001) The AUC (0–∞h) value for the lovastatin nanoparticles, drug suspension and marketed tablet formulation were found to be 301.43 ±0.165 (ng/ml × h), 73.88 ± 0.210 (ng/ml × h) and 120.51 ± 0.338 (ng/ml × h) respectively. (p < 0.001) The mean residence time (MRT) values for the lovastatin nanoparticles, drug suspension and marketed tablet formulation were found to be 1.41 h, 1.35 h and 1.63 h respectively. (P < 0.001) The relative bioavailability was found to be significant improvement in bioavailability (1.5 fold) as compared with the conventional tablets.

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What this paper is about

The aim of the study was to compare the single dose oral bioavailability of lovastatin (LV) nanoparticles in albino rabbits. Plasma was analyzed for lovastatin using a sensitive, reproducible, accurate and validated RP-HPLC method. Pharmacokinetic parameters including AUC, Cmax, Tmax, t1/2, MRT and Kel were determined from plasma concentration of the formulations. The randomly divided into three treatment groups with six animals in each group, as standard I, Standard II and Test. Lovastatin pure drug and lovastatin lovastatin marketed formulation were administered to standard group. Lovastatin loaded nanoparticles suspension was administered to test group. The Cmax of LV nanoparticles was found to be 72.28 ±0.158 ng/ml, whereas Cmax value for the drug suspension and marketed tablet formulation was found to be 33.10 ± 0.176ng/ml and 40.96 ± 0.244ng/ml respectively. (P < 0.001) indicating facilitated absorption of LV by nanoparticles. Tmax of lovastatin nanoparticles was 2 hrs, whereas for the drug suspension and marketed tablet formulation were 1 h respectively. (P < 0.001) The AUC (0–∞h) value for the lovastatin nanoparticles, drug suspension and marketed tablet formulation were found to be 301.43 ±0.165 (ng/ml × h), 73.88 ± 0.210 (ng/ml × h) and 120.51 ± 0.338 (ng/ml × h) respectively. (p < 0.001) The mean residence time (MRT) values for the lovastatin nanoparticles, drug suspension and marketed tablet formulation were found to be 1.41 h, 1.35 h and 1.63 h respectively. (P < 0.001) The relative bioavailability was found to be significant improvement in bioavailability (1.5 fold) as compared with the conventional tablets.

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Available abstract

The aim of the study was to compare the single dose oral bioavailability of lovastatin (LV) nanoparticles in albino rabbits. Plasma was analyzed for lovastatin using a sensitive, reproducible, accurate and validated RP-HPLC method. Pharmacokinetic parameters including AUC, Cmax, Tmax, t1/2, MRT and Kel were determined from plasma concentration of the formulations. The randomly divided into three treatment groups with six animals in each group, as standard I, Standard II and Test. Lovastatin pure drug and lovastatin lovastatin marketed formulation were administered to standard group. Lovastatin loaded nanoparticles suspension was administered to test group. The Cmax of LV nanoparticles was found to be 72.28 ±0.158 ng/ml, whereas Cmax value for the drug suspension and marketed tablet formulation was found to be 33.10 ± 0.176ng/ml and 40.96 ± 0.244ng/ml respectively. (P < 0.001) indicating facilitated absorption of LV by nanoparticles. Tmax of lovastatin nanoparticles was 2 hrs, whereas for the drug suspension and marketed tablet formulation were 1 h respectively. (P < 0.001) The AUC (0–∞h) value for the lovastatin nanoparticles, drug suspension and marketed tablet formulation were found to be 301.43 ±0.165 (ng/ml × h), 73.88 ± 0.210 (ng/ml × h) and 120.51 ± 0.338 (ng/ml × h) respectively. (p < 0.001) The mean residence time (MRT) values for the lovastatin nanoparticles, drug suspension and marketed tablet formulation were found to be 1.41 h, 1.35 h and 1.63 h respectively. (P < 0.001) The relative bioavailability was found to be significant improvement in bioavailability (1.5 fold) as compared with the conventional tablets.

Key concepts: Lovastatin, Cmax, Bioavailability, Pharmacokinetics, Chemistry, Pharmacology, Chromatography, Medicine

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