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Pharmacological and histological examination of atorvastatin-PVP K30 solid dispersions

Jahangiri, Azin, Barzegar-Jalali, Mohammad, Garjani, Alireza, Javadzadeh, Yousef, Hamishehkar, Hamed, Afroozian, Arash, Adibkia, Khosro
Powder technology 2015 v.286 pp. 538-545
X-ray diffraction, blood lipids, blood serum, cholesterol, crystal structure, differential scanning calorimetry, dispersions, drugs, evaporation, fatty liver, high fat diet, histology, hypercholesterolemia, in vivo studies, liver, oral administration, polyvinylpyrrolidone, powders, rats, scanning electron microscopy, solubility, solvents, therapeutics
The objective of the present study was to investigate the pharmacological efficiency of orally administered atorvastatin calcium (ATV) solid dispersions (SDs). SDs of ATV were prepared using polyvinylpyrrolidone K30 (PVP) through the solvent evaporation method. Physicochemical characteristics of the prepared formulations were assessed benefitting scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD). The drug dissolution rates (under sink and non-sink conditions) as well as solubility studies were also examined. Serum lipid levels, liver index and histological analysis of the liver tissue in hyperlipidemic rats were considered to evaluate the pharmacological efficiency of prepared SDs. According to our findings, the drug crystallinity was reduced and the drug dissolution characteristics were improved in the prepared SDs. In vivo studies revealed that oral administration of ATV (3mg/kg/day) in the SD form (ASDT) for 14days along with high fat diet (HFD) to the hypercholesterolemic rats led to a significant decline (P<0.05) in serum level of total cholesterol (TC) and low density lipoprotein-cholesterol (LDL-C). Moreover, ASDT exhibited more beneficial effects on the liver steatosis compared to ATV physical mixture (APMT) and hyperlipidemic control (HC) groups. In the present study, it was concluded that the SDs of ATV with improved physicochemical characteristics provided an increased therapeutic potential for management of hyperlipidemia compared to the corresponding physical mixtures (PMs).