title: Atorvastatin calcium encapsulated eudragit nanoparticles with enhanced oral bioavailability, safety and efficacy profile.
abstract: Atorvastatin calcium (ATR), a second generation statin drug, was encapsulated in eudragit RSPO-based polymeric nanoparticles. The effect of independent variables (polymer content, stabilizer concentration, volume of chloroform and homogenization speed) on response variables (mean diameter particle size and entrapment efficiency) were investigated by employing central composite experimental design. All the independent variables were found to be significant for determining the response variables. Solid-state characterization study indicated the absence of physicochemical interaction between drug and polymer in formulation. Morphological study exhibited homogenous spherical shape of formulated nanoparticles. In vitro release study in phosphate buffer (pH 7.4) demonstrated sustained release profile over 24 h. Pharmacokinetic study in Charles Foster rats showed significant enhancement in oral bioavailability as compared to pure drug suspension. Efficacy study (lipid profile and blood glucose level) significantly justified the effectiveness of formulation having 50% less dose of ATR as compared to pure drug suspension. The effectiveness of formulation was further justified with an improved plasma safety profile of treated rats. Hence, ATR encapsulated eudragit RSPO nanoparticles can serve as potential drug delivery approach to enhance drug bioavailability, efficacy and safety profiles to alter existing marketed drug products.
authors.affiliation: a Department of Pharmaceutics , Indian Institute of Technology (Banaras Hindu University) , Varanasi, Uttar Pradesh , India.
authors.forename: Nagendra
authors.initials: N
authors.lastname: Kumar
authors.affiliation: a Department of Pharmaceutics , Indian Institute of Technology (Banaras Hindu University) , Varanasi, Uttar Pradesh , India.
authors.forename: Sundeep
authors.initials: S
authors.lastname: Chaurasia
authors.affiliation: a Department of Pharmaceutics , Indian Institute of Technology (Banaras Hindu University) , Varanasi, Uttar Pradesh , India.
authors.forename: Ravi R
authors.initials: RR
authors.lastname: Patel
authors.affiliation: a Department of Pharmaceutics , Indian Institute of Technology (Banaras Hindu University) , Varanasi, Uttar Pradesh , India.
authors.forename: Gayasuddin
authors.initials: G
authors.lastname: Khan
authors.affiliation: a Department of Pharmaceutics , Indian Institute of Technology (Banaras Hindu University) , Varanasi, Uttar Pradesh , India.
authors.forename: Vikas
authors.initials: V
authors.lastname: Kumar
authors.affiliation: a Department of Pharmaceutics , Indian Institute of Technology (Banaras Hindu University) , Varanasi, Uttar Pradesh , India.
authors.forename: Brahmeshwar
authors.initials: B
authors.lastname: Mishra
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000924:Anticholesteremic Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood* / Q000494:pharmacology; D000069059:Atorvastatin / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood* / Q000494:pharmacology; D001786:Blood Glucose / Q000032:analysis; D003692:Delayed-Action Preparations / Q000737:chemistry*; D008055:Lipids / Q000097:blood; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D011109:Polymethacrylic Acids / Q000737:chemistry*; D051381:Rats
chemical_list: D000924:Anticholesteremic Agents; D001786:Blood Glucose; D003692:Delayed-Action Preparations; D008055:Lipids; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D000069059:Atorvastatin
keywords: Atorvastatin calcium; bioavailability; efficacy; hyperlipidemia; nanoparticles