title: Nanostructured lipid carriers of olmesartan medoxomil with enhanced oral bioavailability.
abstract: The current study explores the potential of nanostructured lipid carriers (NLCs) for oral bioavailability enhancement of olmesartan medoxomil (OLM) by systemic design approach. OLM-NLC was successfully prepared with optimized process parameters (i.e. amount of liquid lipid, total amount of lipid, drug content and surfactant concentration) using the Box-Behnken design of experiments for different response parameters (i.e. particle size, Polydispersity index and entrapment efficiency). Further, optimized formulation was validated which depicted nano size, homogenous distribution with optimum entrapment efficiency. OLM-NLC was characterized by different techniques viz. differential scanning calorimetry (DSC), powder X-Ray diffraction (PXRD), scanning electron microscopy (SEM) and transmission electron microscopy (TEM), which showed reduced crystallinity of the drug with smooth spherical appearance of nanoparticles. Formulation was found to be stable in simulated gastric fluids as no significant changes were found in size, PDI and entrapment efficiency. In vitro release showed extended release of OLM from OLM-NLC. In vitro cellular uptake study revealed 5.2 folds higher uptake of nanoparticles as compare to the free drug, when incubated with Caco-2 cells. In vivo performance showed that AUCtotaland Cmaxof OLM-NLC were found significantly (P<0.01) higher as compare to the free drug. Overall, the present study successfully reports the improvement of oral bioavailability of olmesartan medoxomil.
authors.affiliation: Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sec-67, S.A.S. Nagar, Punjab, 160062, India; Department of Pharmaceutical Technology (Formulations), National Institute of Pharmaceutical Education and Research (NIPER), Sec-67, S.A.S. Nagar, Punjab, 160062, India.
authors.forename: Vikram
authors.initials: V
authors.lastname: Kaithwas
authors.affiliation: Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sec-67, S.A.S. Nagar, Punjab, 160062, India; Department of Pharmaceutical Technology (Formulations), National Institute of Pharmaceutical Education and Research (NIPER), Sec-67, S.A.S. Nagar, Punjab, 160062, India.
authors.forename: Chander Parkash
authors.initials: CP
authors.lastname: Dora
authors.affiliation: Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sec-67, S.A.S. Nagar, Punjab, 160062, India.
authors.forename: Varun
authors.initials: V
authors.lastname: Kushwah
authors.affiliation: Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sec-67, S.A.S. Nagar, Punjab, 160062, India. Electronic address: sanyogjain@niper.ac.in.
authors.forename: Sanyog
authors.initials: S
authors.lastname: Jain
mesh_terms: D000284:Administration, Oral; D047228:Angiotensin II Type 1 Receptor Blockers / Q000008:administration & dosage / Q000493:pharmacokinetics; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D001682:Biological Availability; D018938:Caco-2 Cells; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D004355:Drug Stability; D005750:Gastric Juice / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D008055:Lipids / Q000737:chemistry; D008422:Materials Testing; D053758:Nanoparticles / Q000737:chemistry / Q000648:ultrastructure; D000068557:Olmesartan Medoxomil / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D010316:Particle Size; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D047228:Angiotensin II Type 1 Receptor Blockers; D000959:Antihypertensive Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008055:Lipids; D013501:Surface-Active Agents; D000068557:Olmesartan Medoxomil
keywords: Bioavailability; Box-Behnken design; Caco-2 cells; Nanostructured lipid carrier (NLC); Olmesartan medoxomil