title: Formulation and Optimization of Candesartan Cilexetil Nano Lipid Carrier: In Vitro and In Vivo Evaluation.
abstract: The objective of this study was to formulate and optimize Candesartan Cilexetil (CC) loaded nanostructured lipid carriers (NLCs) for enhanced oral bioavailability.
  
  
  
  Glycerol monostearate (GMS), Oleic acid, Tween 80 and Span 40 were selected as a solid lipid, liquid lipid, surfactant and co- surfactant, respectively. The CC-NLCs were prepared by hot emulsion probe sonication technique and optimized using experimental design approach. The formulated CC-NLCs were evaluated for various physicochemical parameters and further optimized formulation (CC-NLC-Opt) was assessed for in vivo pharmacokinetic and pharmacodynamic activity.
  
  
  
  The optimized formulation (CC-NLC-Opt) showed particle size (183.5±5.89nm), PDI (0.228±0.13), zeta potential (-28.2±0.99mV), and entrapment efficiency (88.9±3.69%). The comparative in vitro release study revealed that CC-NLC-Opt showed significantly better (p<0.05) release and enhanced permeation as compared to CC-suspension. The in vivo pharmacokinetic study gave many folds increase in oral bioavailability than CC suspension, which was further confirmed by antihypertensive activity in a murine model.
  
  
  
  Thus, the results of ex vivo permeation, pharmacokinetic study and pharmacodynamics study suggest the potential of CC-NLCs for improved oral delivery.
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India
authors.forename: Anjan
authors.initials: A
authors.lastname: Paudel
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Aljouf University, Sakaka, Aljouf, KSA
authors.lastname: Ameeduzzafar
authors.affiliation: Department of Pharmaceutics, Glocal School of Pharmacy, The Glocal University, Sahararnpur, Uttar Pradesh, India
authors.forename: Syed Sarim
authors.initials: SS
authors.lastname: Imam
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India
authors.forename: Mohd
authors.initials: M
authors.lastname: Fazil
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India
authors.forename: Shahroz
authors.initials: S
authors.lastname: Khan
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India
authors.forename: Abdul
authors.initials: A
authors.lastname: Hafeez
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India
authors.forename: Farhan Jalees
authors.initials: FJ
authors.lastname: Ahmad
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India
authors.forename: Asgar
authors.initials: A
authors.lastname: Ali
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001562:Benzimidazoles / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001682:Biological Availability; D001713:Biphenyl Compounds / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D065546:Drug Liberation; D004355:Drug Stability; D005260:Female; D005989:Glycerides / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D007408:Intestinal Absorption; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D019301:Oleic Acid / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D010316:Particle Size; D017208:Rats, Wistar; D013777:Tetrazoles / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000959:Antihypertensive Agents; D001562:Benzimidazoles; D001713:Biphenyl Compounds; D004337:Drug Carriers; D005989:Glycerides; D013777:Tetrazoles; C048159:glyceryl monostearate; D019301:Oleic Acid; C077793:candesartan cilexetil
keywords: Antihypertensive activity; bioavailability study; candesartan cilexetil; formulation design; lipid formulation; nanoparticle