title: Nanovesicles of nitrendipine with lipid complex for transdermal delivery: pharmacokinetic and pharmacodynamic studies.
abstract: BACKGROUND
  Vesicular transdermal delivery can enhance the bioavailability of a drug especially affected by first-pass metabolism, e.g. nitrendipine. However effective transdermal delivery employs permeation enhancer, e.g oleic acid (OA) with ceramide 2, stearic acid, behenic acid, and cholesteryl sulfate lipid complex.
  
  
  OBJECTIVE
  This study investigated the preparation, characterization of physicochemical properties, ex vivo permeation using human skin, pharmacokinetic parameters and antihypertensive potential in rats, of nitrendipine-loaded nanovesicles of ceramide 2, stearic acid, behenic acid and cholesteryl sulfate containing oleic acid gel (NOVG).
  
  
  METHODS
  The nanovesicles were made using film hydration method and characterized for physicochemical properties, ex vivo permeation using human skin, pharmacokinetic parameters and antihypertensive potential.
  
  
  RESULTS
  Nitrendipine-loaded nanovesicles of ceramide-2 containing oleic acid (NOV-5) have shown fluxes in the range of 4.88-24.72 μg/cm(2)/h nitrendipine oral suspension (NOS) at equal dose. NOVG-5 has shown almost 33% reduction in blood pressure in the first hour and a further decrease of 25% in the second hour to restore the normal pressure.
  
  
  CONCLUSIONS
  The permeation increases with increase in OA content. OA gets integrated in vesicle wall and enhances its permeability, whereas ceramide content makes sure that skin does not become damaged even after permeation.
  
  
  CONCLUSIONS
  NOVG-5 has shown the most favorable physicochemical properties and good permeation through skin providing good management of hypertension during crucial initial hours.
authors.affiliation: a Department of Pharmaceutics , I.T.S. College of Pharmacy , Muradnagar, Ghaziabad , Uttar Pradesh , India .
authors.forename: Praveen
authors.initials: P
authors.lastname: Kumar Gaur
authors.affiliation: b Department of Pharmacognosy and Phytochemistry , Jamia Hamdard , New Delhi , India , and.
authors.forename: Shikha
authors.initials: S
authors.lastname: Mishra
authors.affiliation: c Department of Pharmacology , Faculty of Medicine, Institute of Medical Sciences, Banaras Hindu University , Varanasi , Uttar Pradesh , India.
authors.forename: Suresh
authors.initials: S
authors.lastname: Purohit
mesh_terms: D000818:Animals; D002518:Ceramides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D002788:Cholesterol Esters / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D005227:Fatty Acids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D005260:Female; D006801:Humans; D008297:Male; D053769:Nanocapsules / Q000737:chemistry*; D009568:Nitrendipine / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D019301:Oleic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption / Q000187:drug effects*; D013229:Stearic Acids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D002518:Ceramides; D002788:Cholesterol Esters; D005227:Fatty Acids; D053769:Nanocapsules; D013229:Stearic Acids; D019301:Oleic Acid; C031183:stearic acid; D009568:Nitrendipine; C007547:behenic acid; C007045:cholesteryl sulfate
keywords: Antihypertensive activity; behenic acid; oleic acid; permeability; pharmacokinetic; stearic acid