title: A novel vesicular transdermal delivery of nifedipine - preparation, characterization and in vitro/in-vivo evaluation.
abstract: Nifedipine is a calcium channel blocker extensively used in the treatment of anginal and hypertension. On oral administration it undergoes extensive first pass metabolism, which outweighs its absorbance through gastrointestinal tract (GIT) and bioavailability of the drug in systemic circulation. As an alternative to oral route transdermal route of drug delivery was developed. In the present investigation, proniosomes are prepared by varying the ratio of span-40, lecithin, aqueous phase and polymer. Formulation containing span-40, lecithin, isopropyl alcohol, 0.1% glycerol (5:5:4) and HPMC (2%) showed smaller vesicle size, high entrapment efficiency. The niosomal formation after hydration and their surface morphology of optimized formulation was studied by Motic and transmission electron microscopy. FTIR and differential scanning calorimetry studies were performed to unravel and understand the solid state properties of the drug and chemical interaction with formulation excipients. The ex-vivo Franz-diffusion studies were carried out in pH 6.8 using rat skin and the results showed better permeability of niosomes with good steady state flux and enhancement ratio suggesting the potential of proniosomal carriers for improved transdermal delivery of nifedipine. Skin irritation studies for 7 days, showed that the drug when formulated as proniosomes to be non-irritant with no erythemia development compared to pure drug. From the bio-distribution studies, the vesicles prepared with hydroxy propyl methyl cellulose with span-40 was found to be ideal batch as the concentration of drug at target site was higher.
authors.affiliation: a Department of Pharmaceutics, JSS College of Pharmacy , JSS University , Udhagamandalam , Tamilnadu , India.
authors.forename: Venkata Ramesh
authors.initials: VR
authors.lastname: Yasam
authors.affiliation: a Department of Pharmaceutics, JSS College of Pharmacy , JSS University , Udhagamandalam , Tamilnadu , India.
authors.forename: Satya Lavanya
authors.initials: SL
authors.lastname: Jakki
authors.affiliation: a Department of Pharmaceutics, JSS College of Pharmacy , JSS University , Udhagamandalam , Tamilnadu , India.
authors.forename: Jawahar
authors.initials: J
authors.lastname: Natarajan
authors.affiliation: a Department of Pharmaceutics, JSS College of Pharmacy , JSS University , Udhagamandalam , Tamilnadu , India.
authors.forename: Senthil
authors.initials: S
authors.lastname: Venkatachalam
authors.affiliation: a Department of Pharmaceutics, JSS College of Pharmacy , JSS University , Udhagamandalam , Tamilnadu , India.
authors.forename: Gowthamarajan
authors.initials: G
authors.lastname: Kuppusamy
authors.affiliation: a Department of Pharmaceutics, JSS College of Pharmacy , JSS University , Udhagamandalam , Tamilnadu , India.
authors.forename: Sumeet
authors.initials: S
authors.lastname: Sood
authors.affiliation: a Department of Pharmaceutics, JSS College of Pharmacy , JSS University , Udhagamandalam , Tamilnadu , India.
authors.forename: Kunal
authors.initials: K
authors.lastname: Jain
mesh_terms: D019840:2-Propanol / Q000737:chemistry; D000279:Administration, Cutaneous; D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D002121:Calcium Channel Blockers / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D002152:Calorimetry, Differential Scanning; D004339:Drug Compounding; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry; D005990:Glycerol / Q000737:chemistry; D006601:Hexoses / Q000737:chemistry; D065347:Hypromellose Derivatives / Q000737:chemistry / Q000493:pharmacokinetics; D054709:Lecithins / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D008081:Liposomes; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D009543:Nifedipine / Q000008:administration & dosage* / Q000737:chemistry / Q000633:toxicity; D010316:Particle Size; D051381:Rats; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; D005079:Excipients; D006601:Hexoses; D054709:Lecithins; D008055:Lipids; D008081:Liposomes; D065347:Hypromellose Derivatives; C061705:sorbitan monopalmitate; D009543:Nifedipine; D019840:2-Propanol; D005990:Glycerol
keywords: Biodistribution; nifedipine; proniosomes; stability; transdermal delivery