title: Development of ibuprofen nanoliposome for transdermal delivery: Physical characterization, in vitro/in vivo studies, and anti-inflammatory activity.
abstract: OBJECTIVE
  Ibuprofen is an established non-steroidal anti-inflammatory drug commonly used for general inflammation. However, it causes gastrointestinal troubles when administered orally, thereby decreasing patient compliance. Transdermal application of vesicular formulation of Ibuprofen will provide better patient compliance and efficacy.
  
  
  METHODS
  Six different compositions of lipid constituents have been formulated into nanovesicles using thin-film hydration method and dispersed into gel using Carbopol 934. The formulations were characterized based on physicochemical parameters using photon correlation spectroscopy, transmission electron microscopy, in vitro drug release, ex vivo skin permeation using human skin, and in vivo studies.
  
  
  RESULTS
  The formulation, ibuprofen liposomal gel-5 (ILG-5), had nanoliposome of smallest size (159 nm) and polydispersity index (0.331). This formulation showed moderate zeta potential and the highest encapsulation. All the formulations including IG showed a considerable amount of drug release through in vitro synthetic membrane. ILG-5 showed maximum permeation during skin permeation studies. IG showed no permeation in ex vivo settings. ILG-5 has shown the highest Cmax and AUC during in vivo permeation study.
  
  
  CONCLUSIONS
  The present work clearly shows the superiority of nanoliposome formulation over non-vesicular formulations and that lipid composition containing 7/3/1 molar ratio of phosphatidylcholine, cholesterol, and dicetyl phosphate is optimum for nanoliposome preparations, in the cases where controlled delivery of drug is needed for a sufficient period of time.
authors.affiliation: a Department of Pharmaceutics , I.T.S. Paramedical College (Pharmacy) , Muradnagar, Ghaziabad , U.P. , India.
authors.forename: Praveen Kumar
authors.initials: PK
authors.lastname: Gaur
authors.affiliation: a Department of Pharmaceutics , I.T.S. Paramedical College (Pharmacy) , Muradnagar, Ghaziabad , U.P. , India.
authors.forename: Meenakshi
authors.initials: M
authors.lastname: Bajpai
authors.affiliation: b Department of Pharmacognosy and Phytochemistry , Jamia Hamdard , New Delhi , India.
authors.forename: Shikha
authors.initials: S
authors.lastname: Mishra
authors.affiliation: c Department of Pharmaceutics , School of Pharmaceutical Sciences, IFTM University , Moradabad , India.
authors.forename: Anurag
authors.initials: A
authors.lastname: Verma
mesh_terms: D000179:Acrylates / Q000737:chemistry; D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics / Q000494:pharmacology*; D019540:Area Under Curve; D002351:Carrageenan; D002784:Cholesterol / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000493:pharmacokinetics / Q000494:pharmacology*; D015194:Diffusion Chambers, Culture; D004339:Drug Compounding; D065546:Drug Liberation; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D005782:Gels; D006614:Hindlimb / Q000187:drug effects / Q000473:pathology; D006801:Humans; D007052:Ibuprofen / Q000493:pharmacokinetics / Q000494:pharmacology*; D008081:Liposomes / Q000737:chemistry*; D010755:Organophosphates / Q000737:chemistry; D010539:Permeability; D010713:Phosphatidylcholines / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000187:drug effects / Q000378:metabolism
chemical_list: D000179:Acrylates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D005782:Gels; D008081:Liposomes; D010755:Organophosphates; D010713:Phosphatidylcholines; C002290:dicetylphosphate; D002351:Carrageenan; D002784:Cholesterol; C453622:carbopol 934P; D007052:Ibuprofen
keywords: delivery; entrapment efficiency; ibuprofen; nanoliposome; permeation