title: Effect of non-phospholipid-based cationic and phospholipid-based anionic nanosized emulsions on skin retention and anti-inflammatory activity of celecoxib.
abstract: BACKGROUND
  Celecoxib (CXB, 0.2 g)-loaded anionic and cationic nanosized emulsions were prepared by a well-established combined emulsification method.
  
  
  OBJECTIVE
  To investigate the effect of non-phospholipid-based cationic and phospholipid-based anionic emulsions on skin retention and anti-inflammatory activity of CXB.
  
  
  METHODS
  Using Keshary-Chien diffusion cells with cellulose acetate membrane or excised rat skin, in vitro release and skin retention of CXB from solution and emulsions were studied. The anti-inflammatory activity was evaluated by the carrageenan-induced hind paw edema method in Wistar rats.
  
  
  RESULTS
  The amount of drug released through artificial membrane has decreased from 122.00 ± 0.70 μg/cm(2) for the CXB solution to 55.80 ± 0.70 μg/cm(2) for anionic emulsion, and then further decreased to 24.79 ± 0.90 μg/cm(2) for cationic emulsion. The JSS value obtained with solution, anionic, and cationic emulsions were 6825.79 ± 920.86, 2513.15 ± 382.71, and 1925.67 ± 147.42, respectively. Cationic emulsion showed a significantly higher level (P ≤ 0.05) of drug accumulation in full-thickness rat skin than anionic emulsion, and a substantially lesser percentage inhibition of edema values compared with both solution and anionic emulsion.
  
  
  CONCLUSIONS
  Sustained drug release together with increased skin accumulation and simultaneously decreased skin permeation as observed with cationic emulsion should substantiate its suitability as a topical delivery vehicle for CXB.
authors.affiliation: International Medical University SDN BHD, Bukit Jalil, 57000 Kuala Lumpur, Malaysia. tamilvanan2k@yahoo.com
authors.forename: S
authors.initials: S
authors.lastname: Tamilvanan
authors.forename: Raj
authors.initials: R
authors.lastname: Baskar
mesh_terms: D000818:Animals; D000838:Anions; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D002351:Carrageenan / Q000633:toxicity; D002412:Cations; D000068579:Celecoxib; D002482:Cellulose / Q000031:analogs & derivatives / Q000378:metabolism; D003692:Delayed-Action Preparations; D004058:Diffusion; D004195:Disease Models, Animal; D004487:Edema / Q000188:drug therapy / Q000473:pathology; D004655:Emulsions; D007249:Inflammation / Q000188:drug therapy / Q000473:pathology; D008297:Male; D053758:Nanoparticles; D010743:Phospholipids / Q000737:chemistry; D011720:Pyrazoles / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013449:Sulfonamides / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D000838:Anions; D000893:Anti-Inflammatory Agents; D002412:Cations; D003692:Delayed-Action Preparations; D004655:Emulsions; D010743:Phospholipids; D011720:Pyrazoles; D013449:Sulfonamides; C005062:acetylcellulose; D002351:Carrageenan; D002482:Cellulose; D000068579:Celecoxib