title: Preparation, optimization, and evaluation of Zaltoprofen-loaded microemulsion and microemulsion-based gel for transdermal delivery.
abstract: BACKGROUND
  Zaltoprofen, a non-steroidal anti-inflammatory drug, has potent inhibitory action against nociceptive responses. However, gastrointestinal ulcer accompanied with anemia due to the bleeding are most cited side effects associated with it. Due to this, administration of Zaltoprofen is not suitable for individuals with gastric ulcer. Thus, there is unmet need to develop an alternative delivery system that will be easy to administer and can avoid ulcerogenic side effects associated with it.
  
  
  OBJECTIVE
  Present study was aimed to prepare and evaluate microemulsion (ME) and microemulsion-based gel formulation of Zaltoprofen for transdermal delivery.
  
  
  METHODS
  Pseudo-ternary phase diagrams were utilized to prepare ME formulations. Effect of surfactant and co-surfactant mass ratio on the ME formation and permeation of ME were evaluated and formulation was optimized. Permeation studies were performed using excised pigskin was studied. Efficacy of optimized formulations was evaluated in rat model of inflammation and pain.
  
  
  RESULTS
  Composition of optimized formulation was 1% (w/w) Zaltoprofen, 20% (w/w) Capryol 90, 50% (w/w) Smix (2:1, Cremophor RH 40 and Transcutol P). Optimized formulation showed globule size of 22.11 nm, polydispersity index of 0.251 and zeta potential of -11.4 mV. ME gel was found safe in skin irritation study. Significant analgesic activity and anti-inflammatory activity of ME gel was observed in hot plate test and rat paw edema test, respectively.
  
  
  CONCLUSIONS
  In conclusion, results of present study suggest that ME could be a promising formulation for transdermal administration of Zaltoprofen.
authors.affiliation: a Department of Quality Assurance and.
authors.forename: Ratnesh
authors.initials: R
authors.lastname: Mishra
authors.affiliation: b Department of Pharmacology , SVKM's Dr. Bhanuben Nanavati College of Pharmacy , Mumbai , Maharashtra , India.
authors.forename: Kedar S
authors.initials: KS
authors.lastname: Prabhavalkar
authors.affiliation: b Department of Pharmacology , SVKM's Dr. Bhanuben Nanavati College of Pharmacy , Mumbai , Maharashtra , India.
authors.forename: Lokesh Kumar
authors.initials: LK
authors.lastname: Bhatt
mesh_terms: D000279:Administration, Cutaneous; D000700:Analgesics / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D001578:Benzopyrans / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical; D004195:Disease Models, Animal; D016503:Drug Delivery Systems; D004655:Emulsions / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D005782:Gels / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D007249:Inflammation / Q000188:drug therapy; D007700:Kinetics; D010146:Pain / Q000188:drug therapy; D011422:Propionates / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000187:drug effects; D012869:Skin Absorption / Q000187:drug effects; D013501:Surface-Active Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001578:Benzopyrans; D004655:Emulsions; D005782:Gels; D011422:Propionates; D013501:Surface-Active Agents; C043940:pyranoprofen
keywords: Analgesic; Zaltoprofen; microemulsion-based gel