Effect of non-phospholipid-based cationic and phospholipid-based anionic nanosized emulsions on skin retention and anti-inflammatory activity of celecoxib

Pharm Dev Technol. 2013 Jul-Aug;18(4):761-71. doi: 10.3109/10837450.2011.586038.

Abstract

Context: Celecoxib (CXB, 0.2 g)-loaded anionic and cationic nanosized emulsions were prepared by a well-established combined emulsification method.

Objectives: 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.

Discussion and conclusion: 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.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Anions
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / pharmacokinetics
  • Anti-Inflammatory Agents / pharmacology*
  • Carrageenan / toxicity
  • Cations
  • Celecoxib
  • Cellulose / analogs & derivatives
  • Cellulose / metabolism
  • Delayed-Action Preparations
  • Diffusion
  • Disease Models, Animal
  • Edema / drug therapy
  • Edema / pathology
  • Emulsions
  • Inflammation / drug therapy
  • Inflammation / pathology
  • Male
  • Nanoparticles*
  • Phospholipids / chemistry
  • Pyrazoles / administration & dosage
  • Pyrazoles / pharmacokinetics
  • Pyrazoles / pharmacology*
  • Rats
  • Rats, Wistar
  • Skin / metabolism
  • Skin Absorption*
  • Sulfonamides / administration & dosage
  • Sulfonamides / pharmacokinetics
  • Sulfonamides / pharmacology*

Substances

  • Anions
  • Anti-Inflammatory Agents
  • Cations
  • Delayed-Action Preparations
  • Emulsions
  • Phospholipids
  • Pyrazoles
  • Sulfonamides
  • acetylcellulose
  • Carrageenan
  • Cellulose
  • Celecoxib