Non-ionic surfactant based in-situ forming nanovesicles as controlled parenteral delivery systems

Introduction: Non-ionic surfactant (NIS) based in-situ forming vesicles (ISVs) present an attractive alternative to the traditional vesicular systems for the parental control of drug release.Methods: NIS based ISVs... [ view full abstract ]

Introduction: Non-ionic surfactant (NIS) based in-situ forming vesicles (ISVs) present an attractive alternative to the traditional vesicular systems for the parental control of drug release.

Methods: NIS based ISVs encapsulating tenoxicam were prepared using the emulsion method. TX-loaded ISVs were prepared using a 2².3¹ full factorial experimental design, where three factors were evaluated as independent variables; type of NIS; Span^®60 or Brij^®52 (A), molar ratio of NIS:Tween^® 80 (B) and phase ratio of the internal ethyl acetate to the external Captex^® oil phase (C). Percentage drug released after 1hr, particle size of the obtained vesicles and mean dissolution time were chosen as the dependent variables. Selected formulation was subjected to morphological investigation, injectability, viscosity measurements and solid state characterization. Results and Discussion: Optimum formulation showed spherical nano-vesicles in the size of 379.08 nm with an initial drug release of 37.32% in the first hour followed by a sustained drug release pattern for 6 days. DSC analysis of the optimized formulation confirmed the presence of the drug in an amorphous form with the nanovesicles. Biological evaluation of the selected formulation was performed on New Zealand rabbits as IM injection. The prepared ISVs exhibited a 45 and 28 fold larger AUC and MRT-values, respectively, compared to those for drug suspension. The obtained findings boost the use of ISVs for the treatment of many chronic inflammatory conditions.