Formulation, Optimization, Heamocompatibility and pharmacokinetic evaluation of PLGA Nanoparticles containing Paclitaxel.

OBJECTIVE: Paclitaxel (PTX) loaded Polymer (PLGA) based nanoformulation was developed with the objective of formulating cremophore EL free nanoformulation intended for i.v use.

SIGNIFICANCE: The polymeric PTX nanoparticles free from the cremophore EL will help in eliminating the shortcomings of the existing delivery system as cremophore EL causes serious allergic reactions to the subjects after intravenous use. Methods& Results: PTX loaded nanoparticles were formulated by nanoprecipitation method. The diminutive nanoparticles (143.2 nm) with uniform size throughout (PDI-0.115) and high entrapment efficiency (95.34%) were obtained by the employing Box Behnken design for the optimization of the formulation with the aid of desirability approach based numerical optimization technique. Optimized levels for each factor viz. polymer concentration (X1), amount of organic solvent (X2) & surfactant concentration (X3) were 0.23%, 5ml % & 1.13% respectively. Results of the haemocompatibility studies confirmed the safety of PLGA based nanoparticles for intravenous administration. Pharmacokinetic evaluations confirmed the longer retention of PTX in systemic circulation.

CONCLUSION: In a nutshell, the developed polymeric nanoparticle formulation of PTX precludes the inadequacy of existing PTX formulation and can be considered as superior alternative carrier system of the same.