Electrospray technology as a probe for single step fabrication of glipizide loaded nanocochleates with enhanced bioavailability

Abstract

Nanocochleates (NCs) are amongst the nanoformulations gaining wide popularity owing to their ability to improve biopharmaceutical performance of drug molecules remarkably. However, biggest drawback of this nanocarrier is that it requires minimum two steps for synthesis which limits its industrial scalability. Considering the same, the present work was designed with an objective to assess suitability of electrospray technique in the preparation of biomaterial based NCs. Glipizide (GPZ) was chosen as a model drug for preparation of NCs. Briefly, GPZ, phosphatidylcholine and cholesterol were dissolved in methanol and co-axially sprayed into a pool of CaCl2 solution. Factorial design (22) approach was used for batch optimization. The optimized batch was evaluated for surface morphology, FTIR, DSC, zeta potential, in-vitro drug release study and in-vivo evaluation in male wistar rats. FESEM images confirmed formation of NCs using electrospray technique. Negative zeta potential (-14.36 ± 0.55 mV) of optimized batch reflected high stability of the sample. GPZ was released in a controlled manner from the optimized GPZNC. In-vivo pharmacokinetic study demonstrated significant increase in Cmax (2-fold) and AUC (3-fold) upon entrapment of GPZ into NCs. Thus, the present work unfolded suitability of electrospray technology toward single step preparation of Phosphatidylcholine and Cholesterol biomaterial based nanocochleates over currently used two step preparation techniques.