Stability study and lyophilization of vitamin E-loaded nanocapsules prepared by membrane contactor.

In this research, we studied the accelerated stability of vitamin E-loaded nanocapsules (NCs) prepared by the nanoprecipitation method. Vitamin E-loaded NCs were optimized firstly at the laboratory scale and then scaled up using the membrane contactor technique. The optimum conditions of the membrane contactor preparation (pilot scale) produced vitamin E-loaded NCs with an average size of 253 nm, polydispersity index 0.19 and a zeta potential -16 mV. The average size, polydispersity index and zeta potential values were 185 nm, 0.12 and -15 mV, respectively for the NCs prepared at laboratory scale. No significant changes were noticed in these values after 3 and 6 months of storage at high temperature (40±2 °C) and relative humidity (75±5%) in spite of vitamin E sensitivity to light, heat and oxygen. The entrapment efficiency of NCs prepared at pilot scale was 97% at the beginning of the stability study, and became (95%, 59%) after 3 and 6 months of storage, respectively. These values at lab-scale were (98%, 96%, and 89%) at time zero and after 3 and 6 months of storage, respectively. This confirms the ability of vitamin E encapsulation to preserve its stability, which is one major goal of our work. Lyophilization of the optimized formula at lab-scale was also performed. Four types of cryoprotectants were tested (poly(vinyl pyrrolidone), sucrose, mannitol, and glucose). Freeze-dried NCs prepared with sucrose were found acceptable. The other lyophilized NCs obtained at different conditions presented large aggregates.

Preparation of vitamin E loaded nanocapsules by the nanoprecipitation method: from laboratory scale to large scale using a membrane contactor.

Vitamin E or α-tocopherol is widely used as a strong antioxidant in many medical and cosmetic applications, but is rapidly degraded, because of its light, heat and oxygen sensitivity. In this study, we applied the nanoprecipitation method to prepare vitamin E-loaded nanocapsules, at laboratory-scale and pilot-scale. We scaled-up the preparation of nanocapsule with the membrane contactor technique. The effect of several formulation variables on the vitamin E-loaded nanocapsules properties (mean diameter, zeta potential, and drug entrapment efficiency) was investigated. The optimized formulation at laboratory-scale and pilot-scale lead to the preparation of vitamin E-loaded nanocapsules with mean diameter of 165 and 172 nm, respectively, and a high encapsulation efficiency (98% and 97%, respectively).