Freeze-drying of liposomal nanohybrid cerasomes with cryoprotectants: In vitro and in vivo evaluation

ABSTRACT

Liposomal nanohybrid cerasomes as a new type of drug carrier has been widely applied in the controlled release of drugs. However, such vesicles containing polysiloxane networks on the surface were liable to aggregate during the process of freeze-drying for routine storage. To solve this problem, several previously reported cryoprotectants including sucrose, mannitol, sodium alginate, and glucose were chosen for protecting the 10-hydroxycamptothecin-loaded liposomal nanohybrid cerasomes (The drug encapsulation efficiency was of 67.31 ± 7.42% and the drug loading content was of 6.73 ± 0.74%.) in freeze-drying process. It was found that liposomal nanohybrid cerasomes treated with mannitol can be well dispersed, and the results of particle size and zeta potential showed that the drug-loaded vesicles were well protected with mannitol. In vitro drug release and in vivo pharmacokinetic study showed that the optimal addition amount of mannitol was twice the mass of the drug-loaded vesicles, whereby the cumulative release profile and the pharmacokinetic parameters were similar in the freeze-dried and fresh vesicles.

KEYWORDS:

• Cryoprotectant
• freeze-drying
• liposomal nanohybrid cerasomes

Additional information

Funding

This research is financially supported by the “948” Project of the State Forestry Administration, China (2012-4-04), the Fundamental Research Funds for the Central Universities (DL13EA02).