Helmy Yusuf and Nugraheni, Raditya and Mulyadi, Nur Aini and Setyawan, Dwi and Rosita, Noorma (2017) Phase Behavior of Dried-DDA Liposomal Formulation Dispersed in HPMC Matrix in the presence of Saccharides. International Journal of Pharm Tech Research, 10 (1). pp. 50-56. ISSN 0974-4304

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Abstract

The present study describes the effect of saccharides and hydroxypropyl methylcellulose (HPMC) matrix on phase behavior of dehydrated cationic dimethyl- dioctadecylammonium (DDA)-based liposomes. Saccharides such as sucrose, lactose and mannitol,have been reportedpreserve the lipid membranes during drying, whilst HPMC matrix is widely used in solid dispersion to prevent aggregation and/or recrystallization.The study revealed that addition of sucrose and HPMCin the formulation demonstrated a miscible mixture that might construct a stable dried liposomal formulation. DTA data showed that sucrose (5%w/v) and HPMC added to DDA liposomal formulation were relatively more miscible with the mixtures; whereas lactose and mannitol at the same concentration of 5% showed phase separation from the mixtures in the dehydrated state. Furthermore, XRD and SEM analysis exhibited supporting evidences in which formulation using sucrose and lactose showedrelatively less crystalline-forming properties compared to formulation using mannitol. Recrystallization that cause phase separation might trigger leakage and further affect the efficacy of the entrapped drug/antigen. From these data, it might be concluded that a driedliposomal formulation can be prepared in the presence of sucrose (lyoprotectant) that is dispersed in HPMC matrix. The protective mechanism of sucrose (5%w/v) and HPMC matrix is proposed through inhibition of the recrystallization which causes phase separation; indicated by DTA, SEM and XRDdata. The present study revealed prospective advantages of using sucrose and HPMC in development of dried – DDA liposomal formulations. Keywords : Liposomes, DDA, Sucrose, Lactose, Mannitol, HPMC, Phase Separation.

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