Phase Behavior of Dried-DDA Liposomal Formulation Dispersed in HPMC Matrix in the presence of Saccharides

• Main Authors: Yusuf, Helmy, Nugraheni, Raditya, Mulyadi, Nur Aini, Setyawan, Dwi, Rosita, Noorma
• Format: Article PeerReviewed
• Language: English; English
• Published: 2017
• Subjects: R Medicine; RS Pharmacy and materia medica; RS1-441 Pharmacy and materia medica; RS200-201 Pharmaceutical dosage forms
• Online Access: http://repository.unair.ac.id/73336/1/C-18%20Artikel.pdf; http://repository.unair.ac.id/73336/2/C-18%20Validasi%20dan%20Peer%20Reviewer.pdf; http://repository.unair.ac.id/73336/; http://sphinxsai.com/2017/ph_vol10_no1/ph01.htm
• Institution: Universitas Airlangga

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.