Spontaneous In Situ Formation of Liposomes from Inert Porous Microparticles for Oral Drug Delivery

Published on Aug 15, 2020in Pharmaceutics4.421
· DOI :10.3390/PHARMACEUTICS12080777
Maryam Farzan4
Estimated H-index: 4
(University of Basel),
Gabriela Québatte6
Estimated H-index: 6
(University of Basel)
+ 4 AuthorsMaxim Puchkov14
Estimated H-index: 14
(University of Basel)
Sources
Abstract
Despite the wide-spread use of liposomal drug delivery systems, application of these systems for oral purposes is limited due to their large-scale formulation and storage issues. Proliposomes are one of the formulation approaches for achieving solid powders that readily form liposomes upon hydration. In this work, we investigated a dry powder formulation of a model low-soluble drug with phospholipids loaded in porous functionalized calcium carbonate microparticles. We characterized the liposome formation under conditions that mimic the different gastrointestinal stages and studied the factors that influence the dissolution rate of the model drug. The liposomes that formed upon direct contact with the simulated gastric environment had a capacity to directly encapsulate 25% of the drug in situ. The emerged liposomes allowed complete dissolution of the drug within 15 min. We identified a negative correlation between the phospholipid content and the rate of water uptake. This correlation corroborated the results obtained for the rate of dissolution and liposome encapsulation efficiency. This approach allows for the development of solid proliposomal dosage formulations, which can be scaled up with regular processes.
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