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)
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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It has been known that a considerable number of drugs in clinical use or under development are water-insoluble drugs with poor bioavailability (BA). The liposomal delivery system has drawn attention as one of the noteworthy approaches to increase dissolution and subsequently absorption in the gastrointestinal (GI) tract because of its biocompatibility and ability to encapsulate hydrophobic molecules in the lipid domain. However, there have been several drawbacks, such as structural instability i...
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Abstract The recently introduced functionalized calcium carbonate (FCC), a porous microparticle with a nano-structured, lamellar surface, shows promising properties in the field of oral drug delivery. In this work, FCC was loaded with biomolecules e.g. lysozyme (Lys) and bovine serum albumin (BSA) in order to investigate its suitability to deliver protein based drugs. Loading efficiency for our model proteins was >90% and enzyme activity was preserved as demonstrated by Michaelis-Menten enzyme k...
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Cited By2
#1Huijuan Zheng (NCU: Nanchang University)
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The use of lipid-based nanosystems, including lipid nanoparticles (solid lipid nanoparticles—SLN, and nanostructured lipid carriers—NLC), nanoemulsions, and liposomes, among others, is widespread. [...]