Year-end Sale % OFF 
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.
Highlights
Liposomes are one of the most studied drug delivery systems, owing to their ability to encapsulate various active substances of hydrophobic and hydrophilic nature, their biocompatibility, and design flexibility
Cumulant analysis of the samples obtained a z-average of 261 ± 83.07 and 420 ± 86.86 nm P(hpaormlyacdeiustpicse2r0s2it0y, 1i2n, dx edxoi0: .60 ± 010) for the liposomes in Simulated gastric fluid without enzyme (SGF) and phosphate buffer, respectively. 7 of 18
The in situ formation of liposomes from a combination of phospholipids and porous carriers in the simulated GI conditions is an effective approach for formulating liposomes for oral delivery
Summary
Liposomes are one of the most studied drug delivery systems, owing to their ability to encapsulate various active substances of hydrophobic and hydrophilic nature, their biocompatibility, and design flexibility. Liposomes are used for oral bioavailability enhancement of low-soluble or low-permeable active ingredients [4,5,6,7], as well as compounds with low stability in the gastrointestinal (GI) tract [2,8,9,10,11]. Compared to the widely used conventional solid dosage forms (i.e., tablets), production of liposomes is demanding due to production challenges, as well as physical and chemical stability issues. Liposomal dispersions that are stored in liquid form have a limited stability due to the risk of sedimentation, aggregation, and phospholipid hydrolysis [14]. It would be beneficial to produce solid powders that can be processed using conventional tableting equipment
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
