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.
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...
Abstract Myricitrin has many pharmacological effects, such as anti-inflammation, liver protection and anti-oxidation. However, its clinical application is limited by poor solubility and low oral bioavailability. The preparation of myricitrin-loaded proliposomes (MPs) was achieved via the combination of thin-film dispersion technique and freeze-drying method. The in vitro release of MPs compared with free myricitrin was measured in different dissolution media while the pharmacokinetic study was a...
#1Jingfu Jia(SYSU: Sun Yat-sen University)H-Index: 4
#2Kerong Zhang(SYSU: Sun Yat-sen University)H-Index: 3
Last. Fahuan Ge(SYSU: Sun Yat-sen University)H-Index: 5
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Abstract In present study, berberine proliposomes (ber-PL) of powder state that can form liposomal structure via self-assemble in water was prepared using solution enhanced dispersion by supercritical CO2 (SEDS) to improve the oral bioavailability of berberine. Several important parameters were optimized using Box-Behnken design to get ber-PL with high entrapment efficacy (EE) of 90.3% ± 4.9%. Physicochemical characterization showed the optimum ber-PL was amorphous spherical nanoparticles and co...
Accurate analysis of intraparticle distribution of substances within porous drug carriers is important to optimize loading and subsequent processing. Mercury intrusion porosimetry, a common technique used for characterization of porous materials, assumes cylindrical pore geometry, which may lead to misinterpretation. Therefore, imaging techniques such as focused ion beam scanning electron microscopy (FIB-SEM) help to better interpret these results. The purpose of this study was to investigate th...
Abstract Liposomes mimic natural cell membranes and have long been investigated as drug carriers due to excellent entrapment capacity, biocompatibility and safety. Despite the success of parenteral liposomes, oral delivery of liposomes is impeded by various barriers such as instability in the gastrointestinal tract, difficulties in crossing biomembranes, and mass production problems. By modulating the compositions of the lipid bilayers and adding polymers or ligands, both the stability and perme...
Nowadays, the freeze-drying of liposome dispersions is still necessary to provide a solid dosage form intended for different routes of administration (i.e., parenteral, oral, nasal and/or pulmonary). However, after decades of studies the optimization of process conditions remains still challenging since the freezing and the dehydration destabilize the vesicle organization with the concomitant drug leakage. Starting from the thermal properties of phospholipids, this work reviews the main formulat...
Proliposome powders were prepared via a slurry method using sorbitol or D-mannitol as carbohydrate carriers in 1:10 or 1:15 w/w lipid phase to carrier ratios. Soya phosphatidylcholine (SPC) and cholesterol were employed as a lipid phase and Beclometasone dipropionate (BDP) was incorporated as a model drug. Direct compaction using a Minipress was applied on the lipid-enriched powder in order to manufacture proliposome tablets. Sorbitol-based proliposome tablets in a 1:15 w/w ratio were found to b...
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...
Orally disintegrating tablets (ODT) are comfortable and safe drug delivery methods beneficial for all age groups of patients. ODTs are characterized by fast disintegration, high physical stability, taste masking and acceptable mouthfeel. In this work, the applicability of Functionalized Calcium Carbonate (FCC) to formulate ODTs with enhanced mouthfeel was elaborated and tested for acceptability on twenty healthy volunteers, using a 10-step visual analog scale Mechanical characteristics of the OD...
The knowledge and experiences obtained with oral phospholipid excipients is increasing continuously. Nevertheless the present number of oral products using these excipients as essential excipient is very limited. This is remarkable to note, since phospholipids play a significant role in the food uptake mechanisms of the GI tract and these mechanisms could be translated into suitable dosage forms and corresponding drug delivery strategies. In addition, phospholipid excipients are multifunctional ...
Last. Yang Shuibing(ZJU: Zhejiang University)H-Index: 7
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Medium-chain fatty acids (MCFAs) have been proven as an easy energy source and active ingredient to prevent obesity and other metabolic disorders. However, the inherent hydrophobic nature of MCFAs causes poor aqueous solubility and dissolution in the gastrointestinal (GI) tract, thus limiting their applications in aqueous foods. To address these issues, a nutraceutical carrier system was developed by coating nanoliposomes with carboxymethyl chitosan (CMCS) through a series of well-designed proce...
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. [...]
