ABSTRACT Phospholipid nanosomes are small, uniform liposomes manufactured utilizing supercritical fluid technologies. Supercritical fluids are first used to solvate phospholipid raw materials, and then decompressed to form phospholipid nanosomes that can encapsulate hydrophilic molecules such as proteins and nucleic acids. Hydrophobic therapeutics are co-solvated with phospholipid raw materials in supercritical fluids that, when decompressed, form phospholipid nanosomes encapsulating these drugs in their lipid bilayers. Mathematical modeling and semi-empirical experiments indicate that the size and character of phospholipid nanosomes depend on the several process parameters and material properties including the size and design of decompression nozzle, bubble size, pressure and the rate of decompression, interfacial forces, charge distribution and the nature of compound being encapsulated. Examples are presented for the encapsulation of a protein and hydrophobic drugs. In vitro and in vivo data on breast cancer cells and xenografts in nude mice indicate that paclitaxel nanosomes are less toxic and much more effective than paclitaxel in Cremophor EL (Taxol). Camptothecin nanosomes demonstrate that the normally very water-insoluble camptothecin can be formulated in a biocompatible aqueous medium while retaining in vivo efficacy against lymphoma xenografts in nude mice. In vitro data for betulinic acid nanosomes demonstrate enhanced efficacy against HIV-1 (EC50 of 1.01 microg/ml versus 6.72 microg/ml for neat betulinic acid). Phospholipid nanosomes may find utility in the enhanced delivery of hydrophilic drugs such as recombinant proteins and nucleic acid as well as hydrophobic anticancer and anti-HIV drugs.
- SourceAvailable from: Chau Beh
[Show abstract] [Hide abstract]
- "6. Depressurization of an Expanded Solution into Aqueous Media (DESAM)  . 7. Depressurization of an Expanded Liquid Organic Solution (DELOS)  . 8. SuperFluids (SFS-CFN) . 9. Supercritical Liposome Method . "
ABSTRACT: Formation of nano-carriers such as vesicles and micelles using dense gas processing has been under extensive research for decades. Several dense gas processes have been developed to produce nano-carriers, most of them being batch processes. In the present study, a novel continuous dense gas, known as nano-carrier by a continuous dense gas (NADEG) process was developed as an evolution of a dense gas batch process known as the Depressurization of an Expanded Solution into Aqueous Media (DESAM) process. Transforming a batch process into a continuous process is a main aspect of process intensification. The NADEG process developed in this work enhances the production output of the batch process while producing nano-carriers free of harmful residual organic solvent. The NADEG process is a one-step process for the production of nano-carriers with lower size and higher encapsulation efficiency than the nano-carriers produced by other batch processes. Encapsulation efficiencies as high as 15% were achieved using liposomes to encapsulate a model hydrophilic compound (isoniazid) while encapsulation efficiencies of 10% were achieved in polymersomes for the same model compound. Full Article: http://www.sciencedirect.com/science/article/pii/S1385894714016957Chemical Engineering Journal 04/2015; 266. DOI:10.1016/j.cej.2014.12.072 · 4.32 Impact Factor
[Show abstract] [Hide abstract]
- "However, none of these approaches has been satisfactory enough to be introduced to the clinical practice, mostly because of the lack of biocompatibility to meet the requirements of intravenous preparations. Of these, the use of lipidic carriers in the form of emulsions (Nornoo, 2008) nanoscale lipocores and liposomes (Terwogt, et al., 1997; Nuijen, et al. 2001; Singla et al. 2002; Castor, 2005; Safavy, 2008) for increasing the drug solubility are one of the most promising, but still awaiting further characterization. "
ABSTRACT: The aim of this study was to study the basic features of Taxol recognition with phospholipids by applying the thermodynamic and spectroscopic measurements. The obtained information could be used further for deductions on its precise cellular and pharmacological mechanisms of action, on improvements of its solubility properties by phospholipids, as well as for designing the novel lipidic carriers for drug delivery.Brazilian Archives of Biology and Technology 12/2010; 53(6):1351-1358. DOI:10.1590/S1516-89132010000600011 · 0.45 Impact Factor
- [Show abstract] [Hide abstract]
ABSTRACT: Essential oils have important commercial applications as preservatives and flavours, and more recently as natu-ral antimicrobial agents. These applications require a suitable formulation constituted by biodegradable compounds that protect the essential oil from degradation and evaporation at the same time that allows for a sustained release. Microcap-sules of biopolymers loaded with essential oils meet these requirements. Such microcapsules can be prepared with differ-ent processes such as spray-drying, freeze-drying and coacervation, and supercritical fluids are an advantageous medium for this purpose. Some supercritical fluid-based precipitation processes have already been applied to produce these micro-capsules. Amongst them, the results obtained with Particles from Gas Saturated Solutions (PGSS), PGSS-drying and Con-centrated Powder Form (CPF) processes are particularly promising. Recent developments in the preparation of formula-tions with supercritical fluids include the preparation of liposomes and micelles, which can be suitable carriers for essen-tial oils.