Abstract
Lipid-based formulations encompass a diverse group of formulations with very different physical appearance, ranging from simple triglyceride vehicles to more sophisticated formulations such as self-emulsifying drug delivery systems (SEDDS). Lipid-based drug delivery systems may contain a broad range of oils, surfactants, and co-solvents. They represent one of the most popular approaches to overcome the absorption barriers and to improve the bioavailability of poorly water-soluble drugs. Diversity and versatility of pharmaceutical grade lipid excipients and drug formulations as well as their compatibility with liquid, semi-solid and solid dosage forms make lipid systems most complex. Digestion of triglyceride lipids, physicochemical characteristics and solubilisation of lipid digestion products as well as intestinal permeability are some of the variable parameters of such formulations. Furthermore, among the factors affecting the bioavailability of the drug from lipid-based formulations are the digestion of lipid, the mean emulsion droplet diameter, the lipophilicity of the drug and the type of lipids. The solubility of the Active Pharmaceutical Ingredient in the Lipid System, the desorption/sorption isotherm and the digestibility of lipid vehicle are important issues to be considered for formulations of isotropic lipid formulations. This review also describes the fate of lipid formulations in the gut and the factors influencing the bioavailability from lipid-based formulations. Novel formulation systems and currently marketed products conclude this review.
Highlights
Oral lipid-based products entered the market in 1981 and currently account for approximately 3% of commercially available oral formulations
The total daily dose of active pharmaceutical excipient (API) administered by these formulations ranges from 0.25 μg to 2000mg
The GI-tract basically influences the performance of lipid-based formulations as triglycerides and their derivatives are quantitatively hydrolyzed prior to absorption
Summary
Oral lipid-based products entered the market in 1981 and currently account for approximately 3% of commercially available oral formulations. The total daily dose of active pharmaceutical excipient (API) administered by these formulations ranges from 0.25 μg to 2000mg. The total amount of lipid administered in a single capsule ranges from 0.5 to 5 g, but can be 0.1 ml up to 20 ml for oral solutions [2]. Lipid-based formulations range in complexity from simple, oneexcipient solutions based on e.g. sesame or corn oil to multi-excipient, self-emulsifying drug delivering systems (SEDDS). The excipients in lipid-based formulations include water-insoluble triglycerides (e.g., corn oil, olive oil, peanut oil, sesame oil, soyabean oil, rapeseed oil, hydrogenated vegetable oil, hydrogenated soybean oil and medium chain triglycerides of coconut oil and palm seed oil), organic liquids/semisolids (e.g., beeswax, DL-α-tocopherol, oleic acid, medium chain mono and diglycerides, propylene glycol ester of fatty acids), nonionic surfactants (e.g., cremophor EL, cremophor RH 40, cremophor RH 60, d-α-tocopherol propylene glycol 1000 succinate, glyceryl monooleate, polysorbate 20, polysorbate 80, Sorbitan monolaurate, Labrafil M-1944CS, Labrafil® M-2125CS, and Labrasol®), a phospholipid (phosphatidylcholine), and water-miscible organic solvents (polyethylene glycol 400, ethanol, propylene glycol, glycerin)
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