Lipid based formulations as supersaturating oral delivery systems: from current to future industrial applications

Lipid-based formulations, in particular supersaturated lipid-based formulations, are important delivery approaches when formulating challenging compounds, as especially low water-soluble compounds profit from delivery in a pre-dissolved state. In this article, the classification of lipid-based formulation is described, followed by a detailed discussion of different supersaturated lipid-based formulations and the recent advances reported in the literature. The supersaturated lipid-based formulations discussed include both the in situ forming supersaturated systems as well as the thermally induced supersaturated lipid-based formulations. The in situ forming drug supersaturation by lipid-based formulations has been widely employed and numerous clinically available products are on the market. There are some scientific gaps in the field, but in general there is a good understanding of the mechanisms driving the success of these systems. For thermally induced supersaturation, the technology is not yet fully understood and developed, hence more research is required in this field to explore the formulations beyond preclinical studies and initial clinical trials.

Table 3. Tradenames of lipid excipients, their composition and main function mentioned in the main text or tables.

Tradename	Potential synonym	Composition
Oils
Capmul® MCM		Mixture of medium chain mono- and diglycerides
Captex® 300		Medium chain triglyceride
LabrafacTM lipophile WL1349	LabrafacTM CC	Medium chain triglyceride
Maisine® CC	Maisine® 35-1	Mixture of long chain mono-, di- and triglycerides
Miglyol® 812N		Medium chain triglyceride
PeceolTM		Glyceryl monooleate
Surfactants
BrijTM L4		Polyethylene glycol dodecyl ether
Capmul® PG8		Propylene glycol monocaprylate
Caproyl® 90		Propylene Glycol Monocaprylate
Gelucure® 44/14		Lauroyl polyoxyl-32 glycerides
Gelucure® 48/16		Polyoxyl-32 stearate
Kolliphor® EL	Cremophor EL	PEG-35 hydrogenated castor oil
Kolliphor® RH40	Cremophor RH40	PEG-40 hydrogenated castor oil
Kolliphor® HS15	Solutol HS15	Polyoxyl 15 hydrostearate
Labrafac® PG		Propylene glycol dicaprolate/dicaprate
Labrafil® M1944CS		Oleoyl polyoxyl-6 glycerides
Labrasol® ALF	Labrasol®	Caprylocaproyl polyoxyl-8 glycerides
LauroglycolTM FCC		Propylene glycol monolaurate
Pluronic® F-127	Poloxamer 407	2-[2-(2-hydroxyethoxy)propoxy]ethanol
Polysorbate 80	Tween 80	Polyoxyethylene (80) sorbitan monooleate
Polysorbate 20	Tween 20	Polyoxyethylene (20) sorbitan monolaurate
Vitamin E-TPGS		D-α-tocopheryl polyethylene glycol succinate
Cosolvents
PEG		Polyethylenglycol
Tetraglycol		Tetraethylene glycol
Transcutol® P	Transcutol® HP	Diethylene glycol monoethyl ether

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René Holm, Martin Kuentz, Alexandra-Roxana Ilie-Spiridon, Brendan T. Griffin, Lipid based formulations as supersaturating oral delivery systems: from current to future industrial applications, European Journal of Pharmaceutical Sciences, 2023, 106556, ISSN 0928-0987,
https://doi.org/10.1016/j.ejps.2023.106556.