Amelioration of lipophilic compounds in regards to bioavailability as self-emulsifying drug delivery system (SEDDS)
High lipophilicity and poor aqueous solubility are the endemic problems of new drug molecules. Sixty to seventy percent of these drugs are unable to solubilize completely in aqueous media, or have very low permeability. This hampers their oral absorption and further leads to their poor bioavailability. Various researches are in progress to overcome these limitations. Novel technologies like nano-carrier systems have become popular for improving the solubility of drugs.
Main body
Lipid-based formulations, among nano systems, are taking pace for the enhancement of solubility, oral absorption, and hence the bioavailability of drugs. Among the lipid formulations, self-emulsification systems are gaining popularity by offering various advantages to delivery systems. Self-emulsifying drug delivery systems (SEDDS) are isotropic blends of oil and surfactant/co-surfactants. These ingredients upon gentle agitation in aqueous media results in the formation of o/w emulsion. In spite of many works published in SEDDS, the major concerns of this article are to discuss the various approaches to formulate a good lipid-based carrier system for poorly aqueous soluble drugs, role of various polymers, and their categories used in the formulation along-with the modern technologies used for enhancing the stability of liquid SEDDS. This review majorly focuses upon the problems related to the poor aqueous solubility of the newer lipid molecules and the solutions to overcome their solubility and in addition bioavailability.
Conclusion
As per the researches done in formulation and optimization of SEDDS for the enhancement of bioavailability of lipophilic molecules, it can be stated that the aqueous solubility as well as bioavailability can be increased by many folds compared to their marketed or other oral formulations. Continue here and access the full open access publication
List of oils used in the formulation of SEDDS/SMEDDS/SNEDDS:
- Glyceryl monolinoleate
- Maisine 35-1
- Neobee M5
- Miglyol 840
- Labrafac lipophile WL139
- Kolliphor RH 40
- Oleic acid
- Captex 200
- Captex 355 EP/NF
- Other vegetable ad edible oils (castor, sesame, olive, coconut, etc.)
Some examples of co-surfactants and co-solvents:
- Mixture of glycerol an ethanol
- Transcutol
- Capmul MCM
- Glycerol
- Polyethylene glycol
- PEG 400
- Glycofurol
Baghel, P., Roy, A., Verma, S. et al. Amelioration of lipophilic compounds in regards to bioavailability as self-emulsifying drug delivery system (SEDDS). Futur J Pharm Sci 6, 21 (2020). https://doi.org/10.1186/s43094-020-00042-0