Review – An update on the use of oral phospholipid excipients
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 biodegradable, non-toxic excipients, which can be used in oral dosage forms as wetting agents, emulsifier, solubilizer and matrix forming excipients. Especially natural phospholipid excipients, made from renewable sources, may be considered as environmentally friendly excipients and as a viable alternative to synthetic phospholipid and non-phospholipid analogues. This review describes 1) essential physico-chemical properties of oral phospholipid excipients 2) the fate of orally administered phospholipids with respect to absorption and metabolism in the GI tract 3) the main dosage forms used for oral administration containing phospholipids. These elements are critically assessed and areas of future research of interest for the use of oral phospholipid excipients are summarized.
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About this aritcle: Peter van Hoogevest, Review – An update on the use of oral phospholipid excipients, European Journal of Pharmaceutical Sciences, Volume 108, 2017, Pages 1-12, ISSN 0928-0987, https://doi.org/10.1016/j.ejps.2017.07.008. (https://www.sciencedirect.com/science/article/pii/S0928098717304074)
Conclusions
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 principle, due to their diversity in physicochemical properties and lack of toxicity (natural) phospholipids can replace many alternative synthetic excipients. For the pharmaceutical industry this means that the use of natural phospholipids will increase the over-all sustainability balance of their products. In addition, phospholipid excipients offer excellent opportunities to circumvent existing formulation patents or generate formulation patents and generate resulting exclusive line extension products.
In this Special Issue many interesting studies are presented highlighting the potential use of these excipients. In addition, they invite to intensify the pharmaceutical technological research with these fascinating excipients.
The review also shows that certain areas of interest need to be elaborated in order to increase or complete the understanding of the underlying beneficial mechanisms related with the use of phospholipids. Need for further research can e.g. be found in area like taste masking, use of phospholipids in buccal/chewable formulations, improvement of the degree of oral absorption of poorly water soluble drugs by systematically comparing the available phospholipid classes (saturated or unsaturated di- and monoacyl phospholipids), bridging solid dispersion with excess of drug to lipid and phytosome formulations with drug to lipid weight ratios of about 1:1, triggering the excretion of bile by means of cholecystokinin release, which release is triggered by hydrolyzed fatty acids from diacyl or monoacyl- phospholipids, and the use of higher melting phospholipid as matrix material for controlled release solid dosage forms.
The Phospholipid Research Center in Heidelberg, Germany will continue to support research in these directions.