Lipid-based formulations, bioenhancers by nature

27 January 2022

FiercePharma

Oral bioavailability of drugs is often limited due to poor solubility and/or limited intestinal permeability. To overcome these issues numerous strategies have been developed, among which lipid-based formulations deserved a special place thanks to many benefits illustrated hereafter by selected examples. 

Addressing more challenges with an augmented range of bioenhancers

Gattefossé is a leading provider of lipid excipients and lipid-based drug delivery technologies. Pioneering in the field, with early concepts and patents, including the development of SEDDS (Self Emulsifying Drug Delivery System), Gattefossé continues to innovate with new excipients and applications. With strong expertise in the formulation of challenging drugs, we offer a complete portfolio of products for oral bioavailability enhancement. 

We have recently widened our range of high quality, functional excipients for oral bioavailability enhancement with Labrafac™ MC60, glycerol monocaprylocaprate EP/NF and Gelucire® 59/14, mixture of lauroyl PEG-32 glycerides EP/NF and PEG 6000 EP/NF. Depending on the drug properties, the process and the desired final dosage form, formulators can choose the excipients that best suits their needs.


Unlocking oral bioavailability potential with lipid-based formulations 

Poor solubility, poor permeability, and pre-systemic elimination are factors that can limit absorption of some drugs. Lipid excipients have the capability to overcome these hurdles and to enhance oral bioavailability through different mechanisms:


Getting inspired from marketed medicines

A review of marketed lipid-based formulations showed that soft gel capsules and oral solutions/suspensions are the predominant dosage forms, followed by hard gel capsules1.


H. Bennett-Lenane, J.P. O'Shea, C.M. O'Driscoll, B.T. Griffin. J. Pharm. Sci. 109 (2020) 3248–3261
https://www.tga.gov.au/sites/default/files/auspar-enzalutamide-141124.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/021319s032lbl.pdf
https://www.medicines.org.uk/emc/product/11305/smpc#PRODUCTINFO 
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212157s000lbl.pdf 
Soraya Hengsawas Surasarang and Robert O. Williams. (2016), Co-solvent and Complexation Systems, Pages 215-256, in Formulating Poorly water-soluble drugs ISBN 2210-7371
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021951s000lbl.pdf

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