Non‐Aqueous Phospholipid Concentrates for Increasing the Bioavailability of Poorly Soluble Compounds

Abstract

The properties and use of liquid non-aqueous phospholipid concentrates (NAPC) are reviewed. They are mainly used to solubilize poorly water-soluble drug substances to enhance their oral bioavailability, but they also find applicability in dietetics and cosmetics. Due to the large-scale availability of these concentrates at good manufacturing practice quality including Drug Master File (DMF) documentation, they can be used for pre-clinical screening and clinical testing and as market form, as demonstrated by the product of Wyeth/Pfizer, Rapamune, enabling a cost effective and fast dosage form development. When needed, NAPC can be converted to solid dosage forms by means of a capsule fill or addition of adsorbing excipients. It is concluded that NAPC deserve more attention and a broader use in the life science industry. Practical Applications: NAPCs are suitable as pre-clinical formulation vehicle for screening of the oral bioavailability of poorly water-soluble compounds. The same formulation can be used for clinical testing and market introduction, allowing a fast track dosage form development. When needed NAPC can be converted to solid dosage forms. NAPC have also applicability in dietetics and cosmetics to solubilize poorly water-soluble compounds.

The Use of Phospholipids to Make Pharmaceutical Form Line Extensions

“…Such liquid concentrates may accelerate the pharmaceutical dosage form development, gives great dose flexibility, and enable a quick introduction of the product on the market. [ 312 ]…”

“…Such liquid concentrates may accelerate the pharmaceutical dosage form development, gives great dose flexibility, and enable a quick introduction of the product on the market. [312] Most databases on the pediatric use of excipients only mention the excipients, which may cause problems for this patient population. [355] The developer of a dosage form would like to know as well which excipients can be used.…”

“…[ 313 ] Also, the gastric irritation caused by acetylsalicylic acid (Aspirin) could be reduced in preclinical models by using PHOSAL 35 SB (the composition of PHOSAL 35 SB can be found in ref. [312]). These observations were the impetus for the commercial development of PL2200 Aspirin (Vazalore) by PLx Pharma Inc. (Houston, USA) combining aspirin with PHOSAL 35 SB.…”

“…PLx Pharma is reported to perform soon a bioequivalence study of Vazalore 325 mg dose (in comparison of the original formulation of 2013 and a new formulation), and a corresponding sNDA (subordination, non-disturbance and attornment agreement) submission is expected by year-end of 2021. [317] The [ 312] company develops similar phospholipid-based Pharmaceutical Form Line Extensions for ibuprofen (Phase I), indomethacin, and diclofenac, which show improved GI safety in preclinical models.…”

The Phospholipid Research Center: Current Research in Phospholipids and Their Use in Drug Delivery

“…Due to their physiological roles, phospholipids possess a very low toxicity profile and can be used for any route of administration [ 8 ]. The structural diversity of phospholipids and the resulting variability of chemical, biophysical, and technological properties leads to wide use of phospholipids in various pharmaceutical formulations [ 9 , 10 , 11 , 12 , 13 ]. They can be technologically used as an emulsifier, wetting agent, solubilizer, and agent in the formation of liposomes and mixed micelles, to name but a few.…”