Nano-formulated sterile aqueous solutions of active compounds

Lipodisq™ are novel lipid/polymer nanoparticles that have been developed as mimics of naturally-occurring high-density lipoproteins (HDL). Lipodisq™ particles are in the size range of 11 to 40 nm in diameter enabling enhanced penetration and diffusion into membranes. These nanodisc lipid particles are composed of a hydrophilic shell and hydrophobic core in which hydrophobic active agents can be carried and protected.

The size and shape of the chaperone molecule is a critical factor in Lipodisq™ formation and also defines the properties of the particle, i.e. particle size and/or its biodegradability. Internal properties of the phospholipid membrane support the disposition and stabilization of drug molecule candidates and preserve the native conformation of membrane-bound molecules. The resulting encapsulated actives are rendered water-soluble and optimized for intracellular penetration/delivery via endosomal uptake mechanisms.

Figure: Nanoparticle (11-40 nm) drug delivery system comprising a discoidal phospholipid bilayer membrane stabilized by an annular chaperone molecule.

Compounds powered by Lipodisq™ features

• Actives in Lipodisq™ are biosynthetic water-soluble nanodiscs prepared under SOPs using selected optimized lipid compositions for stable, high-loading capacity of encapsulated active ingredients.
• Actives in Lipodisq™ are detergent-free nano-formulations made of styrene-maleic acid copolymer-lipid particles (SMALP).
• Actives in Lipodisq™ retain the biological activity of the active compound with enhanced bioavailability.
• Lipodisq™ solutions show a good safety profile and are suitable for in vitro and in vivo investigations.

Special features of Innaxon compounds powered by Lipodisq™

• >10¹¹ particles per ml as determined by Dynamic Light Scattering (DLS).
• Tested in cell culture (human macrophage cell line as tested by MTT viability test).
• Formulations are soluble in water, PBS, Tris and other physiological solutions as formulated in a proprietary, thermostable, aqueous lipid nanoparticulate formulation.
• Formulations are certified sterile solutions with a physiological pH range.

Selection of antiviral and immunomodulating compounds powered by Lipodisq™:

New Ready-to-use Nano-formulated Aqueous Solutions (1 mg/ml)

Literature references

• Tonge SR, Tighe BJ. Responsive hydrophobically associating polymers: a review of structure and properties. Adv Drug Deliv Rev. 2001;53(1):109-122.
• Orwick MC, Judge PJ, Procek J, et al. Detergent-free formation and physicochemical characterization of nanosized lipid-polymer complexes: Lipodisq. Angew Chem Int Ed Engl. 2012;51(19):4653-4657.
• Dörr JM, Scheidelaar S, Koorengevel MC, et al. The styrene-maleic acid copolymer: a versatile tool in membrane research. Eur Biophys J. 2016;45(1):3-21.
• Tanaka M, Miyake H, Oka S, Maeda S, Iwasaki K, Mukai T. Effects of charged lipids on the physicochemical and biological properties of lipid-styrene maleic acid copolymer discoidal particles. Biochim Biophys Acta Biomembr. 2020;1862(5):183209.
• Torgersen ML, Judge PJ, Bada Juarez JF, et al. Physicochemical characterization, toxicity and in vivo biodistribution studies of a discoidal, lipid-based drug delivery vehicle: lipodisq nanoparticles containing doxorubicin. J Biomed Nanotechnol. 2020;16(4):419-431.

Not for cosmetic, diagnostic or therapeutic human or veterinary use!