Liposeuticals, Inc. is a specialty pharmaceuticals firm focused on the development of next-generation proprietary formulations of sterile injectable drugs, principally aimed at the domains of anesthesiology, oncology and infectious disease. The firm has developed a revolutionary approach to the formulation of non-water-soluble drugs, which enables the creation of products with greater stability, superior shelf life, improved ease of manufacturing and enhanced safety. The firm's pipeline is specifically geared towards development via the 505(b)(2) pathway at the United States Food and Drug Administration (FDA), which substantially expedites the development, review and approval timeline. Liposeuticals also seeks to extend the commercial window of its products through the generation of novel intellectual property and other regulatory exclusivity available via the Hatch-Waxman Act.
Sterile Injectable Products Market
The use of intravenous injection is a preferred mode of administration in the hospital setting. Currently, the U.S. sterile injectables market is estimated to be $7 billion annually, and comprises many broadly-used pharmaceuticals, which are typically deployed to treat potentially life-threatening conditions such as cancer and infectious disease. The U.S. injectables market is slated to grow at a double-digit percentage pace annually for the foreseeable future.
Existing Technology Platform Limitations
In our view, existing methods used to formulate water-insoluble compounds for sterile injectable delivery are sub-optimal and may place patients at risk. Certain drugs may be difficult or inconvenient to reconstitute and prepare, while others are the subject of chronic shortages due to poor stability and shelf life. Manufacturing inconsistencies and product recalls have historically plagued the sterile injectables sector due to deficiencies in the processes used to produce emulsion-, nanoparticle- or liposomally-based products.
Sugar-Lipid Conjugate Approach
The core of the LipoSeuticals value proposition is the firm's patented, non-toxic, drug reformulation technology platform, which utilizes pure sugar-lipid polymers (oligomer purity > 95%). Sugar-lipid polymers are made of lipid molecules, carbohydrates and inert biological polymers, i.e., PEG (polyethylene glycol). They can solubilize compounds and disperse them in an aqueous solution.
Both sugar and PEG are polar; they have a hydrophilic and ionizable head, while the hydrophobic tail consists of long fatty acid chains. When enough sugar-lipid polymer molecules are present in water, the hydrophobic tails spontaneously associate to exclude water, forming a bi-layer, which allows therapeutic agents with poor native water solubility to be solubilized. This permits Liposeuticals to produce true solutions - not emulsions or suspensions - of water-insoluble drugs for administration via intravenous injection. The firm only uses excipients that have Generally Regarded As Safe (GRAS) status, permitting product development via the 505(b)(2) route on the basis of clinical bioequivalence alone. A full GLP of toxicology studies in animals and a broad spectrum of safety pharmacology has been successfully completed on the selected sugar-lipid polymer for intravenous applications. Liposeuticals has validated the bioequivalence of its formulations vs. existing marketed preparations that employ emulsion-based technology.
We have demonstrated complete solubilization of organic APIs in a single sugar-lipid-polymer system by a ratio of 1:2 (w/w) or 2% of the sugar lipid without using any co-solvent. This simplified formulation shows >90% reduction in lipid content vs. currently marketed products. The finished preparation is produced by a simple mixing procedure at ambient room temperature (25 ± 5⁰); no high energy process is required for mixing and sterilization can also be easily done using (0.2 µm) membrane filtration. Sugar-lipid-formulated product has been shown to be stable even under ambient room temperature conditions for over two years.
Our products could potentially benefit patients and healthcare practitioners in the hospital setting. The technology platform we have developed confers the following advantages:
- Less drug wastage through vial reuse and enhanced stability at room temperature
- Reduced costs via extended shelf-life
- Elimination of antibiotic resistance by removing the need for anti-microbial additives
- No need for reconstitution
- Potentially improved patient safety through the elimination of toxic excipients