Poor water solubility is one of the major hurdles drug candidates must clear to advance into clinical applications. Lipid-based formulations such as liposomes, emulsion, and micelles have excellent safety profiles and are an attractive choices for water-insoluble drugs; however, these formulations are best suited for either hydrophilic or hydrophobic drugs and are not useful for drugs that are only moderately hydrophobic or hydrophilic. Inadequate mixing of moderately-hydrophobic agents with highly lipophilic carriers leads to low drug loading capacity and formulation instability, as the drugs slowly disassociate from the emulsion particles. Drugs with moderate hydrophobicity or hydrophilicity also have leakage problems in liposome formulations. Compounding this problem, drug and carrier formulations are assembled via a trial-and-error technique, which is inefficient and potentially misses designs that accommodate compounds with moderate hydrophobicity or hydrophilicity. A new strategy for drug formulation as well as a new structure for these unique compounds is necessary for better drug delivery and formulation reliability, as well as lower costs and more timely results.
Description
Presented is a new mechanistic approach to the development of novel drug carrier systems. Rather than relying on off-the-shelf surfactants and oils for creating lipid-based formulations, a bottom-up approach is undertaken, beginning by selecting a simple structural element capable of interacting with the active ingredient. This drug-interactive segment is then assembled between hydrophobic lipid chains and a PEG or other hydrophilic groups. The drug-interactive segment is thus positioned at the interfacial region, permitting drugs that are only moderately hydrophobic to be incorporated in a less stringent environment. This design principle can be extended to other drugs for both lipid-based and polymer-based systems for improved in vivo drug delivery, especially for those for which the traditional assembly method has failed in the past.
Applications
· Creation of safe and effective drug delivery formulations for drugs that are moderately hydrophobic or hydrophilic
Advantages
· Availability to safely and reliably delivery moderately hydrophobic or hydrophilic drugs
· Assembly is quicker and costs significantly less than trial-and-error methods
Invention Readiness
In vivo
IP Status
https://patents.google.com/patent/US20190038556A1
