Anatolii shared his results centered on “Trehalose-Based Diblock Copolymers as Excipients for Enhancing Solubility of Poorly Water Soluble Drugs.”
From his research abstract:
Oral administration is the most preferable route of drug delivery, especially during prolonged therapy of chronic diseases. Unfortunately, many effective pharmaceuticals are poorly water-soluble, which leads to decreased bioavailability and shelf life. One of the ways to improve drug solubility and efficacy is to prepare an amorphous solid dispersion (ASD) with a polymer excipient. It is important that the polymer matrix of an ASD will stabilize the drug in the amorphous state and maintain its supersaturated concentration long enough in the dissolution media. Some of the commercial polymeric systems have shown a positive impact on drug dissolution, but most of them are difficult to characterize due to high polydispersity and system complexity. This makes it difficult to understand the structure property relationships and to quantify the effect of drug-polymer specific interactions. Also, most of the available excipients that improve dissolution of poorly water-soluble drugs tend to Hydrogen-bond to the drug while in solution, thus preventing its crystallization. Therefore, a series of block copolymers were synthesized with varied composition of H-bonding monomers including N-isopropylacrylamide, N,N-dimethylacrylamide, and 2-methacrylamidotrehalose using addition-fragmentation chain transfer (RAFT) polymerization. This family of diblock copolymers offers hydrophobic, hydrophilic, or H-bonding functionalities to serve as noncovalent sites for model drug Probucol binding. Role of each binding moiety as well as overall excipient performance was assessed using in-vitro dissolution testing.