Yoshihiro Takatsu has completed his Ph.D. at Hokkaido University. After working for Takeda Pharmaceutical Company Limited as a principal research scientist for 9 years, he moved to Seikagaku Corporation and has been developing ChonylationTM technology as a associate chief researcher at Glyco Research Department in Central Research Laboratory.
PEG has become the gold standard polymer extending the circularly stability of conjugated therapeutics. However, repeated administration of PEGylated proteins to animals has in some cases been associated with cellular vacuolation of macrophages, histiocytes, renal tubular cells and choroid plexus ependymal cells. In addition, immune responses to PEG itself have been recognized and have caused a loss of therapeutic efficacy. CH is the naturally-occurring biodegradable sugar chain which consists of repeated disaccharide units of D-glucuronic acid and N-acetyl-D-galactosamine. We found that i.v.-injected CH circulated surprisingly for a long period as well as PEG in mice. Consequently, we have been developing ChonylationTM technology comprising conjugation of CH to protein and peptide therapeutics. CH-conjugated asparaginase (CH-Asp) showed a good pharmacokinetic profile (T1/2 = 35.2 hours, MRT = 48.7 hours) although asparaginase (Asp) itself disappeared from the circulation within 24 hours. Similarly, ChonylationTM improved pharmacokinetics of various kinds of protein and peptide, including ovalbumin, interferon α, growth hormone, GLP-1, and insulin. To evaluate the influence of ChonylationTM to the immunogenesity of foreign protein, Asp, PEGylated Asp (Oncaspar®) and CH-Asp were repeatedly injected via the intramuscular route. Asp-treated group induced high immune responses against Asp. Oncaspar®-treated group induced immune responce to PEG but not to Asp. In contrast, CH-Asp induced no immune responces, neither to Asp nor to CH. ChonylationTM technology will be a new generation drug delivery system for protein and peptide therapeutics with significantly improved pharmacological profiles.
Shayan F. Lahiji has completed his education at Yonsei University (South Korea) with outstanding contributions to science and novel drug delivery systems. Due to his various achievements in science, Dr. Lahiji was invited to a wide range of conferences and congresses around the world to participate, present his scientific findings and share his knowledge of novel drug delivery systems with other scientists. So far he has been awarded for “the best researcher”, “the best research awards”, “the best poster presentation”, “the best academic poster” and more. Beside the high impact papers he published over the past few years in reputed journals, he has few patents related to novel drug delivery as well.
Lipophilic drugs require hazardous organic solvents for their solublization which makes it difficult to produce a non-toxic drug for pharmaceutical market. Therefore, recently there were various researches regarding solvent free systems. In this study we developed a solvent-free lipophilic drug delivery system via creating nano-sized colloidal structures and fabrication of dissolving microneedles (DMNs). DMNs are currenly bein used in various research fields such as vaccine delivery, cosmetic application and biological drug delivery. This delivery system provides advantages over topical application as well as hypodermic drug delivery systems, Here, we investigated effects of capsaicin on the mice with rheumatic arthritis by comparing DMN based solvent-free lipophilic delivery system and solvent-based system. Results showed a promising potential of our newly developed system compared with conventional systems used for solvent-free lipophilic drug delivery.