The importance of developing drug delivery systems
A Drug Delivery System (DDS) is designed to precisely control the distribution of drugs within the body to achieve optimal therapeutic effects. However, traditional drug delivery systems face challenges such as limited precision, significant side effects, low patient compliance, and discomfort during treatment. To address these issues, modern drug delivery technology aims to enhance accuracy, thereby improving efficacy, reducing dosage, and minimizing side effects.
A breakthrough in transdermal large molecule drug delivery technology
Professor Simon Li, a distinguished expert in drug delivery, is a professor of Nanomedicine and Chemical Biology at the University of British Columbia (UBC) Faculty of Pharmaceutical Sciences, a global leader in drug delivery research. He directs UBC’s Targeted Drug Delivery and Nanomedicine Laboratory, specializing in large molecule drugs and nucleic acid delivery systems. Having served as chair of the Targeted Drug Delivery and Prodrug Focus Group of the American Association of Pharmaceutical Scientists (AAPS), Professor Li has received numerous academic accolades. His research focuses on developing innovative, safe, and effective therapies using advanced engineering techniques, with the goal of transforming healthcare and enhancing patient outcomes.
As the demand for large molecule drugs—such as peptides, proteins, gene therapies, and nucleic acid-based vaccines—increases, injections remain a common delivery method. These drugs often encounter challenges when taken orally, including degradation by stomach acid, poor membrane permeability, and low stability in the body. While injections are effective, they may not always be convenient, particularly for individuals suffering from needle phobia (trypanophobia). Furthermore, the disposal of needle waste has become a growing concern in light of today’s focus on Environmental, Social, and Governance (ESG) principles.
Professor Li emphasizes that converting injectable drugs into oral formulations has become a pivotal trend in drug delivery. However, oral administration of large molecule drugs faces the challenge of the “First-Pass Effect,” where drugs are metabolized by the liver after gastrointestinal absorption, significantly reducing their efficacy. Consequently, oral formulations often require much higher dosages. For example, Novo Nordisk’s oral glucagon-like peptide-1 receptor agonist (GLP-1 RA) Semaglutide, marketed as Rybelsus, has a bioavailability of less than 1% when taken orally and necessitates nearly a month of continuous use to be effective. High doses also increase the risk of side effects, such as nausea and severe diarrhea.
To overcome these challenges, Professor Li’s lab is developing an “orally dissolving” formulation that employs innovative “large molecule transmembrane delivery technology.” This approach utilizes specialized peptides that bind to the oral mucosa and underlying cells, gently “opening” the intercellular gaps within the mucosal layers. Once the large molecule drugs traverse these gaps, they quickly close, allowing the drugs to efficiently cross the mucosal barrier and enter the bloodstream, thereby bypassing the digestive system and avoiding the First-Pass Effect. Additionally, the rapid absorption of the drugs in the mouth minimizes their entry into the digestive tract, significantly enhancing their efficacy. Compared to traditional oral formulations, this technology may reduce required dosages, offering potential cost benefits and improved market competitiveness.
Reference : https://news.gbimonthly.com/tw/magazine/article_show.php?num=69620&page=47
