After more than 20 years of endeavors, we have successfully developed a world-leading polysaccharide-based new drug discovery system and drug delivery platform called GlycoTDSTM, characterized by our technologies' unique properties. In this platform, several cutting-edge drug candidates have entered into different development phases, including the first-in-class (FIC)of new and improved drug candidates.

Polysaccharides are biomaterials containing repeating sugar units and have been widely used in drug delivery systems. Polysaccharides are biocompatible, non-immunogenic, biodegradable, and non-toxic. These properties make them attractive for use in drug formulations.

GlycoTDSTM is an innovatively proprietary and programable platform and allows the designed polysaccharide-based conjugates to modulate their pharmacokinetics (PK) and improve drug targeting, drug availability, tumor delivery, and tumor loading, while dramatically reducing side effects associated with cancer drugs.

Targeted Supra-molecular Polymer Drug Conjugates

Targeted drug delivery is a crucial aspect of modern medicine, as it allows for more efficient and effective transport of drugs to specific areas of the body. With targeted drugs, a higher concentration of drugs can be delivered to targeted tissues, organs, and cells, which can increase the effectiveness of the treatment while minimizing the risk of systemic toxicity.

Targeted supra-molecular polymer-drug conjugates are a specific type of drug delivery system that utilizes covalent coupling of drugs to polymers with large molecular weights, typically ranging from tens of thousands to several million. These supra-molecular polymers, also known as polymer-drug carriers, can improve the pharmacokinetic properties of the conjugated drugs, control their release, and enable them to reach the target organs.

Moreover, the targeted supra-molecular polymer-drug conjugates take advantage of the permeation and retention effect, also known as the EPR effect, which enables them to passively target tumors. This effect occurs due to the unique properties of tumor blood vessels, which are leaky and lack proper lymphatic drainage, allowing for the accumulation of the polymer-drug conjugates within the tumors.

Targeted drug delivery based on polysaccharides as carriers via macropinocytosis

Polysaccharides are complex carbohydrates that play important roles in various biological processes. Some polysaccharides such as dextran, ficoll, etc.. have been found to exhibit active tumor-targeting ability via macropinocytosis.

Macropinocytosis is a cellular process by which cells engulf large volumes of extracellular fluid and its contents, including nutrients, growth factors, and pathogens. It plays important roles in various physiological and pathological processes, such as immune surveillance, antigen presentation, and cancer progression.

Currently, macropinocytosis is an exciting new therapeutic target that holds great promise for developing targeted therapeutics. By targeting macropinocytosis, researchers can achieve two goals. Firstly, they can use it as a new mechanism to suppress tumor growth. By identifying oncogene proteins related to the macropinocytosis pathway, such as mutant RAS (HRAS, KRAS, NRAS), Rac1, NRF2, galectin-3, deficient PTEN, and deficient P53, etc. some innovative therapeutic approaches for cancer treatment have been developed and exhibited significant advantages over existing therapies. Secondly, macropinocytosis can be manipulated to deliver drugs to tumor sites with greater precision and efficiency. Such an approach offers new opportunities for targeted drug delivery that can potentially minimize side effects and dramatically improve the efficacy of cancer treatments.

Recent literature, including Nature (2019: 568, 410-414), Cancer Cell (2021:39, 68-693), Cancer Discovery (2021:11, 1808-25), Nature Communications (2020:11, 1121), and Theranostics (2022:12(3), 1061-1073), highlights the potential of targeting macropinocytosis in cancer therapy. These studies demonstrated that inhibiting macropinocytosis can reduce tumor growth and sensitize cancer cells to chemotherapy and immunotherapy. 

Polysaccharide-based biomaterials used for the encapsulation of drugs

Polysaccharide-based biomaterials, such as dextran, cyclodextrin, chitosan, alginate, and hyaluronic acid, offer several advantages for encapsulated drug formulations. They can be modified to control the release rate of drugs. These properties make them attractive biomaterials for encapsulated drug nano-formulations.