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PEG-Derivatized FTS as A Simple, Effective, and Dual-Functional Drug Delivery Platform for Hydrophobic Agents

详细技术说明

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*Abstract

DescriptionThe Innovators developed a novel drug formulation system based on PEGylated S-trans, trans-farnesylthiosalicylic acid (FTS). PEGylation improves the drug's solubility while FTS is a synthetic farnesylcysteine mimetic anti-tumor agent. Data demonstrate that PEG-FTS conjugates form small-sized micelles (20-30 nm) that effectively deliver anti-cancer agents.BackgroundThe current drug discovery process is costly and inefficient. Clinical application of paclitaxel (PTX) in cancer therapy is limited by problems such as low water solubility, lack of tissue-specificity,and high toxicity. Current formulations are inadequate with respect to drug loading capacity, stability and toxicity. In addition, most drug delivery systems utilize "inert" excipients that lacktherapeutic effect.Applications1. Appropriate for both lipidic and polymeric systems2. Dual-functional drug delivery platform for hydrophobic agentsAdvantages1. Significantly improved drug loading capacity and formulation stability2. The system has excellent safety profile and shows excellent efficacy in delivering various types of anticancer agents with significantly improved therapeutic outcome3. Broadly applicable in formulating various types of therapeutic agents of diverse structureDevelopment StageIn vivo dataNon-provisional Patent Application FiledPublications1. Zhang X, Lu J, Huang Y, Zhao W, Chen Y, Li J, Gao X, Venkataramanan R, Sun M, Stolz DB, Zhang L, Li S. PEG-farnesylthiosalicylate conjugate as a nanomicellar carrier for delivery of paclitaxel. Bioconjug Chem. 2013 Mar 20;24(3):464-72.doi: 10.1021/bc300608h. Epub 2013 Mar 1. PubMed PMID: 23425093; PubMed Central PMCID: PMC3623935.

*Principal Investigation

Name: Xiang Gao

Department: Pharm-Pharmaceutical Science

Name: Yixian Huang, Postdoctoral Research Associate

Department: Pharm-Pharmaceutical Science

Name: Song Li, Associate Professor

Department: Pharm-Pharmaceutical Science

Name: Xiaolan Zhang

Department: Pharm-Pharmaceutical Science

国家/地区

美国