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PEG for Drugs and Drug Delivery Systems

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PEG for Drugs and Drug Delivery Systems

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  1. Polyethylene Glycol (PEG) Drugs and Drug Delivery Systems Tel: 1-631-504-6093 Email: info@bocsci.com Address: 45-16 Ramsey Road, Shirley, NY 11967, USA

  2. What is Polyethylene Glycol (PEG) TABLE OF CONTENTS 04 02 03 01 05 06 PEG Synthesis Strategies PEGylation Strategies Quantitative Analysis Techniques for PEG Application of PEGylation Derivatives Marketed PEGylated Products

  3. What is Polyethylene Glycol (PEG) ? • Definition • Polyethylene glycol (PEG), a compound composed of repeated ethylene glycol units [-(CH2CH2O)n], is also known as Macrogol. • Characteristics • High structure flexibility • Biocompatibility • Amphiphilicity • Good moisture retention • Excellent lubricity Introduction of Polyethylene Glycol

  4. PEG Synthesis Strategies

  5. PEGylation Strategies PEGylation of Peptides and Proteins The activated PEG achieves coupling through chemical reactions with the amino acid residues on the peptide or protein molecules. PEGylation of Small Molecule Drugs To date, many organic small molecule drugs have gradually the PEGylation technology, and certain progress has been made. PEGylation of Nanocarriers Due to differences in the chemical make-up, strategies used for PEGylation of nanocarriers can be broadly classified as polymeric nanoparticles, liposomes, micelles, and inorganic nanoparticles.

  6. PEGylation of Peptides and Proteins • PEGylation of Peptide and Protein Strategies • Site-selective PEGylation • Enzymatic PEGylation • Releasable and non-covalent PEGylation Journal of Controlled Release.2014, 192:67–81.

  7. PEGylation of Nanocarriers Due to differences in the chemical make-up, strategies used for PEGylation of nanocarriers can be broadly classified as polymeric nanoparticles, liposomes, micelles, and inorganic nanoparticles. Polymeric nanoparticles and inorganic nanoparticles are promising tools for controlled drug delivery or imaging in cancer therapy and many other applications. Nanoparticles Micelles Liposomes Nanoparticles reserved various advantages for drug delivery, such as controlled release and targeting. The introduction of PEG will not only affect the biodegradation behavior of nanoparticles but also the release and distribution of drugs in the body. Liposome is an ideal drug delivery carrier due to its targeted properties, longer blood retention time, and higher organ distribution selectivity, which can improve the efficacy of drugs and reduce toxic side effects. Micelles are frequently the preferred choice for anticancer drug delivery. Preparation of PEGylated micelles mostly utilizes PEGylated polymers or lipids through synthetic approaches. Progress in Natural Science: Materials International. 2019, 29(6): 612-616.

  8. PEGylation of Small Molecule Drugs • Branched PEG • The Umbrella-like structure provides more binding sites and a larger molecular volume. • Forked PEG  • Multiple proximal reactive groups are provided at one or both ends of the linear PEG chain to enhance the drug loading of PEG. • Multi-armed PEG • The star-like structure of multi-armed PEG and multiple hydroxyl groups greatly advance active sites for drug conjugation. Progress in Polymer Science. 2013, 38: 421–444.

  9. Quantification Analytical Techniques for PEG

  10. Application of PEGylation Derivatives Example of PEG Conjugates of Low Molecular Weight Anticancer Drugs • Most of the PEG conjugates of low molecular weight drugs that have entered clinical trials are of the camptothecin family, namely camptothecin itself, SN38 and irinotecan. • PEG-Camptothecin • PEG-SN38 • PEG-Irinotecan • PEG-Docetaxel • PEG-Paclitaxel Tissue Engineering Drug Preparation Imaging Diagnosis Drug Delivery

  11. Marketed PEGylated Products

  12. Tel: 1-631-504-6093 Email: info@bocsci.com Address: 45-16 Ramsey Road, Shirley, NY 11967, USA

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