Polyethylene glycol (PEG), a compound composed of repeated ethylene glycol units [-(CH2CH2O)n], is also known as Macrogol. https://peg.bocsci.com/

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Address: 45-16 Ramsey Road, Shirley, NY 11967, USA
Polyethylene Glycol
(PEG)
Drugs and Drug Delivery Systems

2. TABLE OF CONTENTS
What is Polyethylene Glycol (PEG)
PEG Synthesis Strategies
PEGylation Strategies
04
02
03
01
05
Quantitative Analysis Techniques for PEG
Application of PEGylation Derivatives
06 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 Small Molecule Drugs
To date, many organic small molecule drugs have gradually the PEGylation
technology, and certain progress has been made.
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 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
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.
Progress in Natural Science: Materials International. 2019, 29(6):
612-616.
Liposomes
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
Micelles are frequently the preferred
choice for anticancer drug delivery.
Preparation of PEGylated micelles
mostly utilizes PEGylated polymers or
lipids through synthetic approaches.

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
Method Analysis Content
High-Performance Liquid Chromatography (HPLC) The amount of PEG associated with colloidal carriers
Enzyme-linked Immunosorbent Assay (ELISA) The concentration of PEGylated proteins in serum samples
Colorimetric Assays The concentration and localization of PEG chains
Gas Chromatography (GC) The amount of attached PEG polymer
Mass Spectrometry (MS) The molecular mass of PEGylated species
Liquid Chromatography Mass Spectrometry (LC-MS) The molecular mass of PEGylated species
Matrix-Assisted Laser Desorption Ionization Mass Spectrometry
(MALDI–MS)
The average molecular weight of PEGylated species and degree of PEGylation
Electrospray Ionization Mass Spectrometry (ESI-MS) The average molecular weight of PEGylated species and degree of PEGylation
X-Ray Photoelectron Spectroscopy (XPS)
Changes in elemental composition on the conjugate surface before and after PEGylation
PEGylation
Raman Spectroscopy Determination of PEG content and conformation
Thermogravimetric Analysis (TGA) The content of PEG
Inductively Coupled Plasma Mass Spectrometry (ICP-MS)
The quantitative measurement of metal-containing PEGylated pharmaceuticals or
nanoparticles

10. Application of PEGylation Derivatives
Drug Delivery
Imaging
Diagnosis
Tissue
Engineering
Drug
Preparation
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
Example of PEG Conjugates of Low Molecular
Weight Anticancer Drugs

11. Marketed PEGylated Products
Brand Name Company Indication Comment
Adagen Enzon Severe combined immunodeficiency disease (SCID) PEGylated adenosine deaminase
Cimzia Nektar/UCB Pharma
Rheumatoid arthritis and Crohn's disease
PEGylated Fab' fragment of a humanized TNF
inhibitor monoclonal antibody
Doxil/Caelyx Ortho Biotech/ Schering-Plough Cancer PEGylated liposome of doxorubicin
Macugen Pfizer
Neovascular age-related macular degeneration
Pegylated anti-vascular endothelial growth factor
(VEGF) aptamer
Mircera Roche Anemia associated with chronic kidney disease PEGylated erythropoetin
Neulasta Amgen
Chemotherapy-induced neutropenia
PEGylated recombinant methionyl human
granulocyte colony-stimulating factor
Omontys Affymax/Takeda Pharmaceuticals
Anemia associated with chronic kidney disease
PEGylated synthetic peptide analog of
erythropoietin
Oncaspar Enzon Acute lymphoblastic leukemia PEGylated L-asparaginase
PEGASYS Hoffmann-La Roche Hepatitis B and hepatitis C PEGylated interferon alpha
Pegintron Schering-Plough/Enzon Hepatitis B and hepatitis C PEGylated interferon alpha
Pegloticase Savient Gout PEGylated uricase
Somavert Pfizer
Acromegaly
PEGylated human growth hormone mutein
antagonist

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