Absorption of polyethylene glycol (PEG) polymers: The effect of PEG size on permeability

Journal of Pharmaceutical Sciences

Volumn 98, Issue 8, 2009, Pages 2847-2856

  Gursahani, Hema ^a   Riggs Sauthier, Jennifer ^a   Pfeiffer, Juergen ^a   Lechuga Ballesteros, David ^a,b   Fishburn, C Simone ^a  

^a NEKTAR THERAPEUTICS   (United States)

^b Aridis Pharmaceuticals   (United States)

Author keywords

Absorption; Delivery permeability; Diffusion transport; Epithelial; Passive; Pegylation; Permeability; Pharamcokinetics; Polymers

Indexed keywords

FLUORESCEIN ISOTHIOCYANATE; MACROGOL;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BLOOD LEVEL; CELL FRACTIONATION; CONTROLLED STUDY; DRUG HALF LIFE; DRUG UPTAKE; IN VIVO CULTURE; LUNG; LUNG ALVEOLUS MACROPHAGE; LUNG LAVAGE; MALE; MOLECULAR SIZE; NONHUMAN; PERMEABILITY; RAT; SUPERNATANT;

EID: 68249109077     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.21635     Document Type: Article

References (26)

1. Fishburn CS. 2008. The pharmacology of PEGylation: Balancing PD with PK to generate novel therapeutics. J Pharm Sci 97:4167-4183.
2. Harris JM, Chess RB. 2003. Effect of pegylation on pharmaceuticals. Nat Rev Drug Discov 2:214-221.
3. Roberts MJ, Bentley MD, Harris JM. 2002. Chemistry for peptide and protein PEGylation. Adv Drug Deliv Rev 54:459-476.
4. He YL, Murby S, Warhurst G, Gifford L, Walker D, Ayrton J, Eastmond R, Rowland M. 1998. Species differences in size discrimination in the paracellular pathway reflected by oral bioavailability of poly(ethylene glycol) and D-peptides. J Pharm Sci 87:626-633. (Pubitemid 28225629)
5. Donovan MD, Flynn GL, Amidon GL. 1990. Absorption of polyethylene glycols 600 through 2000: The molecular weight dependence of gastrointestinal and nasal absorption. Pharm Res 7:863-868.
6. Tronde A, Norden B, Marchner H, Wendel AK, Lennernas H, Bengtsson UH. 2003. Pulmonary absorption rate and bioavailability of drugs in vivo in rats: Structure-absorption relationships and physicochemical profiling of inhaled drugs. J Pharm Sci 92:1216-1233. (Pubitemid 36676468)
7. Patton JS, Fishburn CS, Weers JG. 2004. The lungs as a portal of entry for systemic drug delivery. Proc Am Thorac Soc 1:338-344.
8. Matsukawa Y, Lee VH, Crandall ED, Kim KJ. 1997. Size-dependent dextran transport across rat alveolar epithelial cell monolayers. J Pharm Sci 86:305-309. (Pubitemid 27113763)
9. Niven RW, Rypacek F, Byron PR. 1990. Solute absorption from the airways of the isolated rat lung. III. Absorption of several peptidase-resistant, synthetic polypeptides: Poly-(2-hydroxyethyl)-aspartamides. Pharm Res 7:990-994.
10. Patton JS, Bukar J, Nagarajan S. 1999. Inhaled insulin. Adv Drug Deliv Rev 35:235-247.
11. Niven RW, Lott FD, Cribbs JM. 1993. Pulmonary absorption of recombinant methionyl human granulocyte colony stimulating factor (r-huG-CSF) after intratracheal instillation to the hamster. Pharm Res 10:1604-1610.
12. Shin BS, Jung JH, Lee KC, Yoo SD. 2004. Nasal absorption and pharmacokinetic disposition of salmon calcitonin modified with low molecular weight polyethylene glycol. Chem Pharm Bull (Tokyo) 52: 957-960.
13. Adis International Limited. 2004. Insulin inhalation- Pfizer/Nektar Therapeutics: HMR 4006, inhaled PEG-Insulin-Nektar, PEGylated insulin- Nektar. Drugs R&D 5:166-170.
14. Lee KC, Park MO, Na DH, Youn YS, Lee SD, Yoo SD, Lee HS, DeLuca PP. 2003. Intranasal delivery of PEGylated salmon calcitonins: Hypocalcemic effects in rats. Calcif Tissue Int 73:545-549.
15. Niven RW, Whitcomb KL, Shaner L, Ralph LD, Habberfield AD, Wilson JV. 1994. Pulmonary absorption of polyethylene glycolated recombinant human granulocyte-colony stimulating factor (PEG-rhG-CSF). J Control Release 32:177-189.
16. Fishburn CS, Lechuga-Ballesteros D, Viegas T, Kuo M-C, Song Y, Gursahani H, Leach C. 2006. Chemically modified small molecules. US patent application 11/344,404. 2006-08-17.
17. Schanker LS, Less MJ. 1977. Lung pH and pulmonary absorption of nonvolatile drugs in the rat. Drug Metab Dispos 5:174-178. (Pubitemid 8321949)
18. Pauluhn J. 2000. Inhalation toxicity of 1,6-hexamethylene diisocyanate homopolymer (HDI-IC) aerosol: Results of single inhalation exposure studies. Toxicol Sci 58:173-181. (Pubitemid 30815890)
19. Feldman BF, Zinkl JG, Jain NC. 2000. Schalm's veterinary hematology. 5th edition. Baltimore, MD: Lippincott Williams & Wilkins.
20. Dorger M, Munzing S, Allmeling AM, Messmer K, Krombach F. 2001. Phenotypic and functional differences between rat alveolar, pleural, and peritoneal macrophages. Exp Lung Res 27:65-76. (Pubitemid 32063051)
21. Murray MJ, Driscoll KE. 1992. Immunology of the respiratory system. In: Parent RA, editor. Comparative biology of the normal lung. Boca Raton, FL: CRC Press. pp. 725-741.
22. Davies B, Morris T. 1993. Physiological parameters in laboratory animals and humans. Pharm Res 10:1093-1095. (Pubitemid 23211439)
23. Yamaoka T, Tabata Y, Ikada Y. 1994. Distribution and tissue uptake of poly(ethylene glycol) with different molecular weights after intravenous administration to mice. J Pharm Sci 83:601-606. (Pubitemid 24222392)
24. Wolff RK. 1992. Mucociliary function. In: Parent RA, editor. Comparative biology of the normal lung. Boca Raton, FL: CRC Press. pp. 659-680.
25. Laverman P, Brouwers AH, Dams ET, Oyen WJ, Storm G, van Rooijen N, Corstens FH, Boerman OC. 2000. Preclinical and clinical evidence for disappearance of long-circulating characteristics of polyethylene glycol liposomes at low lipid dose. J Pharmacol Exp Ther 293:996-1001. (Pubitemid 30417869)
26. Patton JS, Byron PR. 2007. Inhaling medicines: Delivering drugs to the body through the lungs. Nat Rev Drug Discov 6:67-74.