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Polymers
& Polymerizable Lipids
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| Functionalized PEG Lipids |
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Purity
>99%
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Specify Chloroform or Powder for
these products
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Notes:
Phospholipids conjugated to monomethoxy polyethyleneglycol (PEG)
have been around since 1984 when Sears1 coupled,
via an amide linkage, carboxy-PEG and purified soy phosphatidylethanolamine
(PE). Since then the linkage between PEG and PE has been modified
to include esters2 and carbamate3 derivatives,
the carbamate derivative being the most widely used today. The
molecular weights of the most commonly used PEG's are 2,0004,5
and 5,0006,, but PEG's ranging from 6007
to 12,0008 are also used. The lipid part of the conjugate
varies from saturated9 or unsaturated PE's4
to cholesterol7 and ceramides10 with short
chain (C8), intermediate chain (C14) and long chain (C20) fatty
amides. |
| The use of PEG-lipid derivatives to prolong the in vivo circulation
time of liposomes and to evaluate the stearic stabilization
of the amphipathic polymer has been studied by many research
groups.2,11,12,13,14 The "holy grail" of
liposomeology continues to be a delivery vehicle for targeting
drugs to a specific biologic site. Liposome research has made
great strides toward achieving this goal by the attachment of
antibodies to functionalized PEG-lipid derivatives.15,16
The latest advance in the technology being the synthesis of
detachable PEG-lipid conjugates.17 |
| Avanti Polar Lipids, Inc. is ready and able to supply your
research and pharmaceutical PEG-lipid requirements. Our PEG-lipid
offerings are diverse, both in the PEG and the lipid part of
the conjugate. On the PEG side we offer mPEG's of various molecular
weights (PEGs
and Polymers Page) and several functionalized PEG's.
On the lipid side an infinite variety of lipid anchors from
PE's to PA's, Cardiolipin, Cholesterol or ceramides are available
or possible. Our research staff continues to develop new PEG-lipid
derivatives and other biologically compatible polymeric compounds.
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References
- Sears, B.D. (1984). Synthetic Phospholipid Compounds.
United States Patent 4,426,330
- Klibanov, A.L., K. Maruyama, V.P. Torchilin, and L. Huang.
(1990). Amphipathic polyethyleneglycols effectively prolong
the circulation time of liposomes. FEBS Lett 268:235-7.
- Woodle, M.C., G. Storm, M.S. Newman, J.J. Jekot, L.R.
Collins, F.J. Martin, and F.C. Szoka Jr. (1992). Prolonged
systemic delivery of peptide drugs by long-circulating liposomes:
illustration with vasopressin in the Brattlebororat. Pharm
Res 9:260-5.
- Ng, K., L. Zhao, Y. Liu, and M. Mahapatro. (2000). The
effects of polyethyleneglycol (PEG)-derived lipid on the
activity of target-sensitive immunoliposome. Int J Pharm
193:157-166.
- Ishida, T., D.L. Iden, and T.M. Allen. (1999). A combinatorial
approach to producing sterically stabilized (Stealth) immunoliposomal
drugs. FEBS Lett 460:129-33.
- Liu, F. and D. Liu. (1995). Long-circulating emulsions
(oil-in-water) as carriers for lipophilic drugs. Pharm
Res 12:1060-4.
- Bradley, A.J., D.V. Devine, S.M. Ansell, J. Janzen, and
D.E. Brooks. (1998). Inhibition of liposome-induced complement
activation by incorporated poly(ethylene glycol)-lipids.
Arch Biochem Biophys 357:185-94.
- Bedu-Addo, F.K., P. Tang, Y. Xu, and L. Huang. (1996).
Interaction of polyethyleneglycol-phospholipid conjugates
with cholesterol-phosphatidylcholine mixtures: sterically
stabilized liposome formulations. Pharm Res 13:718-24.
- Parr, M.J., S.M. Ansell, L.S. Choi, and P.R. Cullis. (1994).
Factors influencing the retention and chemical stability
of poly(ethylene glycol)-lipid conjugates incorporated into
large unilamellar vesicles. Biochim Biophys Acta
1195:21-30.
- Mok, K.W., A.M. Lam, and P.R. Cullis. (1999). Stabilized
plasmid-lipid particles: factors influencing plasmid entrapment
and transfection properties. Biochim Biophys Acta 1419:137-50.
- Allen, T.M., G.A. Austin, A. Chonn, L. Lin, and K.C. Lee.
(1991). Uptake of liposomes by cultured mouse bone marrow
macrophages: influence of liposome composition and size.
Biochim Biophys Acta 1061:56-64.
- Mori, A., A.L. Klibanov, V.P. Torchilin, and L. Huang.
(1991). Influence of the steric barrier activity of amphipathic
poly(ethyleneglycol) and ganglioside GM1 on the circulation
time of liposomes and on the target binding of immunoliposomes
in vivo. FEBS Lett 284:263-6.
- Woodle, M.C., L.R. Collins, E. Sponsler, N. Kossovsky,
D. Papahadjopoulos, and F.J. Martin. (1992). Sterically
stabilized liposomes. Reduction in electrophoretic mobility
but not electrostatic surface potential. Biophys J
61:902-10.
- Woodle, M.C. and D.D. Lasic. (1992). Sterically stabilized
liposomes. Biochim Biophys Acta 1113:171-99.
- Allen, T.M., E. Brandeis, C.B. Hansen, G.Y. Kao, and S.
Zalipsky. (1995). A new strategy for attachment of antibodies
to sterically stabilized liposomes resulting in efficient
targeting to cancer cells. Biochim Biophys Acta 1237:99-108.
- Bendas, G., A. Krause, U. Bakowsky, J. Vogel, and U. Rothe.
(1999). Targetability of novel immunoliposomes prepared
by a new antibody conjugation technique. Int J Pharm
181:79-93.
- Zalipsky, S., M. Qazen, J.A. Walker 2nd, N. Mullah, Y.P.
Quinn, and S.K. Huang. (1999). New detachable poly(ethylene
glycol) conjugates: cysteine-cleavable lipopolymers regenerating
natural phospholipid, diacyl phosphatidylethanolamine. Bioconjug
Chem 10:703-7.
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