Chapter title |
Long-Circulating, pH-Sensitive Liposomes
|
---|---|
Chapter number | 16 |
Book title |
Liposomes
|
Published in |
Methods in molecular biology, January 2017
|
DOI | 10.1007/978-1-4939-6591-5_16 |
Pubmed ID | |
Book ISBNs |
978-1-4939-6589-2, 978-1-4939-6591-5
|
Authors |
Denitsa Momekova, Stanislav Rangelov, Nikolay Lambov, Momekova, Denitsa, Rangelov, Stanislav, Lambov, Nikolay |
Abstract |
A major limiting factor for the wide application of pH-sensitive liposomes is their recognition and sequestration by the phagocytes of the reticuloendothelial system, which conditions a very short circulation half-life. Typically prolonged circulation of liposomes is achieved by grafting their membranes with pegylated phospholipids (PEG-lipids), which have been shown, however, to deteriorate membrane integrity on one hand and to hamper the pH-responsiveness on the other. Hence, the need for novel alternative surface modifying agents to ensure effective half-life prolongation of pH-sensitive liposomes is a subject of intensive research. A series of copolymers having short blocks of lipid-mimetic units has been shown to sterically stabilize conventional liposomes based on different phospholipids. This has prompted us to broaden their utilization to pH-sensitive liposomes, too. The present contribution gives a thorough account on the chemical synthesis of these copolymers their incorporation in DOPE:CHEMs pH-sensitive liposomes and detailed explanation on the battery of techniques for the biopharmaceutical characterization of the prepared formulations in terms of pH-responsiveness, cellular internalization, in vivo pharmacokinetics and biodistribution. |
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Unknown | 2 | 17% |
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