Drug delivery by phospholipase A2 degradable liposomes

Jesper Davidsen; Charlotte Vermehren; Sven Frokjaer; Ole G. Mouritsen; Kent Jørgensen

doi:10.1016/S0378-5173(00)00634-7

Drug delivery by phospholipase A₂ degradable liposomes

Jesper Davidsen, Charlotte Vermehren, Sven Frokjaer, Ole G. Mouritsen, Kent Jørgensen^*

^*Corresponding author for this work

Social and Clinical Pharmacy

39 Citations (Scopus)

Abstract

The effect of poly(ethylene glycol)-phospholipid (PE-PEG) lipopolymers on phospholipase A₂ (PLA₂) hydrolysis of liposomes composed of stearoyl-oleoylphosphatidylcholine (SOPC) was investigated. The PLA₂ lag-time, which is inversely related to the enzymatic activity, was determined by fluorescence, and the zeta-potentials of the liposomes were measured as a function of PE-PEG lipopolymer concentration. A significant decrease in the lag-time, and hence an increase in enzymatic activity, was observed with increasing amounts of the negatively charged PE-PEG lipopolymers incorporated into the SOPC liposomes. The enhancement of the PLA₂ enzymatic activity might involve a stronger PLA₂ binding affinity towards the negatively charged and polymer covered PEG liposomes.

Original language	English
Journal	International Journal of Pharmaceutics
Volume	214
Issue number	1-2
Pages (from-to)	67-69
Number of pages	3
ISSN	0378-5173
DOIs	https://doi.org/10.1016/S0378-5173(00)00634-7
Publication status	Published - 19 Feb 2001

Keywords

Degradation
Drug-delivery
Lipopolymer
Liposomes
PEG liposomes
Phospholipase A

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10.1016/S0378-5173(00)00634-7

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title = "Drug delivery by phospholipase A2 degradable liposomes",

abstract = "The effect of poly(ethylene glycol)-phospholipid (PE-PEG) lipopolymers on phospholipase A2 (PLA2) hydrolysis of liposomes composed of stearoyl-oleoylphosphatidylcholine (SOPC) was investigated. The PLA2 lag-time, which is inversely related to the enzymatic activity, was determined by fluorescence, and the zeta-potentials of the liposomes were measured as a function of PE-PEG lipopolymer concentration. A significant decrease in the lag-time, and hence an increase in enzymatic activity, was observed with increasing amounts of the negatively charged PE-PEG lipopolymers incorporated into the SOPC liposomes. The enhancement of the PLA2 enzymatic activity might involve a stronger PLA2 binding affinity towards the negatively charged and polymer covered PEG liposomes.",

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AU - Davidsen, Jesper

AU - Vermehren, Charlotte

AU - Frokjaer, Sven

AU - Mouritsen, Ole G.

AU - Jørgensen, Kent

PY - 2001/2/19

Y1 - 2001/2/19

N2 - The effect of poly(ethylene glycol)-phospholipid (PE-PEG) lipopolymers on phospholipase A2 (PLA2) hydrolysis of liposomes composed of stearoyl-oleoylphosphatidylcholine (SOPC) was investigated. The PLA2 lag-time, which is inversely related to the enzymatic activity, was determined by fluorescence, and the zeta-potentials of the liposomes were measured as a function of PE-PEG lipopolymer concentration. A significant decrease in the lag-time, and hence an increase in enzymatic activity, was observed with increasing amounts of the negatively charged PE-PEG lipopolymers incorporated into the SOPC liposomes. The enhancement of the PLA2 enzymatic activity might involve a stronger PLA2 binding affinity towards the negatively charged and polymer covered PEG liposomes.

AB - The effect of poly(ethylene glycol)-phospholipid (PE-PEG) lipopolymers on phospholipase A2 (PLA2) hydrolysis of liposomes composed of stearoyl-oleoylphosphatidylcholine (SOPC) was investigated. The PLA2 lag-time, which is inversely related to the enzymatic activity, was determined by fluorescence, and the zeta-potentials of the liposomes were measured as a function of PE-PEG lipopolymer concentration. A significant decrease in the lag-time, and hence an increase in enzymatic activity, was observed with increasing amounts of the negatively charged PE-PEG lipopolymers incorporated into the SOPC liposomes. The enhancement of the PLA2 enzymatic activity might involve a stronger PLA2 binding affinity towards the negatively charged and polymer covered PEG liposomes.

KW - Degradation

KW - Drug-delivery

KW - Lipopolymer

KW - Liposomes

KW - PEG liposomes

KW - Phospholipase A

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Drug delivery by phospholipase A₂ degradable liposomes

Abstract

Keywords

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