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Binding of paclitaxel to lipid interfaces: Correlations with interface compliance

Publication ,  Journal Article
Needham, D; Sarpal, RS
Published in: Journal of Liposome Research
January 1, 1998

In the present work, we have studied the paclitaxel loading efficiency of lipid bilayers with respect to their compositional behavior, which in turn determines their mechanical properties. We have found that, if a drug with a low water solubility like paclitaxel (or at least a part of this molecule) associates with lipid bilayers, then binding is enhanced if the interface was soft, i.e., highly expandable (low elastic area modulus and tensile strength). We have systematically varied the surface softness of stearoyl oleoyl phosphatidylcholine (SOPC) bilayers by incorporating the lysolipid, monooleoyl phosphatidylcholine (MOPC) to create maximum softness and 50 mol% cholesterol (CHOL) to create less soft, and more stiff membranes, respectively. It was observed that the least soft SOPC bilayers (high elastic area modulus and tensile strength) composed of 50 mol% CHOL, load a negligible amount of paclitaxel (~5μM) in comparison to soft SOPC bilayers made by the incorporation of 28 mol% MOPC, which load 2 mM paclitaxel (12 mol% paclitaxel with respect to total lipid). The paclitaxel loading can be increased to almost 20 mol% for the ultimate in 'soft' interfaces, the lysolipid.

Duke Scholars

Published In

Journal of Liposome Research

DOI

ISSN

0898-2104

Publication Date

January 1, 1998

Volume

8

Issue

2

Start / End Page

147 / 163

Related Subject Headings

  • Pharmacology & Pharmacy
  • 3214 Pharmacology and pharmaceutical sciences
  • 1115 Pharmacology and Pharmaceutical Sciences
 

Citation

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Needham, D., & Sarpal, R. S. (1998). Binding of paclitaxel to lipid interfaces: Correlations with interface compliance. Journal of Liposome Research, 8(2), 147–163. https://doi.org/10.3109/08982109809035523
Needham, D., and R. S. Sarpal. “Binding of paclitaxel to lipid interfaces: Correlations with interface compliance.” Journal of Liposome Research 8, no. 2 (January 1, 1998): 147–63. https://doi.org/10.3109/08982109809035523.
Needham D, Sarpal RS. Binding of paclitaxel to lipid interfaces: Correlations with interface compliance. Journal of Liposome Research. 1998 Jan 1;8(2):147–63.
Needham, D., and R. S. Sarpal. “Binding of paclitaxel to lipid interfaces: Correlations with interface compliance.” Journal of Liposome Research, vol. 8, no. 2, Jan. 1998, pp. 147–63. Scopus, doi:10.3109/08982109809035523.
Needham D, Sarpal RS. Binding of paclitaxel to lipid interfaces: Correlations with interface compliance. Journal of Liposome Research. 1998 Jan 1;8(2):147–163.
Journal cover image

Published In

Journal of Liposome Research

DOI

ISSN

0898-2104

Publication Date

January 1, 1998

Volume

8

Issue

2

Start / End Page

147 / 163

Related Subject Headings

  • Pharmacology & Pharmacy
  • 3214 Pharmacology and pharmaceutical sciences
  • 1115 Pharmacology and Pharmaceutical Sciences