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Effect of Fluidizing Agents on Paclitaxel Penetration in Cervical Cancerous Monolayer Membranes

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Abstract

The aim of this study was to compare modulation of paclitaxel penetration in cancerous and normal cervical monolayers by four fluidizing agents: PCPG (9:1 DPPC:PG), PCPE (9:1 DPPC:DOPE), ALEC (7:3 DPPC:PG) and Exosurf (13.5:1.5:1.0 DPPC:hexadecanol:tyloxapol). Presence of the fluidizing agents improved drug penetration significantly. PCPG and PCPE were promising penetration enhancers. PCPG 0.1% caused 3.8– and 1.7-fold higher maximum increments in surface pressure due to drug penetration, (Δπ)max, than the control in cancerous and normal monolayers, respectively, at 20 mN/m. In cancerous monolayer at 20 mN/m, presence of 0.1%, 0.5%, 1%, 5% and 10% PCPE produced 3.4-, 5.7-, 7.4-, 9.6- and 9.8-fold higher drug penetration compared to the control monolayer without PCPE, respectively. In cancerous monolayer at 20 mN/m, PCPG and PCPE liposomes having 1 mg lipid gave 2.1 and 3.6 times higher (Δπ)max compared to the control, respectively. Further, the liposomal drug penetration was found to be directly proportional to the liposomal lipid content. The effect of the fluidizing agents was confirmed by increased calcein release from model cervical cancer liposomes. These results may have implications in using the above biocompatible lipids and surfactants as penetration enhancers along with anticancer drugs or as carriers for liposomal formulations of anticancer drugs for improved membrane penetration.

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Acknowledgements

This work was partly funded by the All India Council for Technical Education in the form of a Career Award for Young Teachers to R. B.

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Authors and Affiliations

  1. School of Biosciences and Bioengineering, Indian Institute of Technology, Mumbai, 400076, India

    A. Preetha & R. Banerjee

  2. Division of Radiation Oncology, Nanavati Hospital, Mumbai, 400 056, India

    N. Huilgol

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  1. A. Preetha
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  2. N. Huilgol
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  3. R. Banerjee
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Correspondence to R. Banerjee.

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Preetha, A., Huilgol, N. & Banerjee, R. Effect of Fluidizing Agents on Paclitaxel Penetration in Cervical Cancerous Monolayer Membranes. J Membrane Biol 219, 83–91 (2007). https://doi.org/10.1007/s00232-007-9064-6

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  • DOI: https://doi.org/10.1007/s00232-007-9064-6

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