Comparison of paclitaxel penetration in normal and cancerous cervical model monolayer membranes

Preetha, A.; Huilgol, Nagraj G; Banerjee, Rinti

doi:10.1016/j.colsurfb.2006.09.005

Cited by 34 publications

(30 citation statements)

References 23 publications

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“…Indeed, the structures adopted by the parts of a membrane protein that are located in the lipid head group region are determined, in part, by hydrogen bonding to the head groups. 50 The findings about the interaction of GBP and LEV with glycerol backbone and head groups of lipids may indicate that they have the potential to change structure, relatively function, of peripheral proteins. Similarly, the localization of these drugs within hydrophobic core of bilayer may also suggest that they have the potential to change transmembrane segments of integral proteins.…”

Section: Discussionmentioning

confidence: 99%

Divergent interaction profiles of gabapentin and levetiracetam with dipalmitoylphosphatidylcholine lipids

Türker-Kaya

Kına

Alın

2017

International Journal of Epilepsy

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Background/Objectives The lipid solubility of antiepileptic drugs directly affects central nervous system availability. In relation to this, the interactions of gabapentin and levetiracetam with dipalmitoylphosphatidylcholine lipids depending on concentrations were comparatively investigated in the present study. Methods The effects of gabapentin and levetricetam as a function of concentration (1–5–10–20 mol%) on biophysical parameters of dipalmitoylphosphatidylcholine multilammelar vesicles were studied by differential scanning calorimetry and fourier transform infrared spectroscopy. Results The data revealed that gabapentin at all concentrations and levetiracetam at 1–5 mol% lowered main transition temperature, enthalpy, cooperativity, lipid fluidity, lipid order, and increased hydrogen binding capacity of glycerol and phosphate groups. However, 10–20 mol% of levetiracetam tend to show different effect on transition temperature, which could also reflect its opposing effect on lipid order and glycerol and phosphate group’s hydrations. Conclusions According to the corresponding findings depending on concentrations both drugs incorporate into phosphatidylcholines, perturbing the packing of lipids and affecting their thermotropic properties. Their binding affinity to acyl chains and hydrophilic parts of lipids was found to highly correlate with lipid-water partition and their solubility degree in water. Hence, the obtained results may offer evaluation of partition profile of the drugs into biological membranes depending on concentration.

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Section: Discussionmentioning

confidence: 99%

Divergent interaction profiles of gabapentin and levetiracetam with dipalmitoylphosphatidylcholine lipids

Türker-Kaya

Kına

Alın

2017

International Journal of Epilepsy

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“…The changes in the biophysical characteristics of the membrane, such as the lipid packing density and membrane fluidity, are known to influence the membrane’s transport properties 7, 40. The lower drug uptake seen in resistant cells than in sensitive cells (Figure 9) thus could, in part, be related to the relatively higher packing density and lower fluidity of the resistant cell membrane lipids than the sensitive cell membrane lipids.…”

Section: Discussionmentioning

confidence: 99%

Drug Resistance in Breast Cancer Cells: Biophysical Characterization of and Doxorubicin Interactions with Membrane Lipids

et al. 2010

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Understanding the role of lipids in drug transport is critical in cancer chemotherapy to overcome drug resistance. In this study, we isolated lipids from doxorubicin-sensitive (MCF-7) and -resistant (MCF-7/ADR) breast cancer cells to characterize the biophysical properties of membrane lipids (particularly lipid packing and membrane fluidity) and to understand the role of the interaction of cell membrane lipids with drug/nanocarrier on drug uptake and efficacy. Resistant cell membrane lipids showed significantly different composition and formed more condensed, less fluid monolayers than did lipids from sensitive cells. Doxorubicin, used as a model anticancer agent, showed a strong hydrophobic interaction with resistant cell membrane lipids but significantly less interaction, as well as a different pattern of interaction (i.e., ionic), with sensitive ones. The threshold intracellular doxorubicin concentration required to produce an antiproliferative effect was similar for both sensitive and resistant cell lines, suggesting that drug transport is a major barrier in determining drug efficacy in resistant cells. In addition to the biophysical characteristics of resistant cell membrane lipids, lipid-doxorubicin interactions appear to decrease intracellular drug transport via diffusion as the drug is trapped in the lipid bilayer. The rigid nature of resistant cell membranes also seems to influence endosomal functions that inhibit drug uptake when a liposomal formulation of doxorubicin is used. In conclusion, biophysical properties of resistant cell membrane lipids significantly influence drug transport, and hence drug efficacy. A better understanding of the mechanisms of cancer drug resistance is vital to developing more effective therapeutic interventions. In this regard, biophysical interaction studies with cell membrane lipids might be helpful to improve drug transport and efficacy through drug discovery and/or drug delivery approaches by overcoming the lipid barrier in resistant cells.

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“…In fact, it was observed that the incorporation of paclitaxel into the 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) bilayer induced a reduction in the cooperativity of the phase transition, which translates into the fluidizing effect that the compound exerts in the membrane [71]. Preetha et al evaluated the penetration profile of paclitaxel in monolayers of normal and cancerous cervical membranes and compared it with a DPPC monolayer [74]. It was observed that due to differences in lipid composition, which in turn affect membrane fluidity, the drug's penetration profile was different between normal and cancer membrane.…”

Section: Studies Using Dsc and Langmuir Isotherms Demonstrated That Pmentioning

confidence: 97%

Biophysics in cancer: The relevance of drug-membrane interaction studies

Alves

Ribeiro

Nunes

et al. 2016

Biochimica et Biophysica Acta (BBA) - Biomembranes

179

144

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Lipidomics has been proving that membrane lipids play a crucial role in several cell functions and are involved in several pathologies, including cancer. In fact, beyond a scaffold where proteins and other components are embedded, the cell membrane can also act as a barrier or a target for anticancer drugs. From this point of view, the development of new chemotherapeutic agents should also take into account the role of the membrane in their activity. This Review aims to highlight the importance of anticancer drug-membrane interactions as a powerful strategy to improve cancer therapy. Biophysical techniques emerge, therefore, as essential tools to unveil such interactions.

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Comparison of paclitaxel penetration in normal and cancerous cervical model monolayer membranes

Cited by 34 publications

References 23 publications

Divergent interaction profiles of gabapentin and levetiracetam with dipalmitoylphosphatidylcholine lipids

Divergent interaction profiles of gabapentin and levetiracetam with dipalmitoylphosphatidylcholine lipids

Drug Resistance in Breast Cancer Cells: Biophysical Characterization of and Doxorubicin Interactions with Membrane Lipids

Biophysics in cancer: The relevance of drug-membrane interaction studies

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