P-glycoprotein (P-gp/MDR1)/ABCB1

Lai, Yurong

doi:10.1533/9781908818287.147

Cited by 4 publications

(1 citation statement)

References 323 publications

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“…P-gp is extensively present at physiological barriers such as the blood–brain barrier, placental barrier, and intestinal barrier (Y. Lai, 2013 ). Inhibition of the P-gp transporters in these physiological barriers may disrupt normal physiology and affect the pharmacokinetics of various drugs; hence, targeted anti-P-gp therapy in cancer cells is important to circumvent the adverse effects ( Guo et al., 2017 ).…”

Section: The Menace Of P-gp Facilitated Mdr In Breast Cancermentioning

confidence: 99%

Exploring new Horizons in overcoming P-glycoprotein-mediated multidrug-resistant breast cancer via nanoscale drug delivery platforms

Famta

Shah

Chatterjee

et al. 2021

Current Research in Pharmacology and Drug Discovery

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The high probability (13%) of women developing breast cancer in their lifetimes in America is exacerbated by the emergence of multidrug resistance after exposure to first-line chemotherapeutic agents. Permeation glycoprotein (P-gp)-mediated drug efflux is widely recognized as the major driver of this resistance. Initial in vitro and in vivo investigations of the co-delivery of chemotherapeutic agents and P-gp inhibitors have yielded satisfactory results; however, these results have not translated to clinical settings. The systemic delivery of multiple agents causes adverse effects and drug–drug interactions, and diminishes patient compliance. Nanocarrier-based site-specific delivery has recently gained substantial attention among researchers for its promise in circumventing the pitfalls associated with conventional therapy. In this review article, we focus on nanocarrier-based co-delivery approaches encompassing a wide range of P-gp inhibitors along with chemotherapeutic agents. We discuss the contributions of active targeting and stimuli responsive systems in imparting site-specific cytotoxicity and reducing both the dose and adverse effects.

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Section: The Menace Of P-gp Facilitated Mdr In Breast Cancermentioning

confidence: 99%

Exploring new Horizons in overcoming P-glycoprotein-mediated multidrug-resistant breast cancer via nanoscale drug delivery platforms

Famta

Shah

Chatterjee

et al. 2021

Current Research in Pharmacology and Drug Discovery

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Fully automatic flow-based device for monitoring of drug permeation across a cell monolayer

et al. 2015

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A novel flow-programming setup based on the sequential injection principle is herein proposed for on-line monitoring of temporal events in cell permeation studies. The permeation unit consists of a Franz cell with its basolateral compartment mixed under mechanical agitation and thermostated at 37 °C. The apical compartment is replaced by commercially available Transwell inserts with a precultivated cell monolayer. The transport of drug substances across epithelial cells genetically modified with the P-glycoprotein membrane transporter (MDCKII-MDR1) is monitored on-line using rhodamine 123 as a fluorescent marker. The permeation kinetics of the marker is obtained in a fully automated mode by sampling minute volumes of solution from the basolateral compartment in short intervals (10 min) up to 4 h. The effect of a P-glycoprotein transporter inhibitor, verapamil as a model drug, on the efficiency of the marker transport across the cell monolayer is thoroughly investigated. The analytical features of the proposed flow method for cell permeation studies in real time are critically compared against conventional batch-wise procedures and microfluidic devices.

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Lipid nanocarrier of selegiline augmented anti-Parkinson’s effect via P-gp modulation using quercetin

Qamar

Ashhar

Annu

et al. 2021

International Journal of Pharmaceutics

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P-glycoprotein (P-gp/MDR1)/ABCB1

Cited by 4 publications

References 323 publications

Exploring new Horizons in overcoming P-glycoprotein-mediated multidrug-resistant breast cancer via nanoscale drug delivery platforms

Exploring new Horizons in overcoming P-glycoprotein-mediated multidrug-resistant breast cancer via nanoscale drug delivery platforms

Fully automatic flow-based device for monitoring of drug permeation across a cell monolayer

Lipid nanocarrier of selegiline augmented anti-Parkinson’s effect via P-gp modulation using quercetin

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