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Biodistribution of TAT or QLPVM coupled to receptor targeted liposomes for delivery of anticancer therapeutics to brain in vitro and in vivo. | LitMetric

Biodistribution of TAT or QLPVM coupled to receptor targeted liposomes for delivery of anticancer therapeutics to brain in vitro and in vivo.

Nanomedicine

Department of Pharmaceutical Sciences, School of Pharmacy, College of Health Professions, North Dakota State University, Fargo, ND, USA. Electronic address:

Published: January 2020

AI Article Synopsis

  • - Combination therapy is a promising strategy for treating glioblastoma by using multiple mechanisms to target cancer cells, which helps to minimize drug resistance.
  • - The challenge of delivering chemotherapy across the blood-brain barrier (BBB) led to the development of dual functionalized liposomes, enhanced with transferrin and cell-penetrating peptides for better drug transport.
  • - Studies demonstrated that these Tf-CPP liposomes significantly improve the accumulation of doxorubicin and erlotinib in the brain compared to free drugs, showing a considerable increase in drug delivery without toxicity.

Article Abstract

Combination therapy has emerged as an efficient way to deliver chemotherapeutics for treatment of glioblastoma. It provides collaborative approach of targeting cancer cells by acting via multiple mechanisms, thereby reducing drug resistance. However, the presence of impermeable blood brain barrier (BBB) restricts the delivery of chemotherapeutic drugs into the brain. To overcome this limitation, we designed a dual functionalized liposomes by modifying their surface with transferrin (Tf) and a cell penetrating peptide (CPP) for receptor and adsorptive mediated transcytosis, respectively. In this study, we used two different CPPs (based on physicochemical properties) and investigated the influence of insertion of CPP to Tf-liposomes on biocompatibility, cellular uptake, and transport across the BBB both in vitro and in vivo. The biodistribution profile of Tf-CPP liposomes showed more than 10 and 2.7 fold increase in doxorubicin and erlotinib accumulation in mice brain, respectively as compared to free drugs with no signs of toxicity.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6935563PMC
http://dx.doi.org/10.1016/j.nano.2019.102112DOI Listing

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