Anti-tumor activity of intravenously administered plumbagin entrapped in targeted nanoparticles

Research output: Contribution to journalArticle

Abstract

Plumbagin, a naphthoquinone extracted from the officinal leadwort, has recently been shown to exert promising anti-cancer effects. However, its therapeutic use is hampered by its failure to specifically reach tumors after intravenous administration, without secondary effects on normal tissues. Its poor aqueous solubility and rapid elimination in vivo further limit its potential use.
We hypothesize that the entrapment of plumbagin within PEGylated PLGA nanoparticles conjugated with transferrin, whose receptors are overexpressed on many cancer cells, could result in a selective delivery to tumors following intravenous administration and enhance its chemotherapeutic effects.
The objectives of this study were therefore to prepare and characterize transferrin-targeted, PEGylated PLGA nanoparticles entrapping plumbagin, and to evaluate their therapeutic efficacy in vitro and in vivo.
The intravenous administration of transferrin-bearing PEGylated PLGA nanoparticles led to the complete suppression of 10% of B16-F10 tumors and regression of 30% of the tumors, with improvement of the animal survival compared to controls. The treatment was well tolerated by the animals.
Transferrin-bearing PEGylated PLGA nanoparticles entrapping plumbagin are therefore highly promising therapeutic systems, able to lead to tumor regression and even suppression after intravenous administration without visible toxicity.
LanguageEnglish
JournalJournal of Biomedical Nanotechnology
Publication statusAccepted/In press - 1 Aug 2019

Fingerprint

Nanoparticles
Tumors
Bearings (structural)
Transferrin
Intravenous Administration
Neoplasms
Animals
Naphthoquinones
Transferrin Receptors
Toxicity
Solubility
Therapeutic Uses
Cells
plumbagin
Tissue
polylactic acid-polyglycolic acid copolymer
Therapeutics

Keywords

  • Plumbagin
  • transferrin
  • tumor targeting
  • PEGylated OLGA nanoparticles
  • cancer treatment

Cite this

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title = "Anti-tumor activity of intravenously administered plumbagin entrapped in targeted nanoparticles",
abstract = "Plumbagin, a naphthoquinone extracted from the officinal leadwort, has recently been shown to exert promising anti-cancer effects. However, its therapeutic use is hampered by its failure to specifically reach tumors after intravenous administration, without secondary effects on normal tissues. Its poor aqueous solubility and rapid elimination in vivo further limit its potential use.We hypothesize that the entrapment of plumbagin within PEGylated PLGA nanoparticles conjugated with transferrin, whose receptors are overexpressed on many cancer cells, could result in a selective delivery to tumors following intravenous administration and enhance its chemotherapeutic effects.The objectives of this study were therefore to prepare and characterize transferrin-targeted, PEGylated PLGA nanoparticles entrapping plumbagin, and to evaluate their therapeutic efficacy in vitro and in vivo.The intravenous administration of transferrin-bearing PEGylated PLGA nanoparticles led to the complete suppression of 10{\%} of B16-F10 tumors and regression of 30{\%} of the tumors, with improvement of the animal survival compared to controls. The treatment was well tolerated by the animals. Transferrin-bearing PEGylated PLGA nanoparticles entrapping plumbagin are therefore highly promising therapeutic systems, able to lead to tumor regression and even suppression after intravenous administration without visible toxicity.",
keywords = "Plumbagin, transferrin, tumor targeting, PEGylated OLGA nanoparticles, cancer treatment",
author = "Intouch Sakpakdeejaroen and Sukrut Somani and Partha Laskar and Craig Irving and Margaret Mullin and Christine Dufes",
year = "2019",
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AU - Sakpakdeejaroen, Intouch

AU - Somani, Sukrut

AU - Laskar, Partha

AU - Irving, Craig

AU - Mullin, Margaret

AU - Dufes, Christine

PY - 2019/8/1

Y1 - 2019/8/1

N2 - Plumbagin, a naphthoquinone extracted from the officinal leadwort, has recently been shown to exert promising anti-cancer effects. However, its therapeutic use is hampered by its failure to specifically reach tumors after intravenous administration, without secondary effects on normal tissues. Its poor aqueous solubility and rapid elimination in vivo further limit its potential use.We hypothesize that the entrapment of plumbagin within PEGylated PLGA nanoparticles conjugated with transferrin, whose receptors are overexpressed on many cancer cells, could result in a selective delivery to tumors following intravenous administration and enhance its chemotherapeutic effects.The objectives of this study were therefore to prepare and characterize transferrin-targeted, PEGylated PLGA nanoparticles entrapping plumbagin, and to evaluate their therapeutic efficacy in vitro and in vivo.The intravenous administration of transferrin-bearing PEGylated PLGA nanoparticles led to the complete suppression of 10% of B16-F10 tumors and regression of 30% of the tumors, with improvement of the animal survival compared to controls. The treatment was well tolerated by the animals. Transferrin-bearing PEGylated PLGA nanoparticles entrapping plumbagin are therefore highly promising therapeutic systems, able to lead to tumor regression and even suppression after intravenous administration without visible toxicity.

AB - Plumbagin, a naphthoquinone extracted from the officinal leadwort, has recently been shown to exert promising anti-cancer effects. However, its therapeutic use is hampered by its failure to specifically reach tumors after intravenous administration, without secondary effects on normal tissues. Its poor aqueous solubility and rapid elimination in vivo further limit its potential use.We hypothesize that the entrapment of plumbagin within PEGylated PLGA nanoparticles conjugated with transferrin, whose receptors are overexpressed on many cancer cells, could result in a selective delivery to tumors following intravenous administration and enhance its chemotherapeutic effects.The objectives of this study were therefore to prepare and characterize transferrin-targeted, PEGylated PLGA nanoparticles entrapping plumbagin, and to evaluate their therapeutic efficacy in vitro and in vivo.The intravenous administration of transferrin-bearing PEGylated PLGA nanoparticles led to the complete suppression of 10% of B16-F10 tumors and regression of 30% of the tumors, with improvement of the animal survival compared to controls. The treatment was well tolerated by the animals. Transferrin-bearing PEGylated PLGA nanoparticles entrapping plumbagin are therefore highly promising therapeutic systems, able to lead to tumor regression and even suppression after intravenous administration without visible toxicity.

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KW - transferrin

KW - tumor targeting

KW - PEGylated OLGA nanoparticles

KW - cancer treatment

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