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  • One platform comparison of estrone and folic acid anchored surface engineered MWCNTs for doxorubicin delivery.

One platform comparison of estrone and folic acid anchored surface engineered MWCNTs for doxorubicin delivery.

Molecular pharmaceutics (2014-12-18)
Neelesh Kumar Mehra, N K Jain
ABSTRACT

Our main aim in the present investigation was to assess and compare the in vitro and in vivo cancer targeting propensity of doxorubicin (DOX) loaded folic acid (FA) and estrone (ES) anchored PEGylated multiwalled carbon nanotubes (MWCNTs) employing tumor bearing Balb/c mice. The DOX was loaded into the developed functionalized MWCNTs after proper characterization using dialysis diffusion method. The in vitro, ex vivo, and in vivo studies were performed on the MCF-7 cell line for assessment of the cancer targeting propensity. Both qualitative and quantitative cell uptake studies indicated the preferential higher uptake of estrone anchored nanotube formulation compared to other formulations and free DOX owing to the overexpression of estrogen receptors (ERs) on human breast MCF-7 cells. Similarly, the pharmacokinetic and increased antitumor activities also confirmed the elevated cancer targeting propensity of the estrone and folic acid anchored MWCNT formulations. The DOX/ES-PEG-MWCNTs has also shown significantly longer survival span (43 days) than free DOX (18 days) and control group (12 days). Present outcomes from the ex vivo and in vivo studies are deemed to be of great scientific value and shall assist targeted drug delivery formulation scientists for selection of the targeting moieties in the treatment of human breast cancer.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Acetone, natural, ≥97%
Sigma-Aldrich
Acetone, ≥99%, FCC, FG
Sigma-Aldrich
Triethylamine, ≥99.5%
Sigma-Aldrich
Doxorubicin hydrochloride, suitable for fluorescence, 98.0-102.0% (HPLC)
Supelco
Acetone, analytical standard
Sigma-Aldrich
Hydrogen peroxide solution, 34.5-36.5%
Millipore
Hydrogen peroxide solution, 3%, suitable for microbiology
Sigma-Aldrich
Triethylamine, puriss. p.a., ≥99.5% (GC)
Sigma-Aldrich
Triethylamine, for amino acid analysis, ≥99.5% (GC)
Sigma-Aldrich
Triethylamine, BioUltra, ≥99.5% (GC)
Sigma-Aldrich
Triethylamine, ≥99%
USP
Estrone, United States Pharmacopeia (USP) Reference Standard
Doxorubicin hydrochloride, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
Acetone, ACS reagent, ≥99.5%
Sigma-Aldrich
Triethylamine, ampule, ≥99.5% (GC)
Estrone, European Pharmacopoeia (EP) Reference Standard
Supelco
Acetone, Pharmaceutical Secondary Standard; Certified Reference Material
USP
Acetone, United States Pharmacopeia (USP) Reference Standard
Supelco
Triethylamine, analytical standard
Sigma-Aldrich
Acetone, ACS reagent, ≥99.5%
Sigma-Aldrich
Acetone, puriss., meets analytical specification of Ph. Eur., BP, NF, ≥99% (GC)
Sigma-Aldrich
Acetone, puriss. p.a., ACS reagent, reag. ISO, reag. Ph. Eur., ≥99.5% (GC)
Sigma-Aldrich
Hydrogen peroxide solution, contains inhibitor, 35 wt. % in H2O
Sigma-Aldrich
Hydrogen peroxide solution, contains ~200 ppm acetanilide as stabilizer, 3 wt. % in H2O
Sigma-Aldrich
Acetone, histological grade, ≥99.5%
Sigma-Aldrich
Acetone, Laboratory Reagent, ≥99.5%
Sigma-Aldrich
Acetone, suitable for HPLC, ≥99.9%
Sigma-Aldrich
Acetone, HPLC Plus, for HPLC, GC, and residue analysis, ≥99.9%
Sigma-Aldrich
Acetone, suitable for HPLC, ≥99.8%
Supelco
Estrone, Pharmaceutical Secondary Standard; Certified Reference Material