Skip to Content
Merck

Improved delivery of the natural anticancer drug tetrandrine.

International journal of pharmaceutics (2014-12-17)
Chen Shi, Saeed Ahmad Khan, Kaiping Wang, Marc Schneider
ABSTRACT

The study aims at designing a nanoparticle-based delivery system to improve the efficacy of the natural compound tetrandrine against lung cancer. Nanoparticles from poly(lactic-co-glycolic acid) (PLGA) were prepared by the emulsion solvent diffusion method and characterized for their physicochemical properties and drug-loading efficiency. Furthermore, the cellular uptake and the anti-cancerous activity was studied on A549 cell line. To investigate the surface properties and uptake, three different stabilizers were used to analyze the effect on size and zeta potential of nanoparticles as well as the effect on the cellular uptake. Nanoparticles in the size range of 180-200 nm with spherical shape were obtained with polyvinyl alcohol (PVA), Pluronic-F127 (PF127) and didodecyldimethylammonium bromide (DMAB), 2%, 1% and 0.1%, respectively. An entrapment efficiency of 50-60% with a loading of 1.5-2% was observed. In vitro release profile at pH 7.4 PBS solution showed a consistent release over 168 h. All particle systems showed an improved performance over the pure drug at the same drug concentration. DMAB stabilized particles demonstrated the most pronounced effect against A549 cells compared to pure drug while PVA stabilized particles were least effective in terms of antitumor activity.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Phosphoric acid-16O4 solution, 70 wt. % in D2O, 99.9 atom % 16O
Sigma-Aldrich
4-(Dimethylamino)pyridine, purum, ≥98.0% (NT)
Sigma-Aldrich
Phosphoric acid, crystalline, ≥99.999% trace metals basis
Sigma-Aldrich
Phosphoric acid, 85 wt. % in H2O, 99.99% trace metals basis
Sigma-Aldrich
Ethyl alcohol, Pure, 190 proof, ACS spectrophotometric grade, 95.0%
Sigma-Aldrich
Ethyl alcohol, Pure, 190 proof, meets USP testing specifications
Sigma-Aldrich
Phosphoric acid, ≥85 wt. % in H2O, ≥99.999% trace metals basis
Sigma-Aldrich
4-(Dimethylamino)pyridine, ReagentPlus®, ≥99%
Supelco
Ethanol standards 10% (v/v), 10 % (v/v) in H2O, analytical standard
Sigma-Aldrich
Ethanol, BioUltra, for molecular biology, ≥99.8%, (absolute alcohol, without additive, A15 o1)
Sigma-Aldrich
Ethyl alcohol, Pure, 200 proof, meets USP testing specifications
Sigma-Aldrich
Ethyl alcohol, Pure, 200 proof
Sigma-Aldrich
Phosphoric acid, BioReagent, suitable for insect cell culture, 85%
Sigma-Aldrich
Hydrogen chloride, ReagentPlus®, ≥99%
Sigma-Aldrich
Ethanol, ACS reagent, prima fine spirit, without additive, F15 o1
Sigma-Aldrich
Ethyl alcohol, Pure 200 proof, for molecular biology
Sigma-Aldrich
Ethyl alcohol, Pure, 200 proof, ACS reagent, ≥99.5%
Sigma-Aldrich
Phosphoric acid, BioUltra, ≥85% (T)
Sigma-Aldrich
Ethyl alcohol, Pure, 200 proof, anhydrous, ≥99.5%
Sigma-Aldrich
Phosphoric acid, puriss. p.a., crystallized, ≥99.0% (T)
Sigma-Aldrich
Phosphoric acid, ACS reagent, ≥85 wt. % in H2O
Sigma-Aldrich
Phosphoric acid, puriss. p.a., ACS reagent, reag. ISO, reag. Ph. Eur., ≥85%
Sigma-Aldrich
Phosphoric acid, ACS reagent, ≥85 wt. % in H2O
Sigma-Aldrich
Phosphoric acid, puriss., meets analytical specification of Ph. Eur., BP, NF, FCC, 85.0-88.0%
Sigma-Aldrich
Ethanol, purum, absolute ethanol, denaturated with 2% 2-butanone, A15 MEK1, ≥99.8% (based on denaturant-free substance)
Sigma-Aldrich
Ethanol, purum, fine spirit, denaturated with 4.8% methanol, F25 METHYL1, ~96% (based on denaturant-free substance)
Supelco
Dehydrated Alcohol, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Acetone, natural, ≥97%
Sigma-Aldrich
Phosphoric acid solution, NMR reference standard, 85% in D2O (99.9 atom % D), NMR tube size 4.2 mm × 8 in. , WGS-5BL Coaxial NMR tube
Sigma-Aldrich
Hydrogen chloride solution, 3 M in cyclopentyl methyl ether (CPME)