Studying the effect of physically-adsorbed coating polymers on the cytotoxic activity of optimized bisdemethoxycurcumin loaded-PLGA nanoparticles.
The aim of this work was to study the effect of different physically-adsorbed coating polymers on the cytotoxic activity of optimized bisdemethoxycurcumin (BDMC) loaded-PLGA nanoparticles. BDMC-loaded poly(DL-lactide-co-glycolide) (PLGA) nanoparticles were prepared adopting the nanoprecipitation technique according to a full factorial study design. The effects of three independent variables each at two levels, namely: the polymer type, polymer concentration, and poly vinyl alcohol concentration were studied. The particles were optimized regarding particle size and entrapment efficiency where sizes <200 nm and entrapment efficiencies reaching ∼98% were obtained. The particles were further characterized using x-ray diffraction, transmission electron microscopy, and in-vitro release studies. A selected formulation was subjected to physical coating using various coating moieties, namely: PEG 4000, Tween 80 and Pluronic F68, to impart a hydrophilic stealth character to the surface. The surface hydrophobicity was assessed using the Rose Bengal dye test where the hydrophilicity character followed the following order: Tween 80 > PEG 4000 > Pluronic F68. The particles coating rendered the particles suitable for cancer-targeting regarding particle size measurements, morphology, release kinetics, and stability studies. Moreover, cytotoxicity testing was performed using HepG-2 cells. Coated NPs showed the highest inhibition of malignant cells viability compared to the uncoated NPs and free BDMC where the IC50of Pluronic-F68 coated NPs was 0.54 ± 0.01 µg/mL. The augmented effect against malignant cells poses these particles as a successful cancer remedy. © 2017 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 105A: 1433-1445, 2017.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Mina
M
Mehanny
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Rania M
RM
Hathout
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Ahmed S
AS
Geneidi
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.|Department of Pharmaceutical Technology, Faculty of Pharmacy and Biotechnology, German University in Cairo, Egypt.
Samar
S
Mansour
D020099:Coated Materials, Biocompatible / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D003474:Curcumin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D003603:Cytotoxins / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D036381:Diarylheptanoids; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D056945:Hep G2 Cells; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D053758:Nanoparticles / Q000737:chemistry / Q000627:therapeutic use; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D011100:Polyglycolic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
D020099:Coated Materials, Biocompatible; D003603:Cytotoxins; D036381:Diarylheptanoids; D004337:Drug Carriers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; C034786:bisdemethoxycurcumin; D019344:Lactic Acid; D003474:Curcumin
PLGA; bisdemethoxycurcumin; cytotoxicity; nanoparticles; physical adsorption