Preparation and characterization of albumin nanoparticles encapsulating curcumin intended for the treatment of breast cancer

Abstract

Introduction:For the real-time clinical utilization of curcumin (an ayurvedic natural product) to treat breast cancer, its dissolution, rate limited solubility, poor tissue absorption, and extensive in vivo metabolism that leads to its poor systemic bioavailability should be overcome. A polymer-based nanoparticle formulation using bovine serum albumin can increase its aqueous solubility and can achieve protected, sustained, and targeted therapy in breast cancer.Materials and Methods:Desolvation technique was optimized for the preparation of albumin nanoparticles. Particle size, drug release, encapsulation efficiency, drug polymer interaction were the in vitro properties that were determined. Cell culture studies, in vivo pharmacokinetics in rats were used for biological characterization of the formulation.Results:The formulations were successfully prepared using 1:1, 1:2, 1:3, 1:4 drug: polymer ratios and the percent entrapment was found to be 74.76%, 91.01%, 85.36%, 86.42%, respectively, and particle size determined by zetasizer was found to be 225.1, 223.5, 226.3, 228.7 nm, respectively, and in vitro release was sustained for at least one month with drug release of 75.74%, 65.97%, 64.42%, 54%, respectively. The dissolution rate and aqueous solubility of curcumin was enhanced with this formulation. Fourier transform infrared spectroscopy (FTIR) studies demonstrated that the drug was not changed in the formulation during the fabrication process. The proliferation assays in MDA-MB-231 tumor cell lines indicated more effectiveness of the formulation compared to its solution form. In rats, albumin nanoparticles sustained drug release, demonstrated more bioavailability, improved pharmacokinetic properties, and enhanced tissue targetability of the drug.Conclusions:An effective curcumin-albumin nanoparticle formulation was successfully developed using a desolvation technique.

Therapeutic actions of curcumin in bone disorders

“…Consequently, this enhancement leads to a significant antiproliferative effect (IC 50 ¼ 70 mM) in MDA-MB-231 cells as compared with free curcumin (IC 50 ¼ 90 mM at 72 h). 59 In consistence with that data, Wartlick et al 66 previously reported that the presence of albumin in nano-formulation increased the endocytic uptake and the accumulation of the loaded drug within tumor site.…”

“…57 Pharmacokinetic studies reported that curcumin nano-formulation displayed a larger area under curve (AUC)-time curve as compared with free curcumin. [57][58][59] For example, encapsulation of curcumin by poly(lactic-co-glycolide) (PLGA) nanoparticles provided a significant higher maximal concentration (1000-fold increase) as compared with free curcumin following 60 min of i.v. administration in mice.…”

“…59,65 In addition, because of its various drug-binding sites, albumin enhances considerably the amount of curcumin within particle matrices. By modulating the curcumin polymer ratio, Jithan et al 59 obtained a final entrapment efficiency of 86.42% and a percent yield of 85.2%.…”

“…59,65 In addition, because of its various drug-binding sites, albumin enhances considerably the amount of curcumin within particle matrices. By modulating the curcumin polymer ratio, Jithan et al 59 obtained a final entrapment efficiency of 86.42% and a percent yield of 85.2%. Interestingly, the curcumin released from albumin nanoparticles dissolved in phosphate buffer pH 7.4 was almost fourfold higher than that of free curcumin, strongly suggesting that solubility of curcumin with curcumin nanoparticles can be enhanced in vivo.…”

In situ preparation of water-soluble ginsenoside Rh2-entrapped bovine serum albumin nanoparticles: in vitro cytocompatibility studies

“…Prominently, these protein nanocarriers possess many surface charge groups which are found to be advantageous in the loading or entrapment of numerous drug molecules. 11 Moreover, the unique ligand delivery property of albumin is found to be advantageous in enhancing the solubility of various hydrophobic drugs combined with serum albumin by loading, entrapment, or conjugation and helps in improving the pharmacokinetics of drug molecules in a biological environment. 9 These unique properties of serum albumin make it an ideal choice for drug delivery applications and development of drug delivery carriers.…”