A Cost-Effective Nano-Sized Curcumin Delivery System with High Drug Loading Capacity Prepared via Flash Nanoprecipitation.

Zhuo Chen,Li Li,Xuhong Guo,Zhinan Fu,Enguang Ma

doi:10.3390/nano11030734

Abstract

Flash nanoprecipitation (FNP) is an efficient technique for encapsulating drugs in particulate carriers assembled by amphiphilic polymers. In this study, a novel nanoparticular system of a model drug curcumin (CUR) based on FNP technique was developed by using cheap and commercially available amphiphilic poly(vinyl pyrrolidone) (PVP) as stabilizer and natural polymer chitosan (CS) as trapping agent. Using this strategy, high encapsulation efficiency (EE > 95%) and drug loading capacity (DLC > 40%) of CUR were achieved. The resulting CUR-loaded nanoparticles (NPs) showed a long-term stability (at least 2 months) and pH-responsive release behavior. This work offers a new strategy to prepare cost-effective drug-loaded NPs with high drug loading capacity and opens a unique opportunity for industrial scale-up.

Highlights

(NPs) showed a long-term stability and pH-responsive release behavior
Polymeric nanoparticles (NPs) have been demonstrated as a promising opportunity to load hydrophobic anti-cancer drugs [9,10,11,12,13], in which amphiphilic polymers are commonly used as stabilizers to protect hydrophobic drugs through the intermolecular forces such as hydrogen bonding, hydrophobic, and electrostatic interactions, improving the solubility of hydrophobic drugs in aqueous solution and prolonging the internal circulation time [14,15]
In Flash nanoprecipitation (FNP), amphiphilic stabilizers and hydrophobic active ingredients are molecularly dissolved in a water-miscible organic solvent and rapidly mixed with aqueous antisolvent streams to drive controlled precipitation of the solutes, leading to the formation of NPs with tunable particle sizes and high encapsulation efficiency (>90%) [22,23]

Summary

Introduction

(NPs) showed a long-term stability (at least 2 months) and pH-responsive release behavior. More and more anti-cancer drugs have been developed, many have low water solubility [2]. Polymeric nanoparticles (NPs) have been demonstrated as a promising opportunity to load hydrophobic anti-cancer drugs [9,10,11,12,13], in which amphiphilic polymers are commonly used as stabilizers to protect hydrophobic drugs through the intermolecular forces such as hydrogen bonding, hydrophobic, and electrostatic interactions, improving the solubility of hydrophobic drugs in aqueous solution and prolonging the internal circulation time [14,15]. In FNP, amphiphilic stabilizers and hydrophobic active ingredients are molecularly dissolved in a water-miscible organic solvent and rapidly mixed with aqueous antisolvent streams to drive controlled precipitation of the solutes, leading to the formation of NPs with tunable particle sizes (from 30 nm to 2 μm) and high encapsulation efficiency (>90%) [22,23]. Chow’s group successfully stabilized hydrophobic drug CUR with poly(DL-lactide)-b-polyethylene glycol (PLA-b-PEG) via FNP approach followed

Methods

Results

Conclusion