scholarly journals Evaluation of Drug-Loading Ability of Poly(Lactic Acid)/Hydroxyapatite Core–Shell Particles

Materials ◽  
2021 ◽  
Vol 14 (8) ◽  
pp. 1959
Author(s):  
Seiya Suzuki ◽  
Sungho Lee ◽  
Tatsuya Miyajima ◽  
Katsuya Kato ◽  
Ayae Sugawara-Narutaki ◽  
...  

Poly(lactic acid)/hydroxyapatite (PLA/HAp) core–shell particles are prepared using the emulsification method. These particles are safe for living organisms because they are composed of biodegradable polymers and biocompatible ceramics. These particles are approximately 50–100 nm in size, and their hydrophobic substance loading can be controlled. Hence, PLA/HAp core–shell particles are expected to be used as drug delivery carriers for hydrophobic drugs. In this work, PLA/HAp core–shell particles with a loading of vitamin K1 were prepared, and their drug-loading ability was evaluated. The particles were 40–80 nm in diameter with a PLA core and a HAp shell. The particle size increased with an increase in the vitamin K1 loading. The drug-loading capacity (LC) value of the particles, an indicator of their drug-loading ability, was approximately 250%, which is higher than the previously reported values. The amount of vitamin K1 released from the particles increased as the pH of the soaking solution decreased because the HAp shell easily dissolved under the acidic conditions. The PLA/HAp particles prepared in this work were found to be promising candidates for drug delivery carriers because of their excellent drug-loading ability and pH sensitivity.

2021 ◽  
Vol 8 (3) ◽  
Author(s):  
Sungho Lee ◽  
Tatsuya Miyajima ◽  
Ayae Sugawara-Narutaki ◽  
Katsuya Kato ◽  
Fukue Nagata

Biodegradable nanoparticles have been well studied as biocompatible delivery systems. Nanoparticles of less than 200 nm in size can facilitate the passive targeting of drugs to tumour tissues and their accumulation therein via the enhanced permeability and retention (EPR) effect. Recent studies have focused on stimuli-responsive drug delivery systems (DDS) for improving the effectiveness of chemotherapy; for example, pH-sensitive DDS depend on the weakly acidic and neutral extracellular pH of tumour and normal tissues, respectively. In our previous work, core–shell nanoparticles composed of the biodegradable polymer poly(lactic acid) (PLA) and the widely used inorganic biomaterial hydroxyapatite (HAp, which exhibits pH sensitivity) were prepared using a surfactant-free method. These PLA/HAp core–shell nanoparticles could load 750 wt% of a hydrophobic model drug. In this work, the properties of the PLA/HAp core–shell nanoparticles loaded with the anti-cancer drug paclitaxel (PTX) were thoroughly investigated in vitro . Because the PTX-containing nanoparticles were approximately 80 nm in size, they can be expected to facilitate efficient drug delivery via the EPR effect. The core–shell nanoparticles were cytotoxic towards cancer cells (4T1). This was due to the pH sensitivity of the HAp shell, which is stable in neutral conditions and dissolves in acidic conditions. The cytotoxic activity of the PTX-loaded nanoparticles was sustained for up to 48 h, which was suitable for tumour growth inhibition. These results suggest that the core–shell nanoparticles can be suitable drug carriers for various water-insoluble drugs.


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