| DOI: https://doi.org/10.14456/mujps.2015.21 | Pharm Sci Asia 2015; 42(4), 169-177 |
Effect of hydrophobic nanoparticle cores on the characteristics of poly(ε-caprolactone)-co-d-α-tocopheryl polyethylene glycol 1000 succinate nanoparticles loaded with camptothecin Y. Sirithananchai1, VB. Junyaprasert1,2, K. Sakchaisri3, J. Suksiriworapong1,2*
1 Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand
2 Center of Excellence in Innovative Drug Delivery and Nanomedicine, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand
3 Department of Pharmacology, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand
The clinical efficacy of camptothecin (CPT), a potent antitumor drug, is restricted by its insolubility in aqueous and organic solvents and its instability in physiological fluid. The incorporation of drug in nanoparticles can minimize these problems. Since CPT exhibits hydrophobic properties, the nanoparticle core with different hydrophobicity may affect the characteristics of nanoparticles. This study aimed to investigate the effect of hydrophobicity of the nanoparticle core on the characteristics of poly(ε-caprolactone)-co-d-α-tocopheryl polyethylene glycol 1000 succinate (PCL-TPGS) nanoparticles for the entrapment of CPT. The result found that the increasing hydrophobicity of the nanoparticle core significantly enlarged the particle size of blank nanoparticles from 40 nm to 164 nm while it decreased the polydispersity index (PdI) from 0.518 to 0.242 and the zeta potential (ZP) from -1.79 mV to -22.9 mV. After drug loading, the particle size increased but the ZP remained almost unchanged as compared to the blank nanoparticles. The initial fed amount of CPT at 0.1 mg yielded the highest %entrapment efficiency (%EE). The increasing amount of CPT dramatically decreased %EE from 94.03-96.73% to 18.96-22.53% but slightly increased %drug loading from 0.073-0.077% to 0.085-0.092%. The results suggested that the hydrophobicity of the PCL-TPGS nanoparticle core affected the characteristics of nanoparticles. From these results, the 3:1 PCL-TPGS nanoparticles loading with 0.1 mg of CPT showed the desirable size (smaller than 200 nm), narrow PdI, and highest %EE. Therefore, this formulation will be chosen for the development of CPT delivery system.
Keyword:
Camptothecin, Poly(ε-caprolactone), d-α-Tocopheryl polyethylene glycol 1000 succinate, Nanoparticles, Hydrophobic
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