Abstract: The goal of the present work was to study the feasibility of 10-hydroxycamptothecin (HCPT) nanoparticle preparation using supercritical antisolvent (SAS) precipitation. The influences of various experimental factors on the mean particle size (MPS) of HCPT nanoparticles were investigated. The optimum micronization conditions are determined as follows: HCPT solution concentration 0.5 mg/mL, the flow rate ratio of CO2 and HCPT solution 19.55, precipitation temperature 35 °C and precipitation pressure 20 MPa. Under the optimum conditions, HCPT nanoparticles with a MPS of 180 ± 20.3 nm were obtained. Moreover, the HCPT nanoparticles obtained were characterized by Scanning electron microscopy, Dynamic light scattering, Fourier-transform infrared spectroscopy, High performance liquid chromatography-mass spectrometry, X-ray diffraction and Differential scanning calorimetry analyses. The physicochemical characterization results showed that the SAS process had not induced degradation of HCPT. Finally, the dissolution rates of HCPT nanoparticles were investigated and the results proved that there is a significant increase in dissolution rate compared to unprocessed HCPT.
Keywords: 10-hydroxycamptothecin; supercritical antisolvent; nanoparticles; preparation; physicochemical properties
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Zhao, X.; Zu, Y.; Jiang, R.; Wang, Y.; Li, Y.; Li, Q.; Zhao, D.; Zu, B.; Zhang, B.; Sun, Z.; Zhang, X. Preparation and Physicochemical Properties of 10-Hydroxycamptothecin (HCPT) Nanoparticles by Supercritical Antisolvent (SAS) Process. Int. J. Mol. Sci. 2011, 12, 2678-2691.
Zhao X, Zu Y, Jiang R, Wang Y, Li Y, Li Q, Zhao D, Zu B, Zhang B, Sun Z, Zhang X. Preparation and Physicochemical Properties of 10-Hydroxycamptothecin (HCPT) Nanoparticles by Supercritical Antisolvent (SAS) Process. International Journal of Molecular Sciences. 2011; 12(4):2678-2691.
Zhao, Xiuhua; Zu, Yuangang; Jiang, Ru; Wang, Ying; Li, Yong; Li, Qingyong; Zhao, Dongmei; Zu, Baishi; Zhang, Baoyou; Sun, Zhiqiang; Zhang, Xiaonan. 2011. "Preparation and Physicochemical Properties of 10-Hydroxycamptothecin (HCPT) Nanoparticles by Supercritical Antisolvent (SAS) Process." Int. J. Mol. Sci. 12, no. 4: 2678-2691.