[Preparation and Characterization of Netupitant-loaded mPEG-PDLLA Nanoparticles].

Autor:	Wang SJ; Department of Biotherapy, Cancer Center, Sichuan University, Chengdu 610041, China.; School of chemical engineering, Changchun University of Technology, Changchun 130012, China.; Sinopharm A-THINK Pharmaceutical Co., Ltd., Changchun 130016, China., Liu Y; Department of Biotherapy, Cancer Center, Sichuan University, Chengdu 610041, China., Li Y; Department of Biotherapy, Cancer Center, Sichuan University, Chengdu 610041, China., He L; Beijing Funhau Medicine Technology Co., Ltd., Beijing 100176, China., Gou ML; Department of Biotherapy, Cancer Center, Sichuan University, Chengdu 610041, China.
Jazyk:	čínština
Zdroj:	Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition [Sichuan Da Xue Xue Bao Yi Xue Ban] 2019 Dec; Vol. 50 (6), pp. 896-900.
Abstrakt:	Objective: Methoxy poly (ethylene glycol)-poly (lactic acid) (mPEG-PDLLA) was used to increase water solubility of netupitant, thus to provide the experimental basis for development of the injection of netupitant. Methods: Film hydration method was ultilized to prepare the netupitant-loaded mPEG-PDLLA nanoparticles (NT/mPEG-PDLLA-NPs). The preparation formulation and technology were optimized based on the single factor tests by investigating the effect of netupitant/mPEG-PDLLA mass ratio ( m/m ), filming temperature and time on the mean particle diameters and loading capacities. The size distributions and Zeta potentials of NT/mPEG-PDLLA-NPs were investigated using dynamic light scattering analysis, and the morphology was observed under the transmission electron microscope (TEM). The cytotoxicity of NT/mPEG-PDLLA-NPs evaluated by MTT method. Results: The optimal NT/mPEG-PDLLA-NPs were achieved at the netupitant/mPEG-PDLLA mass ratio of 1/6 with filming temperature at 55 ℃ and filming time for 30 min. The resulting NT/mPEG-PDLLA-NPs displayed an opalescent and translucent appearance, with a high loading capacity of 14% and netupitant concentration of 10 mg/mL. NT/mPEG-PDLLA-NPs showed a spherical morphology, with a mean diameter of 58 nm and a nearly neutral Zeta potential of -0.29 mV. The NT/mPEG-PDLLA-NPs showed a cytotoxicity similar to free NT. Conclusion: Netupitant was successfully loaded into mPEG-PDLLA-NPs to significantly increased the water solubility, thus providing the experimental foundation for the further development of injection of netupitant. (Copyright© by Editorial Board of Journal of Sichuan University (Medical Science Edition).)
Databáze:	MEDLINE
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