High mortality of choroidal melanoma(CM)is mainly attributed to the high likelihood of tumorous recurrence.The essential challenge lies in the presence of residual CM cells survived from the antitumor treatment.These ...High mortality of choroidal melanoma(CM)is mainly attributed to the high likelihood of tumorous recurrence.The essential challenge lies in the presence of residual CM cells survived from the antitumor treatment.These residual tumorous cells are most likely to cause tumorous recurrence.This article reports the preparation of a multifunctional nanocomposite which can be used to treat CM efficiently via a chemotherapyassisted-photothermal therapy(CTH-PTT).The nanocomposite comprises of alpha-tocopheryl succinate(α-TOS)and carboxylic chitosan modified graphene(CG).α-TOS has been potentially seen as an efficient CTH antitumor drug while its deficiency such as easy being hydrolyzed by gastrointestinal esterase and poor hydrophilicity inevitable limits the clinic application ofα-TOS.CG is introduced to overcome these shortcomings,offering additional advantages such as the PTT possibility for the antitumor application.The employment of CG-α-TOS on ocular CM cells caused more than 80%inhibition rates after irradiation under an 808 nm laser for 10 min.The outcomes of this work provide a facile and advantageous way to resolve the essential issue of the treatment of ocular tumors such as CM.展开更多
Until now, there are no publications about the preformulation studies on(S)-zaltoprofen((S)-ZPF). Hence, we first investigated the solubility of(S)-ZPF, screened solubilizers and performed the pharmacokinetic study of...Until now, there are no publications about the preformulation studies on(S)-zaltoprofen((S)-ZPF). Hence, we first investigated the solubility of(S)-ZPF, screened solubilizers and performed the pharmacokinetic study of(S)-ZPF in the presence of the solubilizers. The measurement of the solubility of(S)-ZPF in 26 different solvents was carried out, including d-alpha tocopheryl polyethylene glycol 1000 succinate(TPGS), 2-hydroxypropyl-β-cyclodextrin(HPCD), and mixtures of individual solvent. The plasma concentration of(S)-ZPF and the amount of(S)-ZPF retained in stomach were determined after oral(35.0 mg/kg) and intravenous(5.0 mg/kg) administration. The solubility of(S)-ZPF showed an increase of 484-fold in TPGS compared to its aqueous solubility. There was a significant increase of AUC 0-24 h for pure(S)-ZPF in the TPGS group(813.59 ± 64.17 μg h/ml) in comparison with AUC 0-24 h in the HPCD group(595.57 ± 71.76 μg h/ml) and water group(465.57 ± 90.89 μg h/ml). In addition, the T max of(S)-ZPF in the TPGS group was 2 h, much faster than that in the HPCD or water groups(5.50 or 5.67 h, respectively). This suggested that TPGS played a significant role in the increase of solubility and bioavailability of(S)-ZPF.展开更多
基金financially supported by the National Natural Science Foundation of China(Nos.82202354,U20A20338)the Summit Advancement Disciplines of Zhejiang Province(Wenzhou Medical University Pharmaceutics)Key R&D Program of Zhejiang Province(No.2021C04019)。
文摘High mortality of choroidal melanoma(CM)is mainly attributed to the high likelihood of tumorous recurrence.The essential challenge lies in the presence of residual CM cells survived from the antitumor treatment.These residual tumorous cells are most likely to cause tumorous recurrence.This article reports the preparation of a multifunctional nanocomposite which can be used to treat CM efficiently via a chemotherapyassisted-photothermal therapy(CTH-PTT).The nanocomposite comprises of alpha-tocopheryl succinate(α-TOS)and carboxylic chitosan modified graphene(CG).α-TOS has been potentially seen as an efficient CTH antitumor drug while its deficiency such as easy being hydrolyzed by gastrointestinal esterase and poor hydrophilicity inevitable limits the clinic application ofα-TOS.CG is introduced to overcome these shortcomings,offering additional advantages such as the PTT possibility for the antitumor application.The employment of CG-α-TOS on ocular CM cells caused more than 80%inhibition rates after irradiation under an 808 nm laser for 10 min.The outcomes of this work provide a facile and advantageous way to resolve the essential issue of the treatment of ocular tumors such as CM.
基金supported by the Basic Science Research Program (2016R1A2B4011294) through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology
文摘Until now, there are no publications about the preformulation studies on(S)-zaltoprofen((S)-ZPF). Hence, we first investigated the solubility of(S)-ZPF, screened solubilizers and performed the pharmacokinetic study of(S)-ZPF in the presence of the solubilizers. The measurement of the solubility of(S)-ZPF in 26 different solvents was carried out, including d-alpha tocopheryl polyethylene glycol 1000 succinate(TPGS), 2-hydroxypropyl-β-cyclodextrin(HPCD), and mixtures of individual solvent. The plasma concentration of(S)-ZPF and the amount of(S)-ZPF retained in stomach were determined after oral(35.0 mg/kg) and intravenous(5.0 mg/kg) administration. The solubility of(S)-ZPF showed an increase of 484-fold in TPGS compared to its aqueous solubility. There was a significant increase of AUC 0-24 h for pure(S)-ZPF in the TPGS group(813.59 ± 64.17 μg h/ml) in comparison with AUC 0-24 h in the HPCD group(595.57 ± 71.76 μg h/ml) and water group(465.57 ± 90.89 μg h/ml). In addition, the T max of(S)-ZPF in the TPGS group was 2 h, much faster than that in the HPCD or water groups(5.50 or 5.67 h, respectively). This suggested that TPGS played a significant role in the increase of solubility and bioavailability of(S)-ZPF.
