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mPEG-Cholic acid/TPGS mixed micelles for combined delivery of paclitaxel and bufalin to treat hepatocellular carcinoma.
Liu, Yujia; Lu, Xiaoyu; Zhang, Zhenhai; Jiang, Shulong; Lv, Huixia.
Afiliação
  • Liu Y; Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, China.
  • Lu X; Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, China.
  • Zhang Z; Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, China.
  • Jiang S; Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, China.
  • Lv H; Clinical Medical Laboratory Center, Jining No. 1 People's Hospital, Jining, Shandong, China.
Pharm Dev Technol ; 27(2): 215-227, 2022 Feb.
Article em En | MEDLINE | ID: mdl-35105263
ABSTRACT
In this study, amphiphilic block copolymer mPEG-cholic acid was synthesized in conjunction with TPGS as stabilizer to prepare multifunctional micelles. The formed polymeric micelles (PCTm) were used for the delivery of paclitaxel (PTX) and bufalin (BF). PEG group could enhance solubility and extend circulation time, while cholic acid groups achieved the liver targeted function. Combinations of these approaches could realize a synergistic therapeutic effect in the treatment of advanced hepatocellular carcinoma. CLSM in vitro results demonstrated that drug capsulation into PCTm could enhance cellular uptake. FCM results confirmed the uptake amount of C6/PCTm was 7.5-fold higher than that of free C6 after incubation for 2 h. Competitive inhibition test proved the Na+-taurocholate co-transporting polypeptide (NTCP) involved in the uptake mechanism of PCTm. Meanwhile, in vivo imaging assays demonstrated that the fluorescence intensity of Cy5.5/PCTm was higher than that of free Cy5.5 on liver and tumor with extended circulation time to 48 h. In addition, in vivo studies confirmed that the combined therapy exhibited the strongest tumor inhibition rate of 82.29% with lower systemic toxicity. Hence, these results indicated that PCTm could provide a promising strategy for targeting hepatocellular carcinoma and achieve the goal of synergism and attenuation.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Carcinoma Hepatocelular / Neoplasias Hepáticas / Antineoplásicos Fitogênicos Limite: Humans Idioma: En Revista: Pharm Dev Technol Assunto da revista: FARMACIA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: China

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Carcinoma Hepatocelular / Neoplasias Hepáticas / Antineoplásicos Fitogênicos Limite: Humans Idioma: En Revista: Pharm Dev Technol Assunto da revista: FARMACIA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: China