Review Article

Lipid-Based Nanocarrier Systems for Drug Delivery: Advances and Applications

Zhao, Yan-Qi; Li, Li-Jun; Zhou, Er-Fen; Wang, Jiang-Yue; Wang, Ying; Guo, Lin-Miao; Zhang, Xin-Xin

The review summarized the advances and applications of lipid-based nanocarriers from traditional to novel functional lipid preparations, including liposomes, stimuli-responsive lipid-based nanocarriers, ionizable lipid nanoparticles, lipid hybrid nanocarriers, as well as biomembrane-camouflaged nanoparticles, and further discussed the challenges and prospects of this system.

Original Article

Discovery of Indole-Containing Benzamide Derivatives as HDAC1 Inhibitors with In Vitro and In Vivo Antitumor Activities

Gu, Xiu; Peng, Xin-Yan; Zhang, Hao; Han, Bo; Jiao, Min-Ru; Chen, Qiu-Shi; Zhang, Qing-Wei

Compounds 3j was discovered as a novel HDAC1 inhibitor with potent antitumor activities. Compound 3j demonstrated acceptable safety profiles and favorable oral pharmacokinetic properties, and might have therapeutic potential for the treatment of human cancers in the future.

A Novel and Practical Synthesis of Isavuconazonium Sulfate via Anion Exchange Resin

Huang, Lei; Zhang, Yi; Chen, Hua; Wang, Wei-Wei; Li, Jian-Qi; Liu, Yu

An efficient and practical process for the synthesis of isavuconazonium sulfate (1), an antifungal agent, was firstly described through the usage of the ion exchange resin instead of H₂SO₄ to introduce HSO₄- in the formulation of quaternary ammonium salt (1). The overall yield of the process was 57.0%. The high-performance liquid chromatography purity of product was 97.25%, which was higher than that of the reference-listed drug.

Effect of Oxygen and Water on the Stability of Imipenem and Cilastatin Sodium for Injection

Zhang, Meng; Liu, Chun-Feng; Chen, Xiao-Yan; Yang, Li-Na; Zhu, Chun-Mei; Teng, Jian-Hao; Wu, Hao-Xiang; Zhang, Fu-Li

This study showed that oxygen, water, particle shape, and particle size had significant effects on the stability of IMI/CIL, and free water content is a better predictor of the safety and stability of IMI/CIL than the total water content. The study led to a better understanding of the degradation mechanism of IMI/CIL, and could provide a reference for the selection and control of IMI/CIL process conditions. IMI/CIL, imipenem and cilastatin sodium for injection.

A New Colorimetric DPPH Radical Scavenging Activity Method: Comparison with Spectrophotometric Assay in Some Medicinal Plants Used in Moroccan Pharmacopoeia

Babili, Fatiha EL; Nigon, Clotilde; Lacaze, Li; Millé, Juliette; Masiala, Anthony; Simm, Jennifer; Lamade, Virginie M.; Haj, Amal Ait El

This study established a new colorimetry DPPH radical scavenging activity method for some medicinal plants. The method allows us to evaluate substance’s antioxidant activity with almost the same results as a spectrophotometric assay. The developed DPPH• test was easy, fast, low cost and reliable, and can be used as a high-throughput assay for screening DPP-scavenging activity in herb medicines.

Development of a UPLC-MS/MS Method for Pharmacokinetic and Tissue Distribution of Isoeleutherin, Eleutherin, and Eleutherol in Bulbus eleutherinis in Rats

Guo, Peng-Cheng; Chen, Jie-Yu; Su, Jing; Raza, Faisal; Hao, Bin; Wu, Xin-Yi; Cheng, Yi-Qing; Qiu, Ming-Feng

This study established a novel UPLC-MS/MS method to determine the absolute oral bioavailability, and the tissue distribution profile of the active compounds (isoeleutherin, eleutherin and eleutherol) of bulbus eleutherinis with anti-coronary heart disease activity.

The method might help a better understanding of metabolites of the active components in the plant, and also provide a method reference for in vivo study of new drug preparations in the future.

Generating a Bispecific Antibody Drug Conjugate Targeting PRLR and HER2 with Improving the Internalization

Zong, Hui-Fang; Zhang, Bao-Hong; Zhu, Jian-Wei

Prolactin preceptor (PRLR) undergoes rapid internalization compared with HER2 antigen, and has crosstalk signaling with HER2 in breast cancer. This study constructed a BsADC targeting HER2 and PRLR conjugating MMAE as payloads to improve the efficacy of HER2 ADCs through enhancing the target specificity and internalization. The BsADC kept the affinity to two targeting antigens, showed a higher internalization efficiency compared with HER2 (V205C)-MMAE, and was demonstrated to have superior antitumor activity in vitro. BsADC, bispecific antibody drug conjugate.

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