A facile and universal method to achieve liposomal remote loading of non-ionizable drugs with outstanding safety profiles and therapeutic effect

Liposomes have made remarkable achievements as drug delivery vehicles in the clinic. Liposomal products mostly benefited from remote drug loading techniques that succeeded in amphipathic and/or ionizable drugs, but seemed impracticable for nonionizable and poorly water-soluble therapeutic agents, thereby impeding extensive promising drugs to hitchhike liposomal vehicles for disease therapy. In this study, a series of weak acid drug derivatives were designed by a simplistic one step synthesis, which could be remotely loaded into liposomes by pH gradient method. Cabazitaxel (CTX) weak acid derivatives were selected to evaluate regarding its safety profiles, pharmacodynamics, and pharmacokinetics. CTX weak acid derivative liposomes were superior to Jevtana® in terms of safety profiles, including systemic toxicity, hematological toxicity, and potential central nerve toxicity. Specifically, it was demonstrated that liposomes had capacity to weaken potential toxicity of CTX on cortex and hippocampus neurons. Significant advantages of CTX weak acid derivative-loaded liposomes were achieved in prostate cancer and metastatic cancer therapy resulting from higher safety and elevated tolerated doses.

A case of atypical cholesterol side chain defect possibly caused by CYP11A1 heterozygous mutation / 中华内分泌代谢杂志

This paper reports a case of atypical cholesterol side chain enzyme deficiency caused possibly by CYP11A1p.A359V heterozygous mutation. The patient was diagnosed as congenital adrenal hyperplasia because he was born with gonadal dysplasia and there were manifestations of salt losing and pigment changing, combined with high level of plasma ACTH. Further genetic screening revealed CYP11A1p.A359V heterozygous mutations in patients with a final diagnosis of cholesterol side chain enzyme deficiency which was treated effectively to glucocorticoid.

Advances in the relationship between peritoneal microenvironment and peritoneal me-tastasis in colorectal cancer / 中国肿瘤临床

Peritoneal metastasis is very common in colorectal cancer and often indicates bad prognosis. The peritoneum, which con-tains an abundant supply of blood and specific types of resident and migrating cells, lines the surface of the abdominal wall and covers the abdominal organs. The combination of cells, extracellular matrix, and local unique physicochemical composition of the abdominal cavity provide a complex and relatively stable peritoneal microenvironment. The cells in this environment can be induced by cancer cells to be involved in tumor growth, invasion, and peritoneal metastasis. This review summarizes the major cellular components in-volved in the peritoneal microenvironment.

Advances in the relationship between peritoneal microenvironment and peritoneal me-tastasis in colorectal cancer / 中国肿瘤临床

Peritoneal metastasis is very common in colorectal cancer and often indicates bad prognosis. The peritoneum, which con-tains an abundant supply of blood and specific types of resident and migrating cells, lines the surface of the abdominal wall and covers the abdominal organs. The combination of cells, extracellular matrix, and local unique physicochemical composition of the abdominal cavity provide a complex and relatively stable peritoneal microenvironment. The cells in this environment can be induced by cancer cells to be involved in tumor growth, invasion, and peritoneal metastasis. This review summarizes the major cellular components in-volved in the peritoneal microenvironment.