Lipid-Conjugated Reduced Haloperidol in Association with Glucose-Based Nanospheres: A Strategy for Glioma Treatment DOI
Aasia Ansari, Tithi Bhattacharyya, Pritam Das

и другие.

Molecular Pharmaceutics, Год журнала: 2024, Номер unknown

Опубликована: Сен. 20, 2024

Aggressive glioma exhibits a poor survival rate. Increased tumor aggression is linked to both cells and tumor-associated macrophages (TAMs), which induce pro-aggression, invasion, metastasis. Imperatively, for effective treatment, it important target TAMs. Haloperidol, neuropsychotic drug, avidly targets the sigma receptor (SR), expressed in higher levels cell types. Herein, we present development of novel cationic lipid-conjugated reduced haloperidol (±RHPC8), aims mediate SR-targeted antiglioma effect. Hypothetically, ±RHPC8 would act simultaneously as an SR-targeting ligand anticancer agent. As blood-brain barrier (BBB) obstructs direct targeting situ glioma, used BBB-crossing glucose-based carbon nanospheres (CSPs) deliver within tumor-bearing mouse brain. The resultant ±RHPC8-CSP nanoconjugate targeted SR-expressing cells. In orthotopic subcutaneous models, prolonged regressed tumors compared other treated groups. Notably, was significantly taken up by TAMs thus resulting macrophage polarization from M2 M1, exhibited markedly expression immunosuppressive cytokines released TAMs, including TGF-β, IL-10, VEGF. conclusion, designed presented nanodrug delivery system brain cancer treatment.

Язык: Английский

Lipid-Conjugated Reduced Haloperidol in Association with Glucose-Based Nanospheres: A Strategy for Glioma Treatment DOI
Aasia Ansari, Tithi Bhattacharyya, Pritam Das

и другие.

Molecular Pharmaceutics, Год журнала: 2024, Номер unknown

Опубликована: Сен. 20, 2024

Aggressive glioma exhibits a poor survival rate. Increased tumor aggression is linked to both cells and tumor-associated macrophages (TAMs), which induce pro-aggression, invasion, metastasis. Imperatively, for effective treatment, it important target TAMs. Haloperidol, neuropsychotic drug, avidly targets the sigma receptor (SR), expressed in higher levels cell types. Herein, we present development of novel cationic lipid-conjugated reduced haloperidol (±RHPC8), aims mediate SR-targeted antiglioma effect. Hypothetically, ±RHPC8 would act simultaneously as an SR-targeting ligand anticancer agent. As blood-brain barrier (BBB) obstructs direct targeting situ glioma, used BBB-crossing glucose-based carbon nanospheres (CSPs) deliver within tumor-bearing mouse brain. The resultant ±RHPC8-CSP nanoconjugate targeted SR-expressing cells. In orthotopic subcutaneous models, prolonged regressed tumors compared other treated groups. Notably, was significantly taken up by TAMs thus resulting macrophage polarization from M2 M1, exhibited markedly expression immunosuppressive cytokines released TAMs, including TGF-β, IL-10, VEGF. conclusion, designed presented nanodrug delivery system brain cancer treatment.

Язык: Английский

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