The Journal of pharmacy and pharmacology · 2026
Design and optimization of carvedilol-loaded transbilosomes for the control of diabetic high-fat diet-induced atherosclerosis in rats.
СтатьяНазвание и аннотация: Перевод в очереди
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Nagib Marwa M, Haider Ala Hussain, Fouad Amr Gamal, Khalil Sherif Faysal Abdelfattah, Belal Amany, Baali Fahad H, Albezrah Nisreen Khalid Aref, Ismail Alaa, Abo El-Ela Fatma I
Аннотация
OBJECTIVES: Carvedilol (CDL) is an oral beta-adrenergic blocker known for enhancing arterial blood flow and reducing hyperglycemia due to its antioxidant properties. However, CDL's short half-life leads to its low efficacy and poor bioavailability. This study aimed to develop a nasal spray of CDL-loaded transbilosomes (CTB) to improve CDL's sustainability, bioavailability, targeting, and effectiveness in controlling atherosclerosis in rats.
METHODS: Various CTB formulations were created using a Box-Behnken design to examine the effects of phospholipid, Span 60, and sodium deoxycholate (SDC) levels. In vivo evaluation of this optimal CTB formulation in a rat model of experimental diabetic high-fat diet-induced atherosclerosis was conducted.
KEY FINDINGS: The formulation containing 274.33 mg of phospholipid, 26.67 mg of Span 60, and 22.45 mg of SDC was identified as the optimal formulation. When compared with free CDL, the optimal CTB formulation enhanced sustainability, bioavailability, and targeting of CDL by 72.43%, 7.43-fold, and 7.55-fold, respectively. The nasal CTB group showed significant reductions in blood levels of glucose, triglycerides, cholesterol, and LDL, while increasing HDL and survival rates compared with the disease group. A histopathological study confirmed the efficacy of the nasal CTB spray.
CONCLUSION: The nasal CTB spray could be a potential therapy in controlling atherosclerosis in rats.
METHODS: Various CTB formulations were created using a Box-Behnken design to examine the effects of phospholipid, Span 60, and sodium deoxycholate (SDC) levels. In vivo evaluation of this optimal CTB formulation in a rat model of experimental diabetic high-fat diet-induced atherosclerosis was conducted.
KEY FINDINGS: The formulation containing 274.33 mg of phospholipid, 26.67 mg of Span 60, and 22.45 mg of SDC was identified as the optimal formulation. When compared with free CDL, the optimal CTB formulation enhanced sustainability, bioavailability, and targeting of CDL by 72.43%, 7.43-fold, and 7.55-fold, respectively. The nasal CTB group showed significant reductions in blood levels of glucose, triglycerides, cholesterol, and LDL, while increasing HDL and survival rates compared with the disease group. A histopathological study confirmed the efficacy of the nasal CTB spray.
CONCLUSION: The nasal CTB spray could be a potential therapy in controlling atherosclerosis in rats.