Anandamide-nanoformulation obtained by electrospraying for cardiovascular therapy

Area of Science:

• Pharmacology
• Nanotechnology
• Cardiovascular Medicine

Background:

• Anandamide (AEA), an endogenous cannabinoid, possesses antihypertensive properties but faces limitations due to poor physicochemical characteristics and potential psychoactive effects.
• Drug encapsulation in nanocarriers presents a viable strategy to overcome AEA's administration challenges and enhance its therapeutic efficacy.
• The cardioprotective role of AEA remains underexplored, necessitating innovative delivery systems.

Purpose of the Study:

• To encapsulate AEA into poly-ε-caprolactone/Pluronic® F127 nanoparticles (AEA/PCL/PF127 NPs) using electrospraying.
• To characterize the physicochemical properties, cytocompatibility, and in vitro release of AEA from the nanoparticles.
• To evaluate the efficacy of AEA/PCL/PF127 NPs in an in vivo model of hypertension-induced cardiovascular remodeling.

Main Methods:

• AEA was encapsulated in PCL/PF127 nanoparticles via electrospraying.
• Nanoparticles were characterized for morphology, size, polydispersity, Z-potential, hydrophilicity, thermal, and spectroscopic properties.
• In vivo studies involved treating normotensive (WKY) and hypertensive (SHR) rats with AEA/PCL/PF127 NPs, monitoring hemodynamic, structural, functional, and inflammatory parameters.

Main Results:

• AEA/PCL/PF127 NPs exhibited suitable physicochemical properties and adequate cytocompatibility.
• Encapsulation and loading efficiencies, along with in vitro AEA release, were analyzed.
• Treatment with AEA/PCL/PF127 NPs significantly reversed all altered cardiovascular markers and parameters in hypertensive rats (SHR).

Conclusions:

• Electrosprayed nanoformulated AEA (AEA/PCL/PF127 NPs) demonstrates significant efficacy in treating hypertension.
• This nanoformulation effectively reverses cardiovascular remodeling associated with hypertension.
• Nanoencapsulation of AEA offers a promising therapeutic approach for managing hypertension and its related cardiovascular complications.