The sesquiterpene β-caryophyllene (BCP) is a structurally singular cannabinoid and a selective agonist of the CB2 receptor, which in addition to being expressed in the CNS, is intrinsically expressed within the immune system and lacks psychoactivity. Nanoencapsulation of BCP can allow its controlled release into the CNS and intranasal administration. Thus, a protocol for nanoencapsulation of BCP was developed and optimized in order to adjust the desired bioactive content and physicochemical parameters. The formulation was assessed regarding nanoparticle size, zeta potential, morphology, pH, osmolarity, stability, and drug release kinetics in vitro. The final composition of the BCP nanoparticles presented in its organic phase (OP) Tween 20 (0.25%), BCP (0.1%), and PEG 400 (5%); and in its aqueous phase (AP) ultrapure water and poloxamer P188 (0.25%). The formulation showed to be suitable for intranasal administration, presenting pH 6.5 and osmolarity of 150 mmol/kg. The mean particle diameter was 147.2 nm, PDI 0.052, and zeta potential of −24.5. The accelerated stability test showed that nanoparticles were stable for up to 1 month, when reversible creaming effect occurred. Besides, it was noted a low rate of particle accumulation and particle size distribution remained unchanged. BCP nanoparticles were shown to be promptly released in physiological medium (up to 60 min). In this work, a formulation containing β-caryophyllene nanoparticles suitable for physiological administration and preclinical tests was successfully developed.

倍半萜烯β-石竹烯（BCP）是结构上单一的大麻素和CB2受体的选择性激动剂，除了在CNS中表达外，它在免疫系统中也固有表达并且缺乏精神活性。BCP的纳米囊封可以使其受控释放到CNS和鼻内给药。因此，开发并优化了用于BCP纳米封装的方案，以调节所需的生物活性含量和理化参数。在纳米颗粒尺寸，ζ电势，形态，pH，摩尔渗透压浓度，稳定性和体外药物释放动力学方面评估制剂。BCP纳米颗粒的最终组成以有机相（OP）Tween 20（0.25％），BCP（0.1％）和PEG 400（5％）表示；以及在其水相（AP）中的超纯水和泊洛沙姆P188（0。25％）。该制剂显示适用于鼻内给药，pH 6.5，渗透压为150 mmol / kg。平均粒径为147.2nm，PDI为0.052，ζ电位为-24.5。加速稳定性测试表明，当发生可逆的乳脂效应时，纳米粒子可稳定长达1个月。此外，注意到低的颗粒积累速率和粒度分布保持不变。已证明BCP纳米颗粒可在生理介质中迅速释放（长达60分钟）。在这项工作中，成功开发了一种包含适用于生理学给药和临床前测试的β-叶绿素纳米颗粒的制剂。PDI 0.052，ζ电位为-24.5。加速稳定性测试表明，当发生可逆的乳脂作用时，纳米粒子可稳定长达1个月。此外，注意到低的颗粒积累速率和粒度分布保持不变。已证明BCP纳米颗粒可在生理介质中迅速释放（长达60分钟）。在这项工作中，成功开发了一种包含适用于生理学给药和临床前测试的β-叶绿素纳米颗粒的制剂。PDI 0.052，ζ电位为-24.5。加速稳定性测试表明，当发生可逆的乳脂效应时，纳米粒子可稳定长达1个月。此外，注意到低的颗粒积累速率和粒度分布保持不变。已证明BCP纳米颗粒可在生理介质中迅速释放（长达60分钟）。在这项工作中，成功开发了一种包含适用于生理学给药和临床前测试的β-叶绿素纳米颗粒的制剂。已证明BCP纳米颗粒可在生理介质中迅速释放（长达60分钟）。在这项工作中，成功开发了一种包含适用于生理学给药和临床前测试的β-叶绿素纳米颗粒的制剂。已证明BCP纳米颗粒可在生理介质中迅速释放（长达60分钟）。在这项工作中，成功开发了一种包含适用于生理学给药和临床前测试的β-叶绿素纳米颗粒的制剂。