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新型辅酶 Q 纳米乳在婴儿配方食品中的应用:特性与生物利用度

Characterization and bioavailability of a novel coenzyme Q nanoemulsion used as an infant formula supplement.

机构信息

Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Departamento de Tecnología Farmacéutica, Buenos Aires, Argentina; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Instituto de Tecnología Farmacéutica y Biofarmacia (InTecFyB), Buenos Aires, Argentina.

Universidad de Buenos Aires, Facultad de Ciencias Exactas y Naturales, Departamento de Industrias-ITAPROQ, Buenos Aires, Argentina; Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), Argentina.

出版信息

Int J Pharm. 2023 Mar 5;634:122656. doi: 10.1016/j.ijpharm.2023.122656. Epub 2023 Jan 27.

Abstract

Supplementation with Coenzyme Q (CoQ), in patients with its deficiency, has greater odds of success if the treatment is carried out early with an appropriate formulation. For neonatal CoQ deficiency, infant formula supplementation could be an attractive option. However, solid CoQ cannot be solubilized or dispersed in milk matrix leading to an inefficient CoQ dosage and poor intestinal absorption. We developed and characterized a high-dose CoQ oil-in-water (O/W) nanoemulsion suitable to supplement infant formula without modifying its organoleptic characteristics. CoQ powder and soy lecithin were solubilized in an oil phase consisted of Labrasol® and Labrafac. The aqueous phase was Tween 80, TPGS, methylparaben and propylparaben. O/W nanoemulsion was prepared by adding dropwise the oil phase to the aqueous phase under stirring to a final concentration of CoQ 9.5 % w/w followed by ultrasonic homogenization. Pharmacotechnical parameters were determined. This formulation resulted to be easily to be dispersed in milk matrix, stable for at least 90 days, with no cytotoxicity in in vitro assays, and higher bioavailability than CoQ powder. CoQ nanoemulsion supplementation in the infant formula facilitates the individualized administration for the child with accurate dosage, overcome swallowing difficulties and in turn could increase the treatment adherence and efficacy.

摘要

在缺乏辅酶 Q(CoQ)的患者中,如果早期使用适当的配方进行治疗,补充 CoQ 成功的几率更大。对于新生儿 CoQ 缺乏症,婴儿配方奶粉的补充可能是一个有吸引力的选择。然而,固体 CoQ 不能溶解或分散在牛奶基质中,导致 CoQ 剂量效率低下和肠道吸收不良。我们开发并表征了一种高剂量 CoQ 油包水(O/W)纳米乳剂,适用于补充婴儿配方奶粉而不改变其感官特性。CoQ 粉末和大豆卵磷脂溶解在由 Labrasol®和 Labrafac 组成的油相中。水相为吐温 80、TPGS、对羟基苯甲酸甲酯和对羟基苯甲酸丙酯。O/W 纳米乳剂通过将油相逐滴加入搅拌的水相中制备,最终 CoQ 浓度为 9.5%w/w,然后进行超声匀化。确定了药剂学参数。该制剂易于分散在牛奶基质中,至少稳定 90 天,体外试验无细胞毒性,生物利用度高于 CoQ 粉末。CoQ 纳米乳剂在婴儿配方奶粉中的补充便于对儿童进行个体化给药,剂量准确,克服了吞咽困难,从而提高了治疗的依从性和疗效。

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