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负载姜黄素类化合物的纳米结构脂质载体:物理化学表征、体外释放、离体皮肤渗透、稳定性及抗氧化活性

Nanostructured lipid carriers loaded with curcuminoids: Physicochemical characterization, in vitro release, ex vivo skin penetration, stability and antioxidant activity.

作者信息

Espinosa-Olivares M A, Delgado-Buenrostro N L, Chirino Y I, Trejo-Márquez M A, Pascual-Bustamante S, Ganem-Rondero A

机构信息

División de Estudios de Posgrado (Tecnología Farmacéutica), Facultad de Estudios Superiores Cuautitlán, Universidad Nacional Autónoma de México, Av. 1o de Mayo s/n, Cuautitlán Izcalli, C.P. 54740, Estado de México, Mexico.

Laboratorio 10, Unidad de Biomedicina, Facultad de Estudios Superiores Iztacala, Universidad Nacional Autónoma de México, Avenida de los Barrios Número 1, Colonia Los Reyes Iztacala, Tlalnepantla, C.P. 54090, Estado de México, Mexico.

出版信息

Eur J Pharm Sci. 2020 Dec 1;155:105533. doi: 10.1016/j.ejps.2020.105533. Epub 2020 Aug 29.


DOI:10.1016/j.ejps.2020.105533
PMID:32871214
Abstract

Four formulations of nanostructured lipid carriers (NLC) loaded with curcuminoids where prepared, testing two types of solid lipids (Compritol® 888 ATO and Precirol® ATO 5) and two kinds of stabilizers (poloxamer 407 and polysorbate 80). Particle size values between 111 and 214 nm and polydispersity indices < 0.3 were registered, with low Z potential values due to the nonionic character of the stabilizers. The results showed that the type of surfactant had an impact on the in vitro release rate and on the ex vivo skin permeation capability of curcuminoids. Polysorbate 80 delayed the release, but favors the transport of a higher amount of curcuminoids to the receptor solution during the ex vivo permeation studies than the systems with poloxamer 407. Confocal microscopy confirmed that all systems favored the penetration of curcuminoids to deeper layers of the skin and in a greater amount than curcuminoids in solution. Exposure of the systems to intense radiation caused the degradation of curcuminoids, without loss of antioxidant activity, confirming that the degradation products also function as antioxidants. The NLC prepared can be valuable carriers to enhance the penetration of curcuminoids into the skin, to treat different disorders and skin diseases.

摘要

制备了四种负载姜黄素类化合物的纳米结构脂质载体(NLC)制剂,测试了两种类型的固体脂质(Compritol® 888 ATO和Precirol® ATO 5)以及两种稳定剂(泊洛沙姆407和聚山梨酯80)。记录到粒径值在111至214纳米之间,多分散指数<0.3,由于稳定剂的非离子特性,Z电位值较低。结果表明,表面活性剂的类型对姜黄素类化合物的体外释放速率和离体皮肤渗透能力有影响。聚山梨酯80延迟了释放,但在离体渗透研究中,与含有泊洛沙姆407的体系相比,它有利于将更多量的姜黄素类化合物转运到受体溶液中。共聚焦显微镜证实,所有体系都有利于姜黄素类化合物渗透到皮肤更深层,且比溶液中的姜黄素类化合物渗透量更大。将这些体系暴露于强辐射下会导致姜黄素类化合物降解,但不会丧失抗氧化活性,这证实了降解产物也具有抗氧化作用。所制备的NLC可成为增强姜黄素类化合物渗透到皮肤中以治疗不同病症和皮肤疾病的有价值载体。

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