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载维生素 K1 的脂质核纳米胶囊:理化性质表征和体外皮肤渗透。

Vitamin K1-loaded lipid-core nanocapsules: physicochemical characterization and in vitro skin permeation.

机构信息

Postgraduate Program in Pharmaceutical Sciences, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.

出版信息

Skin Res Technol. 2013 Feb;19(1):e223-30. doi: 10.1111/j.1600-0846.2012.00631.x. Epub 2012 Jun 7.

Abstract

BACKGROUND

The incorporation of substances in nanocarriers can modulate and/or manage their delivery profiles (immediate or sustained) and permeation through skin. Consequently, drug nanencapsulation intended for topical treatment can reduce the systemic absorption of the substance.

OBJECTIVE

To obtain and characterize vitamin K1-loaded lipid core nanocapsules as well as to determine whether the nanoencapsulation influences the skin permeation of this vitamin.

METHODS

The skin permeation study was performed by means of Franz-type diffusion cells followed by the tape stripping and retention techniques. The vitamin K1-loaded lipid core nanocapsules were obtained by the preformed polymer precipitation method and the particles were characterized.

RESULTS

The nanocapsules presented average diameter of 211 ± 2 nm, pH of 5.7 ± 0.3, zeta potential of -14.9 ± 0.6 mV and drug content of 10.2 mg/mL (102.1%). The physical stability of the nanocapsule suspension was verified using multiple light backscattering analysis. The amount of vitamin K1 in the dermis after 8 h of drug permeation was higher when the nanocapsules were applied compared to the control. Moreover, retention in the outermost skin layer and a decrease in the skin permeation to the receptor compartment due to the nanoencapsulation were observed.

CONCLUSION

Thus, nanoencapsulation can lead to the selective permeation of vitamin K1 through the skin.

摘要

背景

纳米载体中物质的掺入可以调节和/或控制其输送特性(即时或持续)和透过皮肤的能力。因此,用于局部治疗的药物纳米封装可以减少物质的全身吸收。

目的

获得并表征载有维生素 K1 的脂质核纳米胶囊,并确定纳米封装是否会影响这种维生素的皮肤渗透。

方法

通过Franz 型扩散池进行皮肤渗透研究,然后采用胶带剥离和保留技术。载有维生素 K1 的脂质核纳米胶囊通过预形成的聚合物沉淀法获得,并对颗粒进行了表征。

结果

纳米胶囊的平均直径为 211 ± 2nm,pH 值为 5.7 ± 0.3,zeta 电位为-14.9 ± 0.6mV,药物含量为 10.2mg/mL(102.1%)。使用多重光背散射分析验证了纳米胶囊悬浮液的物理稳定性。与对照组相比,纳米胶囊给药 8 小时后,真皮中维生素 K1 的含量更高。此外,由于纳米封装,观察到最外层皮肤层中的保留和皮肤渗透到受体腔室的减少。

结论

因此,纳米封装可以导致维生素 K1 通过皮肤的选择性渗透。

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