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在基于植物三醇的纳米颗粒中,生理中性 pH 值驱动逐渐的层状到反向立方到反向六方相转变。

Physiological neutral pH drives a gradual lamellar-to-reverse cubic-to-reverse hexagonal phase transition in phytantriol-based nanoparticles.

机构信息

Institute of Chemistry, University of Campinas (UNICAMP), P.O. Box 6154, Campinas, SP, 13084-970, Brazil.

Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, RS, 91501-970, Brazil.

出版信息

Colloids Surf B Biointerfaces. 2019 May 1;177:204-210. doi: 10.1016/j.colsurfb.2019.01.055. Epub 2019 Jan 31.

DOI:10.1016/j.colsurfb.2019.01.055
PMID:30743067
Abstract

Dispersed systems of bicontinuous cubic phases, called cubosomes, show a drug release rate faster than those obtained using other liquid-crystalline phases. To minimize side effects associated with the accelerated release of incorporated drugs, compounds may be added in the dispersions to produce systems of slow initial release and then fast release only in the desired action region. This paper addresses the addition of 10.0% (w/w) of decyl betainate chloride (DBC), a cleavable surfactant, into phytantriol/Pluronic-based dispersions to generate lamellar-to-cubic-to-hexagonal phase transitions. Small-angle X-ray scattering (SAXS) was used to analyze the mesophases obtained with the addition of DBC and pH variation. Transmission electron microscopy (TEM) images confirmed the presence of niosomes after the addition of DBC. The niosomes formed in these systems are pH-responsive with lamellar-to-hexosomes transitions at pH ≥ 7.4. The system investigated herein is gastro-resistant presenting potential therapeutic role for controlled release of drugs in neutral or alkaline environments of the organism.

摘要

分散的双连续立方相体系,称为立方脂质体,其药物释放速度比其他液晶相体系更快。为了最大限度地减少与掺入药物加速释放相关的副作用,可以在分散体中添加化合物,以产生初始缓慢释放的系统,然后仅在所需作用区域快速释放。本文研究了在植物三醇/泊洛沙姆为基础的分散体中添加 10.0%(w/w)的十二烷基甜菜碱盐酸盐(DBC),一种可裂解的表面活性剂,以生成层状到立方到六方相转变。小角 X 射线散射(SAXS)用于分析添加 DBC 和 pH 值变化后获得的中间相。透射电子显微镜(TEM)图像证实了添加 DBC 后存在囊泡。在这些体系中形成的囊泡对 pH 具有响应性,在 pH≥7.4 时发生层状到六面体的转变。本文研究的系统具有胃耐抗性,在机体的中性或碱性环境中具有控制药物释放的潜在治疗作用。

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