Instituto de Química, Universidade Federal do Rio Grande do Norte, Campus Universitário Lagoa Nova, 59072-970 Natal, Rio Grande do Norte, Brasil.
Langmuir. 2020 Sep 1;36(34):10251-10269. doi: 10.1021/acs.langmuir.0c01834. Epub 2020 Aug 18.
Despite having good efficacy in the treatment and prevention of tuberculosis, the administration of rifampicin (RIF) can cause serious side effects, resulting from the prolonged use of this substance. Thus, it is necessary to seek new systems for administering tuberculostatic drugs, to avoid unwanted adverse effects, increase their bioavailability and, consequently, improve their therapeutic efficacy. The present work describes the achievement of a pH-responsive system for RIF, using palygorskite, a fibrous clay mineral, as a nanocarrier. To evaluate the influence of some operational variables on the drug adsorption process, a 2 factorial experimental design was used. The experiment using a maximum concentration (0.125 mg/mL), lower mass of PAL (300 mg), and lower pH (pH 2) was more efficient compared to other experiments, resulting in a higher dose of the incorporated drug, equivalent to 33.62 mg/g. To elucidate the mechanism of interaction between the materials, the hybrid obtained was characterized by different characterization techniques (Fourier transform infrared spectroscopy, X-ray diffraction, thermogravimetry/derived thermogravimetry, zeta potential, scanning electron microscopy, and dispersive energy spectroscopy). In addition, kinetic models and adsorption isotherms were applied to the experimental data. Through release studies, it was possible to verify the effectiveness of the pH-dependent system obtained. The adjustment of experimental release data to the theoretical model of Higuchi indicated that the release of rifampicin occurs in a prolonged way from the palygorskite.
尽管利福平(RIF)在结核病的治疗和预防方面具有良好的疗效,但由于该物质的长期使用,会导致严重的副作用。因此,有必要寻找新的抗结核药物给药系统,以避免不必要的不良反应,提高其生物利用度,从而提高其治疗效果。本工作描述了使用凹凸棒石作为纳米载体来实现利福平的 pH 响应系统。为了评估一些操作变量对药物吸附过程的影响,使用了 2 因素实验设计。与其他实验相比,使用最大浓度(0.125mg/mL)、较低 PAL 质量(300mg)和较低 pH(pH2)的实验更有效,导致更高剂量的药物被包封,相当于 33.62mg/g。为了阐明材料之间的相互作用机制,对获得的杂化材料进行了不同的表征技术(傅里叶变换红外光谱、X 射线衍射、热重分析/衍生热重分析、动电位、扫描电子显微镜和能量色散光谱)。此外,还对实验数据进行了动力学模型和吸附等温线拟合。通过释放研究,验证了所获得的 pH 依赖性系统的有效性。将释放实验数据调整到 Higuchi 的理论模型表明,利福平的释放是从凹凸棒石中缓慢进行的。