Formulation and structural insight of biocompatible microemulsion for enhanced release profile of anticancer methotrexate

IF 2.6 4区 材料科学 Q3 MATERIALS SCIENCE, MULTIDISCIPLINARY
Muhammad Yasir Siddique, Sehrish Zafar, Linta Rizwan, Muhammad Atif Saleem, Sajjad Haider, Waqar Azeem, Kamran Alam, Yasir Iqbal, Sajjad Hussain Sumrra, Muhammad Faizan Nazar
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Abstract

Microemulsions (μEs) are particularly suitable systems for the efficient delivery of anticancer drugs due to their thermodynamic stability, structural flexibility, and patient-friendly chemotherapies. Moreover, μE formulations can efficiently encapsulate the anticancer drugs and deliver them to the desired location. Herein, three new Tween-60-based µE formulations were developed to enhance the dissolution profile of anticancer methotrexate (MTX). For this, μE formulations using an appropriate ratio of castor oil (∼9%), water (∼11%), and Tween-60 (∼40%) were used, while ethanol, 2-propanol, and 1-butanol were selected as co-surfactants for each formulation, respectively. Preliminarily, the phase compatibility of the μE ingredients, the average μE region, and the structural transformation in the microstructure of μE were delineated by mapping the pseudoternary phase diagram, as well as electrical conductivity, viscosity, and optical microscopic measurements. The size distribution profile of the as-formulated μEs analyzed by dynamic light scattering (DLS) revealed the fine monomodal assembly of MTX-μE nanodroplets (∼65 nm), which remained stable over a half year of storage. FTIR analysis showed good compatibility of MTX with μE ingredients with no apparent chemical interaction, while fluorescence measurements endorsed the acquisition of MTX in nonpolar microenvironments. Furthermore, an enhanced dissolution rate (&gt;98% ± 1.5%, p ≤ 0.001) and superior bioavailability of the lyophilized non-aggregated methotrexate nanoparticles (MTX-NPs) were achieved, making them a suitable formulation for oral administration.
增强抗癌药物甲氨蝶呤释放谱的生物相容性微乳液的配方与结构研究
微乳剂(μEs)因其热力学稳定性、结构灵活性和对患者友好的化疗方法,特别适用于高效输送抗癌药物。此外,μE 制剂还能有效地包裹抗癌药物并将其输送到所需的位置。在此,我们开发了三种基于吐温-60的新型μE制剂,以提高抗癌药物甲氨蝶呤(MTX)的溶解度。为此,我们使用了适当比例的蓖麻油(9%∼9%)、水(11%∼11%)和吐温-60(40%∼40%)作为μE制剂,并分别选择乙醇、2-丙醇和1-丁醇作为每种制剂的辅助表面活性剂。通过绘制伪三元相图、电导率、粘度和光学显微镜测量,初步确定了μE成分的相容性、平均μE区域和μE微观结构的结构转变。通过动态光散射(DLS)分析了配方μE的粒度分布曲线,发现MTX-μE纳米微滴(∼65 nm)呈细小的单模态组装,在储存半年后仍保持稳定。傅立叶变换红外光谱分析显示,MTX 与 μE 成分具有良好的兼容性,没有明显的化学作用,而荧光测量则证实了 MTX 在非极性微环境中的获得性。此外,冻干非聚合甲氨蝶呤纳米颗粒(MTX-NPs)的溶出率提高了(&gt;98% ± 1.5%,p ≤ 0.001),生物利用度也更高,是一种适合口服的制剂。
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来源期刊
Frontiers in Materials
Frontiers in Materials Materials Science-Materials Science (miscellaneous)
CiteScore
4.80
自引率
6.20%
发文量
749
审稿时长
12 weeks
期刊介绍: Frontiers in Materials is a high visibility journal publishing rigorously peer-reviewed research across the entire breadth of materials science and engineering. This interdisciplinary open-access journal is at the forefront of disseminating and communicating scientific knowledge and impactful discoveries to researchers across academia and industry, and the public worldwide. Founded upon a research community driven approach, this Journal provides a balanced and comprehensive offering of Specialty Sections, each of which has a dedicated Editorial Board of leading experts in the respective field.
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