Pardo-Figuerez Maria, Teno Jorge, Lafraya Alvaro, Prieto Cristina, Lagaron Jose Maria
Novel Materials and Nanotechnology Group, Institute of Agrochemistry and Food Technology (IATA), Spanish Council for Scientific Research (CSIC), Calle Catedrático Agustín Escardino Benlloch 7, Paterna, 46980 Valencia, Spain.
R&D Department, Bioinicia S.L., Calle Algepser 65 nave 3, Paterna, 46980 Valencia, Spain.
Nanomaterials (Basel). 2022 Jan 27;12(3):438. doi: 10.3390/nano12030438.
The work herein presented aims to develop and characterize carvedilol (CVD) releasable non-water-soluble monolayers and a multilayer patch made of ultrathin micron and submicron fibers for drug delivery into the sublingual mucosa. Firstly, the developed formulations containing CVD within different biopolymers (PDLA, PCL, and PHB) were characterized by scanning electron microscopy (SEM), attenuated total reflectance Fourier transformed infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC), wide-angle X-ray scattering (WAXS), and for their in vitro drug release. SEM micrographs assessed the fiber morphology attained by adding carvedilol. ATR-FTIR spectra revealed good chemical compatibility between CVD and the tested biopolymers, whereas DSC and WAXS confirmed that CVD was in an amorphous state within the biopolymeric fibers. In vitro release studies showed enhanced CVD release kinetics from the electrospun biopolymer monolayers compared to the dissolution rate of the commercial form of the pure drug, except for the slow-releasing PDLA fibers. Finally, the selected CVD-loaded layer, i.e., electrospun PHB, was built into a three-layer patch to tackle mucosa adhesion and unidirectional release, while retaining the enhanced release kinetics. The patch design proposed here further demonstrates the potential of the electro-hydrodynamic processing technology to render unique mucoadhesive controlled delivery platforms for poorly water-soluble drugs.
本文所展示的工作旨在开发并表征可释放卡维地洛(CVD)的非水溶性单层以及由超薄微米和亚微米纤维制成的多层贴片,用于将药物递送至舌下黏膜。首先,通过扫描电子显微镜(SEM)、衰减全反射傅里叶变换红外光谱(ATR-FTIR)、差示扫描量热法(DSC)、广角X射线散射(WAXS)对含有不同生物聚合物(聚-D-乳酸(PDLA)、聚己内酯(PCL)和聚羟基丁酸酯(PHB))的CVD制剂进行表征,并对其体外药物释放进行研究。SEM显微照片评估了添加卡维地洛后获得的纤维形态。ATR-FTIR光谱显示CVD与测试的生物聚合物之间具有良好的化学相容性,而DSC和WAXS证实CVD在生物聚合物纤维中处于无定形状态。体外释放研究表明,与纯药物商业形式的溶解速率相比,电纺生物聚合物单层的CVD释放动力学增强,但缓慢释放的PDLA纤维除外。最后,将选定的负载CVD的层,即电纺PHB,制成三层贴片,以解决黏膜粘附和单向释放问题,同时保持增强的释放动力学。此处提出的贴片设计进一步证明了电流体动力学加工技术在为难溶性药物提供独特的粘膜粘附控释平台方面的潜力。