Dragar Črt, Roškar Robert, Kocbek Petra
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ljubljana, SI-1000 Ljubljana, Slovenia.
Department of Biopharmaceutics and Pharmacokinetics, Faculty of Pharmacy, University of Ljubljana, SI-1000 Ljubljana, Slovenia.
Nanomaterials (Basel). 2024 May 28;14(11):949. doi: 10.3390/nano14110949.
Hydrophilic nanofibers offer promising potential for the delivery of drugs with diverse characteristics. Yet, the effects of different drugs incorporated into these nanofibers on their properties remain poorly understood. In this study, we systematically explored how model drugs, namely ibuprofen, carvedilol, paracetamol, and metformin (hydrochloride), affect hydrophilic nanofibers composed of polyethylene oxide and poloxamer 188 in a 1:1 weight ratio. Our findings reveal that the drug affects the conductivity and viscosity of the polymer solution for electrospinning, leading to distinct changes in the morphology of electrospun products. Specifically, drugs with low solubility in ethanol, the chosen solvent for polymer solution preparation, led to the formation of continuous nanofibers with uniform diameters. Additionally, the lower solubility of metformin in ethanol resulted in particle appearance on the nanofiber surface. Furthermore, the incorporation of more hydrophilic drugs increased the surface hydrophilicity of nanofiber mats. However, variations in the physicochemical properties of the drugs did not affect the drug loading and drug entrapment efficiency. Our research also shows that drug properties do not notably affect the immediate release of drugs from nanofibers, highlighting the dominant role of the hydrophilic polymers used. This study emphasizes the importance of considering specific drug properties, such as solubility, hydrophilicity, and compatibility with the solvent used for electrospinning, when designing hydrophilic nanofibers for drug delivery. Such considerations are crucial for optimizing the properties of the drug delivery system, which is essential for achieving therapeutic efficacy and safety.
亲水性纳米纤维在递送具有不同特性的药物方面具有广阔的潜力。然而，将不同药物掺入这些纳米纤维中对其性能的影响仍知之甚少。在本研究中，我们系统地探究了模型药物，即布洛芬、卡维地洛、对乙酰氨基酚和二甲双胍（盐酸盐），如何影响由聚环氧乙烷和泊洛沙姆188按1:1重量比组成的亲水性纳米纤维。我们的研究结果表明，药物会影响用于静电纺丝的聚合物溶液的电导率和粘度，从而导致静电纺丝产品的形态发生明显变化。具体而言，在用于制备聚合物溶液的所选溶剂乙醇中溶解度低的药物，会导致形成直径均匀的连续纳米纤维。此外，二甲双胍在乙醇中的较低溶解度导致纳米纤维表面出现颗粒。此外，掺入更多亲水性药物会增加纳米纤维垫的表面亲水性。然而，药物理化性质的变化并未影响载药量和药物包封率。我们的研究还表明，药物性质对纳米纤维中药物的即时释放没有显著影响，突出了所用亲水性聚合物的主导作用。本研究强调了在设计用于药物递送的亲水性纳米纤维时，考虑特定药物性质（如溶解度、亲水性以及与用于静电纺丝的溶剂的相容性）的重要性。这些考虑对于优化药物递送系统的性能至关重要，而这对于实现治疗效果和安全性至关重要。
