Hajba-Horváth Eszter, Biró Emese, Mirankó Mirella, Fodor-Kardos Andrea, Trif László, Feczkó Tivadar
Research Institute of Biomolecular and Chemical Engineering, Faculty of Engineering, University of Pannonia Egyetem u. 10. H-8200 Veszprém Hungary
Institute of Materials and Environmental Chemistry, Research Centre for Natural Sciences Magyar Tudósok Körútja 2. H-1117 Budapest Hungary
RSC Adv. 2020 Dec 9;10(72):43915-43926. doi: 10.1039/d0ra07218d.
Valsartan is an antihypertensive drug used primarily orally, however, due to its hydrophobic nature it has got low bio-availability thus requiring higher dosage/frequency and causing more side effects. The aim of our work was to prepare valsartan-loaded nanoparticles by using ethyl cellulose and poly(methyl methacrylate) polymers which can be administered orally and to investigate the preparation conditions and their significance as potential drug carriers for valsartan delivery by release studies. Ethyl cellulose and poly(methyl methacrylate) polymers were used for the preparation of nanoparticles by single emulsion-solvent evaporation technique. The formation of drug-loaded nanoparticles was designed by experimental design for size and encapsulation efficiency, in addition the prepared nanosuspensions were nano spray dried in order to gain a powder form that is easy to handle and store. Both of the nano spray dried formulations had an amorphous structure in contrast to the pure drug according to differential scanning calorimetry and X-ray diffraction analysis, which can be advantageous in drug absorption. The originally processed ethyl cellulose-valsartan nanoparticles increased the solubility of the drug in the model intestinal medium, while poly(methyl methacrylate)-valsartan nanoparticles enabled substantially prolonged drug release. The release kinetics of both types of nanoparticles could be described by the Weibull model.
缬沙坦是一种主要口服的抗高血压药物，然而，由于其疏水性，它的生物利用度较低，因此需要更高的剂量/给药频率，并会引起更多副作用。我们工作的目的是使用乙基纤维素和聚甲基丙烯酸甲酯聚合物制备可口服的载缬沙坦纳米颗粒，并通过释放研究来研究制备条件及其作为缬沙坦递送潜在药物载体的意义。采用单乳液溶剂蒸发技术，使用乙基纤维素和聚甲基丙烯酸甲酯聚合物制备纳米颗粒。通过实验设计来确定载药纳米颗粒的粒径和包封率，此外，将制备的纳米混悬液进行纳米喷雾干燥，以获得易于处理和储存的粉末形式。根据差示扫描量热法和X射线衍射分析，与纯药物相比，两种纳米喷雾干燥制剂均具有无定形结构，这在药物吸收方面可能具有优势。最初制备的乙基纤维素-缬沙坦纳米颗粒增加了药物在模拟肠道介质中的溶解度，而聚甲基丙烯酸甲酯-缬沙坦纳米颗粒能够显著延长药物释放。两种类型纳米颗粒的释放动力学均可用威布尔模型描述。
