Gieroba Barbara, Kalisz Grzegorz, Sroka-Bartnicka Anna, Płazińska Anita, Płaziński Wojciech, Starek Małgorzata, Dąbrowska Monika
Department of Biopharmacy, Medical University of Lublin, ul. Chodzki 4a, 20-093 Lublin, Poland.
Department of Genetics and Microbiology, Institute of Microbiology and Biotechnology, Maria Curie-Skłodowska University, ul. Akademicka 19, 20-033 Lublin, Poland.
Int J Mol Sci. 2021 May 15;22(10):5238. doi: 10.3390/ijms22105238.
The formation of cefuroxime axetil+cyclodextrin (CA+CD) complexes increases the aqueous solubility of CA, improves its physico-chemical properties, and facilitates a biomembrane-mediated drug delivery process. In CD-based tablet formulations, it is crucial to investigate the molecular details of complexes in final pharmaceutical preparation. In this study, Raman spectroscopy and mapping were applied for the detection and identification of chemical groups involved in α-, β-, γ-, and 2-hydroxypropyl-β-CD (2-HP- β-CD)+CA complexation process. The experimental studies have been complemented by molecular dynamics-based investigations, providing additional molecular details of CA+CD interactions. It has been demonstrated that CA forms the guest-host type inclusion complexes with all studied CDs; however, the nature of the interactions is slightly different. It seems that both α- and β-CD interact with furanyl and methoxy moieties of CA, γ-CD forms a more diverse pattern of interactions with CA, which are not observed in other CDs, whereas 2HP-β-CD binds CA with the contribution of hydrogen bonding. Apart from supporting this interpretation of the experimental data, molecular dynamics simulations allowed for ordering the CA+CD binding affinities. The obtained results proved that the molecular details of the host-guest complexation can be successfully predicted from the combination of Raman spectroscopy and molecular modeling.
头孢呋辛酯+环糊精(CA+CD)复合物的形成提高了CA的水溶性,改善了其理化性质,并促进了生物膜介导的药物递送过程。在基于环糊精的片剂配方中,研究最终药物制剂中复合物的分子细节至关重要。在本研究中,拉曼光谱和成像技术被用于检测和识别参与α-、β-、γ-和2-羟丙基-β-环糊精(2-HP-β-CD)+CA络合过程的化学基团。实验研究得到了基于分子动力学的研究的补充,提供了CA+CD相互作用的更多分子细节。结果表明,CA与所有研究的环糊精形成客体-主体型包合物;然而,相互作用的性质略有不同。似乎α-和β-环糊精都与CA的呋喃基和甲氧基部分相互作用,γ-环糊精与CA形成了一种在其他环糊精中未观察到的更多样化的相互作用模式,而2HP-β-CD通过氢键作用与CA结合。除了支持对实验数据的这种解释外,分子动力学模拟还可以对CA+CD的结合亲和力进行排序。所得结果证明,通过拉曼光谱和分子建模的结合,可以成功预测客体-主体络合的分子细节。