Tommasini S, Calabrò M L, Stancanelli R, Donato P, Costa C, Catania S, Villari V, Ficarra P, Ficarra R
Dipartimento Farmaco-Chimico, Facoltà di Farmacia, Università di Messina, Viale Annunziata, 98168 Messina, Italy.
J Pharm Biomed Anal. 2005 Sep 15;39(3-4):572-80. doi: 10.1016/j.jpba.2005.05.009.
The effect of (2-hydroxypropyl)-beta-cyclodextrin (HP-beta-CyD) on the solubility properties and spectroscopic features of hesperetin and its 7-rhamnoglucoside, hesperidin, was qualitatively and quantitatively investigated in water, by means of UV-vis absorption and fluorescence spectroscopy. The stoichiometric ratios and stability constants describing the extent of formation of the complexes have been determined by phase-solubility measurements; in both cases type-A(L) diagrams have been obtained (soluble 1:1 complexes). The higher degree of interaction showed by hesperetin may be attributed to the higher hydrophobicity and smaller size of the aglycone molecule, which therefore exhibits a greater affinity for the CyD and fits better into the cavity. The effect of molecular encapsulation on the two flavanones antioxidant activity was afterwards evaluated by means of different biological assays, concerned to the different mechanisms of in vivo action. The protection efficacy was in all cases higher for the complexed drugs, with respect to the free ones; these results are of great interest for their potential usefulness in pharmaceutics.
通过紫外可见吸收光谱和荧光光谱法，在水中定性和定量研究了（2-羟丙基）-β-环糊精（HP-β-CyD）对橙皮素及其7-鼠李糖葡萄糖苷（橙皮苷）的溶解性和光谱特征的影响。通过相溶解度测量确定了描述配合物形成程度的化学计量比和稳定常数；在这两种情况下均获得了A（L）型图（可溶性1:1配合物）。橙皮素表现出的较高相互作用程度可能归因于苷元分子较高的疏水性和较小的尺寸，因此其对环糊精表现出更大的亲和力，并且能更好地契合环糊精的空腔。随后通过与体内作用的不同机制相关的不同生物学试验，评估了分子包封对这两种黄烷酮抗氧化活性的影响。在所有情况下，与游离药物相比，复合药物的保护效果更高；这些结果因其在pharmaceutics中的潜在用途而备受关注。
