使用不同聚合物的萘醌新型固体分散体用于改善抗恰加斯病活性
Novel Solid Dispersions of Naphthoquinone Using Different Polymers for Improvement of Antichagasic Activity.
作者信息
Oliveira Verônica da Silva, Dantas Elen Diana, Queiroz Anna Thereza de Sousa, Oliveira Johny Wysllas de Freitas, Silva Marcelo de Sousa da, Ferreira Patricia Garcia, Siva Fernando de Carvalho da, Ferreira Vitor Francisco, Lima Ádley Antonini Neves de
机构信息
Department of Pharmacy, Health Sciences Center, Federal University of Rio Grande do Norte, Natal, Rio Grande do Norte 59012-570, Brazil.
Global Health and Tropical Medicine, Institute of Hygiene and Tropical Medicine, NOVA University Lisbon, 1800-166 Lisbon, Portugal.
出版信息
Pharmaceutics. 2020 Nov 24;12(12):1136. doi: 10.3390/pharmaceutics12121136.
IVS320 (3a,10b-dihydro-1-cyclopenta[]naphtho[2,3-]furan-5,10-dione) is a naphthoquinone that has low solubility in aqueous medium, a physical behavior that limits its biological activities, considering that compounds from this class have several activities. In this work, solid dispersions (SDs) prepared between IVS320 and polymers hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG), and polyvinylpyrrolidone (PVP) were developed using physical mixture (PM), kneading (KN), and rotary evaporation (RE) methods. Dispersions were investigated using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetry (TG), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). In addition, in vitro antiparasitic activity in Y strains was evaluated. Physical-chemical characterization demonstrated the formation of SDs through the interaction of IVS320 with polymeric matrices. SDs of IVS320-polymer presented a significant potentiation of antichagasic activity, with inhibitory growth around 62% (IVS320-HPMC/RE), 55% (IVS320-PEG/RE), and 85% (IVS320-PVP/RE), while pure IVS320 showed a value of 48% for the highest concentrations evaluated (50 µg/mL).
IVS320（3a,10b - 二氢 - 1 - 环戊烯并萘并[2,3 - ]呋喃 - 5,10 - 二酮）是一种萘醌，在水性介质中溶解度较低，这种物理特性限制了其生物活性，尽管该类化合物具有多种活性。在本研究中，采用物理混合（PM）、捏合（KN）和旋转蒸发（RE）方法，制备了IVS320与聚合物羟丙基甲基纤维素（HPMC）、聚乙二醇（PEG）和聚乙烯吡咯烷酮（PVP）之间的固体分散体（SDs）。使用傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）、热重分析法（TG）、粉末X射线衍射（PXRD）和扫描电子显微镜（SEM）对分散体进行了研究。此外，还评估了其对Y株的体外抗寄生虫活性。物理化学表征表明，通过IVS320与聚合物基质的相互作用形成了固体分散体。IVS320 - 聚合物固体分散体的抗恰加斯病活性显著增强，抑制生长率约为62%（IVS320 - HPMC/RE）、55%（IVS320 - PEG/RE）和85%（IVS320 - PVP/RE），而纯IVS320在评估的最高浓度（50 µg/mL）下显示的值为48%。
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