Profire Bianca-Ștefania, Lupașcu Florentina Geanina, Sava Alexandru, Turin-Moleavin Ioana-Andreea, Bejan Dana, Stătescu Cristian, Șorodoc Victorița, Sascău Radu-Andy, Șorodoc Laurențiu, Pinteala Mariana, Profire Lenuța
Faculty of Medicine, "Grigore T. Popa" University of Medicine and Pharmacy of Iasi, 16 University Street, 700115 Iași, Romania.
Faculty of Pharmacy, "Grigore T. Popa" University of Medicine and Pharmacy of Iași, 16 University Street, 700115 Iași, Romania.
Pharmaceutics. 2025 Jul 26;17(8):969. doi: 10.3390/pharmaceutics17080969.
: As novel synergistic strategy for heart failure (HF), this study explores the formulation and characterization of liposomal systems co-loaded with SGLT2 inhibitors (dapagliflozin-DAPA and empagliflozin-EMPA) and curcumin (Cur). : To enhance liposomal membrane stability and achieve sustained, controlled drug release, oleanolic acid (OA) was incorporated into the lipid bilayer, while the liposomal surface was coated with polyvinylpyrrolidone (PVP). : The resulting liposomes exhibited favorable physico-chemical properties (particle size ~170 nm, low PDI, negative zeta potential), high encapsulation efficiencies (up to 97%), and spherical morphology as confirmed by STEM. XRD and DSC analyses indicated successful API incorporation and amorphization within the lipid matrix, while PVP coating provided slight improvements in thermal stability. Trehalose proved to be an effective cryoprotectant, preserving liposome integrity after freeze-drying. In vitro release studies demonstrated sustained and delayed drug release, especially in PVP-coated and OA-containing formulations. : All these findings highlight the promise of PVP-coated, OA-stabilized liposomal formulations co-loaded with SGLT2 inhibitors and Cur as biocompatible, multifunctional platforms for targeted HF therapy.
作为一种针对心力衰竭(HF)的新型协同策略,本研究探索了共载有钠-葡萄糖协同转运蛋白2(SGLT2)抑制剂(达格列净-DAPA和恩格列净-EMPA)与姜黄素(Cur)的脂质体系统的制备及其特性。为提高脂质体膜稳定性并实现药物的持续、可控释放,将齐墩果酸(OA)掺入脂质双层中,同时用聚乙烯吡咯烷酮(PVP)包被脂质体表面。所得脂质体表现出良好的物理化学性质(粒径约170 nm、低多分散指数、负ζ电位)、高包封率(高达97%),并且如扫描透射电子显微镜(STEM)所证实的呈球形形态。X射线衍射(XRD)和差示扫描量热法(DSC)分析表明活性药物成分成功掺入脂质基质并形成无定形状态,而PVP包被使热稳定性略有提高。海藻糖被证明是一种有效的冷冻保护剂,可在冻干后保持脂质体完整性。体外释放研究表明药物呈持续和延迟释放,尤其是在PVP包被且含OA的制剂中。所有这些发现突出了共载有SGLT2抑制剂和Cur的PVP包被、OA稳定化脂质体制剂作为用于靶向HF治疗的生物相容性多功能平台的前景。