Abstract In the present investigation, we attempted to develop a lycopene-in- β-CD -in-phospholipid vesicles (LCPV) with the sole aim of combining the solubilizing power of β-CD with the sustained-release pattern of phospholipid vesicles. Inclusion complexes of β-CD and lycopene were formed and characterized by using DSC and FT-IR. Double-loaded liposomes encapsulating lycopene β-CD complex were prepared using soy lecithin, cholesterol, and β-CD by thin film hydration method. The LCPV formulation was optimized using a 33 full factorial design to understand the impact of independent variables on entrapment efficiency and particle size. The formulations were evaluated for particle size, entrapment efficiency, drug release, and in vivo activity. The particle size of the optimized formulation showed entrapment efficiency of 78.9 ± 4.8% with a size of 255.15 ± 3 nm and zeta potential of –32.6, indicated the formation of a stable formulation which sustained the release up to 49.5% in 12 h. The results of the in vivo study indicated significant cardio-protective activity in an experimental animal. From the above results, it can be concluded that, the LCPV could be effectively used for sustained release of the drug.

中文翻译：

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包裹番茄红素β-环糊精复合物的双载脂质体：制备、优化和评估

摘要 在本研究中，我们试图开发一种番茄红素-β-CD-磷脂囊泡（LCPV），其唯一目的是将 β-CD 的增溶能力与磷脂囊泡的缓释模式相结合。β-CD 和番茄红素的包合物形成并使用 DSC 和 FT-IR 表征。以大豆卵磷脂、胆固醇和β-CD为原料，采用薄膜水合法制备了包裹番茄红素β-CD复合物的双载脂质体。LCPV 配方使用 33 个全因子设计进行优化，以了解自变量对截留效率和粒径的影响。对制剂的粒度、包封率、药物释放和体内活性进行评估。优化配方的粒径显示出 78.9 ± 4 的包封率。8%，大小为 255.15 ± 3 nm，zeta 电位为 –32.6，表明形成了稳定的制剂，在 12 小时内持续释放高达 49.5%。体内研究的结果表明在实验动物中具有显着的心脏保护活性。从以上结果可以得出结论，LCPV可以有效地用于药物的缓释。