Wasim Muhammad, Bergonzi Maria Camilla
Department of Chemistry "Ugo Schiff" (DICUS), University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy.
Molecules. 2025 Feb 17;30(4):928. doi: 10.3390/molecules30040928.
The European Union, producing over 2.5 billion tons of waste annually, has prompted the European Parliament to implement legal measures and encourage the shift towards a circular economy. Millions of tons of biowaste from olive plant leaves are generated annually, resulting in environmental and economic challenges. To address this, the biowaste of olive leaves was valorized, resulting in the extraction of valuable components, triterpenes and polyphenols, which hold potential pharmaceutical, food, or cosmetic applications. Our research involved the formulation of a triterpene extract (TTP70, 70% triterpenes) as a solid dispersion using Poloxamer-188 (P188) and Poloxamer-407 (P407). The solid dispersions were prepared using a kneading method and various extract-to-polymer weight ratios, including 1:1, 1:2, and 1:5. The influence of hydrophilic carriers on the solubility, dissolution profile, and in vitro passive permeability of TTP70 was evaluated. Both carriers and all considered weight ratios significantly improved the solubility of hydrophobic extract and the dissolution of triterpenes. PAMPA experiments demonstrated the efficacy of the formulation in improving the passive permeation of triterpenes. Subsequently, the solid dispersions were physically mixed with a polyphenol-enriched extract (OPA40, 49% of polyphenols) also obtained from olive leaves, and they were used to fill hard gelatin capsules and produce an oral dosage form. The composite formulations improved the dissolution of both classes of constituents.
欧盟每年产生超过25亿吨垃圾,这促使欧洲议会实施法律措施并鼓励向循环经济转变。每年产生数百万吨来自橄榄树叶的生物垃圾,带来了环境和经济挑战。为解决这一问题,对橄榄叶生物垃圾进行了增值利用,从而提取出了有价值的成分——三萜类化合物和多酚,它们在制药、食品或化妆品领域具有潜在应用价值。我们的研究涉及使用泊洛沙姆-188(P188)和泊洛沙姆-407(P407)将三萜类提取物(TTP70,70%的三萜类化合物)制成固体分散体。采用捏合方法并使用各种提取物与聚合物的重量比(包括1:1、1:2和1:5)制备固体分散体。评估了亲水性载体对TTP70的溶解度、溶出曲线和体外被动渗透性的影响。两种载体以及所有考虑的重量比均显著提高了疏水性提取物的溶解度和三萜类化合物的溶出度。平行人工膜渗透实验(PAMPA)证明了该制剂在改善三萜类化合物被动渗透方面的效果。随后,将固体分散体与同样从橄榄叶中获得的富含多酚的提取物(OPA40,49%的多酚)进行物理混合,并用于填充硬明胶胶囊,制成口服剂型。复合制剂提高了两类成分的溶出度。