Mayol Laura, Serri Carla, Menale Ciro, Crispi Stefania, Piccolo Maria Teresa, Mita Luigi, Giarra Simona, Forte Maurizio, Saija Antonina, Biondi Marco, Mita Damiano Gustavo
Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, Napoli, Italy; Interdisciplinary Research Centre on Biomaterials - CRIB, Università di Napoli Federico II, P.le Tecchio, 80, Napoli, Italy; Consorzio Interuniversitario INBB: Laboratorio Nazionale Interferenti Endocrini, Via Pietro Castellino 111, Napoli, Italy.
Consorzio Interuniversitario INBB: Laboratorio Nazionale Interferenti Endocrini, Via Pietro Castellino 111, Napoli, Italy; Dipartimento di Scienze Biologiche ed Ambientali, Università di Messina, Piazza Pugliatti 1, Messina, Italy.
Eur J Pharm Biopharm. 2015 Jun;93:37-45. doi: 10.1016/j.ejpb.2015.03.005. Epub 2015 Mar 17.
The pharmacological potential of curcumin (CURC) is severely restricted because of its low water solubility/absorption, short half-life and poor bioavailability. To overcome these issues, CURC-loaded nanoparticles (NPs) were produced by a double emulsion technique. In particular, NPs were made up of an amphiphilic blend of poloxamers and PLGA to confer stealth properties to the NPs to take advantage of the enhanced permeability and retention (EPR) effect. Different surface properties of NPs made up of bare PLGA and PLGA/poloxamer blend were confirmed by the different interactions of these NPs with serum proteins and also by their ability to be internalized by mesothelioma cell line. The uptake of PLGA/poloxamer NPs induces a persistent block in G0/G1 phase of the cell cycle up to 72 h, thus overcoming the drug tolerance phenomenon, normally evidenced with free CURC.
姜黄素（CURC）的药理潜力受到严重限制，因为其水溶性/吸收性低、半衰期短且生物利用度差。为克服这些问题，采用双乳液技术制备了负载姜黄素的纳米颗粒（NPs）。具体而言，NPs由泊洛沙姆和聚乳酸-羟基乙酸共聚物（PLGA）的两亲性混合物组成，以使NPs具有隐形特性，从而利用增强的通透性和滞留（EPR）效应。由裸PLGA和PLGA/泊洛沙姆混合物组成的NPs具有不同的表面性质，这通过这些NPs与血清蛋白的不同相互作用以及它们被间皮瘤细胞系内化的能力得到证实。PLGA/泊洛沙姆NPs的摄取在细胞周期的G0/G1期诱导持续阻滞长达72小时，从而克服了通常在游离姜黄素中出现的耐药现象。
