Freeze-dried eudragit-hyaluronan multicompartment liposomes to improve the intestinal bioavailability of curcumin

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• 作者：Ana Catalan-Latorre^a ; Maryam Ravaghi^b ; Maria Letizia Manca^a ; ^{mlmanca@unica.it" class="auth_mail" title="E-mail the corresponding author} ; Carla Caddeo^a ; Francesca Marongiu^a ; Guido Ennas^c ; Elvira Escribano-Ferrer^c ; José ; Esteban Peris^d ; Octavio Diez-Sales^d ; ^e ; Anna Maria Fadda^a ; Maria Manconi^a
• 关键词：Curcumin ; Polymer ; Liposome ; Antioxidant ; Intestinal biodistribution
• 刊名：European Journal of Pharmaceutics and Biopharmaceutics
• 出版年：2016
• 出版时间：October 2016
• 年：2016
• 卷：107
• 期：Complete
• 页码：49-55
• 全文大小：1418 K

文摘

This work aimed at finding an innovative vesicle-type formulation able to improve the bioavailability of curcumin upon oral administration. To this purpose, phospholipid, Eudragit® S100 and hyaluronan sodium salt were combined to obtain eudragit-hyaluronan immobilized vesicles using an easy and environmentally-friendly method. For the first time, the two polymers were combined in a system intended for oral delivery, to enhance curcumin stability when facing the harsh environment of the gastrointestinal tract. Four different formulations were prepared, keeping constant the amount of the phospholipid and varying the eudragit-hyaluronan ratio. The freeze-drying of the samples, performed to increase their stability, led to a reduction of vesicle size and a good homogeneity of the systems, after simple rehydration with water. X-ray diffraction study demonstrated that after the freeze-drying process, curcumin remained successfully incorporated within the vesicles. All the vesicles displayed similar features: size ranging from 220 to 287 nm, spherical or oval shape, multilamellar or large unilamellar morphology with a peculiar multicompartment organization involving 1–4 smaller vesicles inside. In vitro studies demonstrated the ability of the combined polymers to protect the vesicles from the harsh conditions of the gastro-intestinal tract (i.e., ionic strength and pH variation), which was confirmed in vivo by the greater deposition of curcumin in the intestinal region, as compared to the free drug in dispersion. This enhanced accumulation of curcumin provided by the eudragit-hyaluronan immobilized vesicles, together with an increase in Caco-2 cell viability exposed to hydrogen peroxide, indicated that vesicles can ensure a local protection against oxidative stress and an increase in its intestinal absorption.