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透明质酸脂质体凝胶可持续地将皮质类固醇递送至内耳。

Hyaluronic acid liposomal gel sustains delivery of a corticoid to the inner ear.

作者信息

El Kechai Naila, Mamelle Elisabeth, Nguyen Yann, Huang Nicolas, Nicolas Valérie, Chaminade Pierre, Yen-Nicolaÿ Stéphanie, Gueutin Claire, Granger Benjamin, Ferrary Evelyne, Agnely Florence, Bochot Amélie

机构信息

Institut Galien Paris-Sud, CNRS UMR 8612, Univ. Paris-Sud, Université Paris-Saclay, 92290 Châtenay-Malabry, France.

UMR-S 1159 Inserm/Université Pierre et Marie Curie - Sorbonne Universités "Minimally Invasive Robot-based Hearing Rehabilitation", 16 rue Henri Huchard, 75018 Paris, France; AP-HP, Pitié-Salpêtrière Hospital, Otolaryngology Department, Unit of Otology, Auditory Implants and Skull Base Surgery, 75013 Paris, France.

出版信息

J Control Release. 2016 Mar 28;226:248-57. doi: 10.1016/j.jconrel.2016.02.013. Epub 2016 Feb 6.

Abstract

The inner ear is one of the most challenging organs for drug delivery, mainly because of the blood-perilymph barrier. Therefore, local rather than systemic drug delivery methods are being developed for inner ear therapy. In this work, we have evaluated the benefit of a hyaluronic acid liposomal gel for sustained delivery of a corticoid to the inner ear after local injection into the middle ear in a guinea pig model. The liposomal gel was easily injectable as a result of the shear-thinning behavior of hyaluronic acid. A prolonged residence time at the site of injection as well as in the round window were achieved without any negative effect on the hearing thresholds of the animals. The presence of liposomes in the formulation resulted in sustained release of the drug in the perilymph for 30days and promoted the conversion of the prodrug loaded within the liposomes (dexamethasone phosphate) into its active form (dexamethasone). In this way, therapeutic doses were attained in the perilymph. A small amount of intact liposomes was visualized in the perilymph, whereas the main proportion of liposomes seemed to be trapped in the round window resulting in a reservoir effect. Thus, the administration of hyaluronic acid liposomal gel to the middle ear is an efficient strategy for delivering corticoids to the inner ear in a sustained manner.

摘要

内耳是药物递送最具挑战性的器官之一,主要是因为存在血-外淋巴屏障。因此,正在开发用于内耳治疗的局部而非全身药物递送方法。在这项工作中,我们评估了透明质酸脂质体凝胶在豚鼠模型中耳内局部注射后将皮质类固醇持续递送至内耳的益处。由于透明质酸的剪切变稀行为,脂质体凝胶易于注射。在注射部位以及圆窗处实现了延长的停留时间,且对动物的听力阈值没有任何负面影响。制剂中脂质体的存在导致药物在外淋巴中持续释放30天,并促进了脂质体内负载的前药(磷酸地塞米松)转化为其活性形式(地塞米松)。通过这种方式,在外淋巴中达到了治疗剂量。在外淋巴中观察到少量完整的脂质体,而大部分脂质体似乎被困在圆窗中,从而产生了储库效应。因此,向中耳施用透明质酸脂质体凝胶是一种将皮质类固醇持续递送至内耳的有效策略。

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