Dubald Marion, Bourgeois Sandrine, Andrieu Véronique, Fessi Hatem
Univ Lyon, Université Claude Bernard Lyon 1, Centre National de la Recherche Scientifique (CNRS), Laboratoire d'Automatique et de GEnie des Procédés (LAGEP) Unité Mixte de Recherche UMR 5007, 43 boulevard du 11 novembre 1918, F-69100, Villeurbanne, France.
Horus Pharma, Cap Var, 148 avenue Georges Guynemer, F-06700 Saint Laurent du Var, France.
Pharmaceutics. 2018 Jan 13;10(1):10. doi: 10.3390/pharmaceutics10010010.
The last fifty years, ophthalmic drug delivery research has made much progress, challenging scientists about the advantages and limitations of this drug delivery approach. Topical eye drops are the most commonly used formulation in ocular drug delivery. Despite the good tolerance for patients, this topical administration is only focus on the anterior ocular diseases and had a high precorneal loss of drugs due to the tears production and ocular barriers. Antibiotics are popularly used in solution or in ointment for the ophthalmic route. However, their local bioavailability needs to be improved in order to decrease the frequency of administrations and the side effects and to increase their therapeutic efficiency. For this purpose, sustained release forms for ophthalmic delivery of antibiotics were developed. This review briefly describes the ocular administration with the ocular barriers and the currently topical forms. It focuses on experimental results to bypass the limitations of ocular antibiotic delivery with new ocular technology as colloidal and in situ gelling systems or with the improvement of existing forms as implants and contact lenses. Nanotechnology is presently a promising drug delivery way to provide protection of antibiotics and improve pathway through ocular barriers and deliver drugs to specific target sites.
在过去的五十年里，眼科药物递送研究取得了很大进展，这促使科学家们思考这种药物递送方法的优势和局限性。局部滴眼剂是眼部药物递送中最常用的剂型。尽管患者对其耐受性良好，但这种局部给药方式仅适用于眼前部疾病，并且由于泪液分泌和眼部屏障，药物在角膜前的损失率很高。抗生素通常以溶液或眼膏的形式用于眼科给药途径。然而，为了减少给药频率和副作用并提高治疗效果，需要提高它们的局部生物利用度。为此，开发了用于眼科递送抗生素的缓释剂型。本综述简要描述了眼部给药以及眼部屏障和目前的局部剂型。它着重于通过新的眼部技术（如胶体和原位凝胶系统）或改进现有剂型（如植入物和隐形眼镜）来绕过眼部抗生素递送的局限性的实验结果。纳米技术目前是一种很有前景的药物递送方式，可保护抗生素，改善通过眼部屏障的途径，并将药物递送至特定靶点。
