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基于壳聚糖/明胶微粒的用于递送盐酸普萘洛尔的粘膜粘附口腔片

Mucoadhesive Buccal Tablets Based on Chitosan/Gelatin Microparticles for Delivery of Propranolol Hydrochloride.

作者信息

Abruzzo Angela, Cerchiara Teresa, Bigucci Federica, Gallucci Maria Caterina, Luppi Barbara

机构信息

Department of Pharmacy and Biotechnology, University of Bologna, Bologna 40127, Italy.

Department of Pharmacy and Biotechnology, University of Bologna, Bologna 40127, Italy.

出版信息

J Pharm Sci. 2015 Dec;104(12):4365-4372. doi: 10.1002/jps.24688. Epub 2015 Oct 27.

Abstract

Propranolol administration through buccal route offers some distinct advantages thanks to the easy access to the oral mucosa, fast onset of action, and avoidance of hepatic and intestinal degradation mechanisms. To overcome the effective removal existing in the buccal cavity, mucoadhesive delivery systems are considered a promising approach as they facilitate a close contact with the buccal mucosa. The aim of this study was to prepare mucoadhesive tablets based on chitosan/gelatin microparticles for buccal delivery of propranolol hydrochloride. Spray-dried microparticles were prepared with different chitosan-gelatin weight ratios and characterized in terms of yield and morphology. Microparticles were subsequently compressed with the drug to obtain loaded buccal tablets. In vitro water uptake, mucoadhesion, release, and permeation tests were performed to investigate tablet ability to hydrate, to adhere to the mucosa, and to deliver drug through buccal mucosa. Microparticles showed a different morphology based on the different chitosan-gelatin weight ratios. Moreover, buccal tablets based on the prepared microparticles showed different technological and functional characteristics in virtue of their composition. In particular, tablets with an excess of chitosan showed the best mucoadhesive properties, allowed the permeation of the greatest drug amount among all formulations, and could be promising for buccal administration of propranolol hydrochloride.

摘要

通过颊部途径给药普萘洛尔具有一些明显的优势,这得益于口腔黏膜易于接触、起效迅速以及避免肝脏和肠道的降解机制。为了克服口腔内有效的清除作用,黏膜黏附递送系统被认为是一种有前景的方法,因为它们有助于与颊黏膜紧密接触。本研究的目的是制备基于壳聚糖/明胶微粒的黏膜黏附片剂,用于颊部递送盐酸普萘洛尔。用不同壳聚糖 - 明胶重量比制备喷雾干燥微粒,并对其产率和形态进行表征。随后将微粒与药物压片以获得载药颊用片剂。进行体外吸水、黏膜黏附、释放和渗透试验,以研究片剂水化、黏附于黏膜以及通过颊黏膜递送药物的能力。基于不同壳聚糖 - 明胶重量比,微粒呈现出不同的形态。此外,基于所制备微粒的颊用片剂因其组成而表现出不同的工艺和功能特性。特别是,壳聚糖过量的片剂表现出最佳的黏膜黏附性能,在所有制剂中允许最大量的药物渗透,并且可能有望用于盐酸普萘洛尔的颊部给药。

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