Oral hydrophilic matrices having non uniform drug distribution for zero-order release: A literature review

JOURNAL OF CONTROLLED RELEASE

卷:325

Review

Cerea, Matteo¹  Maroni, Alessandra¹  Palugan, Luca¹  Moutaharrik, Saliha¹  Melocchi, Alice¹  Zema, Lucia¹  Foppoli, Anastasia¹  Gazzaniga, Andrea¹ 

[1] Univ Milan, Dipartimento Sci Farmaceut, Sez Tecnol & Legislaz Farmaceut Maria Edvige Sang, Via G Colombo 71, I-20133 Milan, Italy

关键词: Matrix systems;    Hydrophilic polymer;    Oral prolonged release;    Zero-order release;    Non-uniform drug distribution;    Gradient drug concentration;   

DOI  :  10.1016/j.jconrel.2020.06.033

来源: Elsevier

【 摘 要 】

Oral hydrophilic matrices for prolonged release mostly show a decrease in the rate of drug release over time, owing to the increasing length of the diffusional path and progressive reduction of the area at the interface between glassy and rubbery matrix. In addition, burst effect may also occur due to the fraction of drug present on the surface of the system, which is released when the external polymer particles are not fully swollen yet. Different strategies have been attempted in order to address these issues and, ideally, to reach zero-order release. The approaches proposed are based on geometric modulation of the release area, control of the swelling behavior or initial non-uniform distribution of the active ingredient throughout the polymer matrix. The present article offers an extensive analysis of the various methods described in the literature for reaching zero-order release leveraging non-uniform distribution of the drug in hydrophilic polymeric systems. In this respect, special attention is given to the design of the main delivery platforms reviewed, their manufacturing, in vitro release profiles and analytical techniques for assessing drug concentration patterns within the solid units.

【 授权许可】

Free