Oral pulsatile delivery systems based on swellable hydrophilic polymers

• Published in: European journal of pharmaceutics and biopharmaceutics Vol. 68; no. 1; pp. 11 - 18
• Main Authors: Gazzaniga, Andrea, Palugan, Luca, Foppoli, Anastasia, Sangalli, Maria Edvige
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 2008
• Subjects: Administration, Oral; Chemistry, Pharmaceutical; Delayed-Action Preparations; Dissolution; Drug Carriers - chemistry; Erosion; Hydrophilic cellulose derivatives; Hydrophobic and Hydrophilic Interactions; Oral pulsatile/delayed release; Pharmaceutical Preparations - chemistry; Polymers - chemistry; Solubility; Swellable hydrophilic polymers; Swelling; Swellable hydrophilic polymers; Oral pulsatile/delayed release; Hydrophilic cellulose derivatives; Swelling; Dissolution; Erosion
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2007.05.022

Upon contact with aqueous fluids, swellable hydrophilic polymers undergo typical chain relaxation phenomena that coincide with a glassy–rubbery transition. In the rubbery phase, these polymers may be subject to swelling, dissolution and erosion processes or, alternatively, form an enduring gel barrier when cross-linked networks (hydrogels) are dealt with. Because of the peculiar hydration and biocompatibility properties, such materials are widely exploited in the pharmaceutical field, particularly as far as hydrophilic cellulose derivatives are concerned. In oral delivery, they have for long been employed in the manufacturing of prolonged release matrices and, more recently, for pulsatile (delayed) release devices as well. Pulsatile delivery, which is meant as the liberation of drugs following programmed lag phases, has drawn increasing interest especially in view of emerging chronotherapeutic approaches. In pursuit of pulsatile release, various design strategies have been proposed, chiefly including reservoir, capsular and osmotic formulations. In most cases, water-swellable polymers play a key role in the overall delivery mechanism after being activated by physiological media. Based on these premises, the aim of the present review is to survey the main oral pulsatile delivery systems, for which swelling, dissolution and/or erosion of hydrophilic polymers are primarily involved in the control of release.