Novel co-axial prilling technique for the development of core-shell particles as delayed drug delivery systems

作者：Del Gaudio Pasquale; Auriemma Giulia^*; Russo Paola; Mencherini Teresa; Campiglia Pietro; Stigliani Mariateresa; Aquino Rita Patrizia

来源：European Journal of Pharmaceutics and Biopharmaceutics, 2014, 87(3): 541-547.

DOI：10.1016/j.ejpb.2014.02.010

• Co-axial prilling
• Natural polysaccharides
• Core-shell beads
• Delayed drug delivery systems
• Piroxicam
• Chronotherapy

In this study, biocompatible double layered beads consisting of pectin core and alginate shell were prepared through a single step manufacturing process based on prilling apparatus equipped with co-axial nozzles. The core was loaded with piroxicam (PRX) as model non-steroidal anti-inflammatory drug (NSAID). Morphology, size distribution and shape of the double layered beads varied depending on the operative conditions and polymer concentrations. Co-axial nozzles size, applied vibration frequency, gelling conditions and, mainly, polymers mass ratio were identified as critical variables. Particularly, the relative viscosity of polymeric feed solutions inside the nozzle was the key parameter to obtain homogeneous and well-formed coated particles. The produced beads were investigated for the release kinetic in different media. Once PRX was encapsulated within the pectin core, a controlled release pattern was observed. Particularly, beads produced with 4:1 core/shell ratio (F4) released less than 30% of PRX in simulated gastric fluid (SGF) while total liberation of the drug was achieved during the next 3 h in simulated intestinal fluid (SIF). More interesting, F4 tested in SIF was able to release drug in a delayed and sustained manner at established time points (2h_8.2%, 3h_32.2%, 4h_70.1% and 5h_about 100%). Based on the above results, co-axial prilling approach is expected to provide success in manufacturing systems with delayed drug release profiles. Such systems may be potentially useful in targeting diseases which are affected by the circadian rhythm, such as chronic inflammation.

• 出版日期2014-8