Cetirizine dihydrochloride loaded microparticles design using ionotropic cross-linked chitosan nanoparticles by spray-drying method

Abstract

To control the release rate and mask the bitter taste, cetirizine dihydrochloride (CedH) was entrapped within chitosan nanoparticles (CS-NPs) using an ionotropic gelation process, followed by microencapsulation to produce CS matrix microparticles using a spray-drying method. The aqueous colloidal CS-NPs dispersions with a drug encapsulation efficiency (EE) of <15%, were then spray dried to produce a powdered nanoparticles-in-microparticles system with an EE of >70%. The resultant spherical CS microparticles had a smooth surface, were free of organic solvent residue and showed a diameter range of 0.5~5 μm. The in vitro drug release properties of CedH encapsulated microparticles showed an initial burst effect during the first 2 h. Drug release from the matrix CS microparticles could be retarded by the crosslinking agent pentasodium tripolyphosphate or the wall material. The technique of 'ionotropic gelation' combined with 'spray-drying' could be applicable for preparation of CS nanoparticlesin-microparticles drug delivery systems. CS-NPs based microparticles might provide a potential micro-carrier for oral administration of the freely water-soluble drug--CedH.

A novel spray-dried nanoparticles-in-microparticles system for formulating scopolamine hydrobromide into orally disintegrating tablets

“…10 Our recent work has established a CS-based NiMS that displays high drug entrapment efficiency and controlled drug release. 11,12 The obtained results are quite encouraging, in terms of the further application of NiMS for oral drug delivery.…”

Nano and Microparticulate Chitosan Based System for Formulation of Carvedilol Rapid Melt Tablet

“…Preparation of Carvedilol loaded Chitosan nanoparticles by ionotropic gelation method Ionotropic gelation for the Chitosan nanoparticles formation was performed as previously described. [19][20][21][22] Chitosan solution was prepared by dissolving the required amount of chitosan in dilute acetic acid (0.3%, v/v) at room temperature overnight and passed through a 0.22 μm filter to remove insoluble's. Various amounts of Carvedilol mentioned in Table 1 were dissolved into the 10 ml methanol.…”

“…In vitro Drug release from the microparticles 19,20 In vitro drug release profiles of Carvedilol loaded microparticles were carried out as described here. About 30 mg of microparticles was placed into a dialysis membrane bag that was impermeable to molecular cutoff of 8 kDa.…”

“…14,15 Chitosan based NMCS displays high drug entrapment efficiency and controlled drug release. 16,17 The NMCS of water insoluble model drug was prepared using a spray-drying method. Carvedilol is a non-selective β-adrenergic blocking agent with α1-blocking activity decreases the heart rate, myocardial contractility and myocardial oxygen demand.…”

Chitosan Cross-Linked Pentasodium Tripolyphosphate Micro/Nanoparticles Produced by Ionotropic Gelation

“…Several methods have been employed for the production of chitosan particles, including ionotropic gelation (Bokharaei et al 2011;Rampino et al 2013), spray drying (Li et al 2010), coacervation (Kaloti and Bohidar 2010) and emulsification (Sun et al 2010). Among these methods, the ionotropic gelation is based on electrostatic interaction between the amine group of chitosan and the negatively charged group of a polyanion (Hudson and Margaritis 2014;Nagpal et al 2010), such as pentasodium tripolyphosphate (Li et al 2010;Shu and Zhu 2002), alginate (Elzatahry et al 2009), hyaluronic acid (Oyarzun-Ampuero et al 2009), glutaraldehyde, glyoxal and ethylene glycol diglycidyl ether (Akbuga and Durmaz 1994).…”