Abstract
The objective of the current study was to optimize the composition of alginate beads to produce ambroxol hydrochloride alginate beads with optimum specifications. The study employed beads based on sodium alginate solution (2% w/v) as the main component with calcium chloride solution as crosslinking agent as the prototype beads. The beads were prepared by syringe method. The effect of viscosity modifiers on the morphology, entrapment efficiency and drug release was studied. The prototype beads were spherical semitransparent with entrapment efficiency (EE) of 23%. Incorporation of polyvinylpyrrolidone (PVP) as a viscosity modifier produced spherical semitransparent beads with higher EE values compared with the prototype. Addition of carboxymethyl cellulose (CMC) produced oval opaque beads which have larger size and higher EE values compared with the prototype beads or those containing PVP only. Replacement of CMC with hydroxypropyl methyl cellulose (HPMC) produced semitransparent spherical beads with significant increase in the EE. Monitoring the drug release rate from different beads, the all the tested beads were able to retain the drug in the stomach condition. In the intestinal conditions the release rate depended on the composition of the beads with prototype beads librating most of its contents in the first 15 minutes. Formulations containing either CMC or HPMC were able to retard the drug release in the intestinal phase. In conclusion the study developed beads with optimum entrapment and release of ambroxol hydrochloride.
Highlights
Alginate is a polysaccharide which contains varying amounts of 1,4'-linked β-D-mannuronic acid, α-L-guluronic acid residues
The objective of the current study was to optimize the composition of alginate beads to produce ambroxol hydrochloride alginate beads with optimum specifications
In the intestinal conditions the release rate depended on the composition of the beads with prototype beads librating most of its contents in the first 15 minutes
Summary
Alginate is a polysaccharide which contains varying amounts of 1,4'-linked β-D-mannuronic acid, α-L-guluronic acid residues. As biocompatible and biodegradable biopolymer, it can form a bioadhesive stable gel especially in the presence of divalent cations such as calcium or barium These properties have been employed in development of controlled release drug delivery system (Rasel and Hasan, 2012). The effect of divalent cations on alginate solution is widely used in preparation of solid beads for controlled drug delivery (Kanaka Durga Devi et al, 2010) These beads are acid resistant and can liberate the drug slowly in acidic environment. Ionotropic gelation technique (Poncelet et al, 1999) is the most widely used technique with the majority of researchers employing syringes manually or mechanically via pump to drip alginate solution into a solution of divalent cation This is expected to form beads (Takka and Gürel, 2010). The effect of viscosity modifiers such as hydroxypropyl methylcellulose (HPMC), sodium carboxy methylcellulose (NaCMC) and Polyvinyl pyrrolidone (PVP) on the characteristics of beads was investigated
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