Influence of chitosan type on the properties of extruded pellets with low amount of microcrystalline cellulose

Abstract

The purpose of this research was to study the influence of type of chitosan with different molecular weights, ie, 190 and 419 kDa, on properties of pellets prepared by extrusion/ spheronization. The formulations, consisting of acetaminophen as model drug, chitosan, microcrystalline cellulose (MCC), and dibasic calcium phosphate dihydrate with/without sodium alginate, were extruded using a twin-screw extruder and water as the granulating liquid. With 30% wt/wt MCC and no added sodium alginate, spherical pellets were produced containing low and high molecular weight chitosan at a maximum amount of 60% and 40% wt/wt, respectively. With sodium alginate (2.5% wt/wt), pellets with either type of chitosan (60% wt/wt), MCC (17.5% wt/wt), and acetaminophen (20% wt/wt) could be produced indicating an improved pelletforming ability. Type and amount of chitosan and added sodium alginate affected physical properties of pellets including size, roundness, crushing force, and drug release. Low molecular weight chitosan produced pellets with higher mean diameter, sphericity, and crushing force. Additionally, the pellets made of low molecular weight chitosan and added sodium alginate showed faster drug release in 0.1 N HCl but had slower drug release in pH 7.4 phosphate buffer. This indicated that drug release from pellets could be modified by the molecular weight of chitosan. In conclusion, the molecular weight of chitosan had a major influence on formation, physical properties, and drug release from the obtained pellets.

Use of Chitosan-Alginate as Alternative Pelletization Aid to mMicrocrystalline Cellulose in Extrusion/Spheronization

“…It was indicated that an increase in SA fraction led to an increase in pellet strength. Similar to our previous study, 17 the stronger pellets could be obtained by using lower molecular weight chitosan with addition of an appropriate amount of SA. It was suggested that the lower molecular weight chitosan with added SA provided the wet mass with more rigidity and plasticity, thus stronger pellets could be formed.…”

“…15,17 Moreover, both CSLW and CSHW exhibited a similar effect on the crushing force of pellets (Fig. 6).…”

“…This finding seemed to be contrary to the effect of chitosan fraction on the hardness of pellets with MCC. 15,17 The different results found in this study were attributable to the absence of MCC and different added fillers in the pellets. The added filler in this investigation was lactose monohydrate.…”

“…16 Recently, our group could produce pellets with chitosan at a maximum content of 60% w/w and MCC as low as 17.5% w/w by extrusion/spheronization using twin-screw extruder and water as granulation liquid. 17 Though some studies of chitosan as pelletization aid were presented, further investigation to gain more understanding on using chitosan in pellet production by extrusion/spheronization is still be necessary.…”

Evaluation of Drug Release From Coated Pellets Based on Isomalt, Sugar, and Microcrystalline Cellulose Inert Cores

“…Ph., USP, JP] (4). MCC, the gold standard for extrusion-spheronization, is widely used, but possesses various disadvantages, such as drug adsorption to the surface of its fibers, its chemical incompatibility with a number of drugs, and its lack of disintegration when used in matrix pellets (5)(6)(7)(8). Isomalt, a polyol produced from sucrose, is a novel potential carrier core exhibiting multiple health benefits as having low glycemic and low insulinemic responses, and thus is suitable for diabetics (9).…”