Abstract
A semisynthetic polymer of carboxymethyl sago cellulose (CMSC) was synthesized from Malaysian sago biomass and further used in the development of drug delivery system. Recently, we have reported spray-dried carboxymethyl sago cellulose (CMSC) microspheres for enteric release and dissolution enhancement of piroxicam. In the present investigation, an attempt has been made to improve the enteric release property of CMSC microspheres using aluminium chloride as a cross-linker in the spray drying process and prednisolone as a model drug. CMSC microspheres loaded with prednisolone were prepared using a cross-linker concentration of 0%, 0.01%, 0.025% and 0.05%. All the drug-loaded microspheres were found to have high drug entrapment efficiencies (DEE) ranging from 99% to 106.1%. FT-IR spectroscopy has confirmed the cross-linking in CMSC microspheres as well as intact and amorphous nature of the entrapped drug. Field Emission Scanning Electron Microscope (FESEM) results have shown agglomeration of microspheres and the presence of drugs on the surface. Cross-linked microspheres have shown better efficiency than the uncross-linked microspheres in restricting drug release in stomach pH. Only about 5% of the loaded drug was released from cross-linked microspheres at pH 1.2 while 10% of the drug was released from uncross-linked microspheres. Also, cross-linked microspheres have exhibited faster drug release in pH 6.8 than the uncross-linked microspheres. Spray-dried and AlCl3 cross-linked CMSC microspheres have shown promising results in enteric drug delivery as well as dissolution enhancement.
Highlights
Metroxylon sagu is known as sago palm that rich source of starch and it serves as one of the various forms of staple food for communities across the globe
carboxymethyl sago cellulose (CMSC) microspheres loaded with prednisolone were prepared using a cross-linker concentration of 0%, 0.01%, 0.025% and 0.05%
Fourier-transform infrared spectroscopy (FT-IR) spectroscopy has confirmed the cross-linking in CMSC microspheres as well as intact and amorphous nature of the entrapped drug
Summary
Metroxylon sagu is known as sago palm that rich source of starch and it serves as one of the various forms of staple food for communities across the globe. Malaysia ( in Johor Bharu and Sarawak) is one of the highest producers and exporters of sago starch and at the same time generates a large amount of sago biomass, which poses an environmental problem. It is favourable if sago biomass can be converted into useful products that would greatly decrease the amount of water pollution contributing to the environment. Spray drying is a common method used to prepare microspheres or microcapsules for loading and administration of various drugs [3] [4] It is a relatively rapid and simple technique that can produce a good yield with high drug entrapment efficiency [3]. Prednisolone loaded CMSC microspheres were synthesized by spray drying using different % of aluminium chloride and characterized by entrapment efficiency, Fourier-transform infrared spectroscopy (FT-IR), field emission scanning electron microscopy (FE-SEM) and in vitro release studies
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