摘要
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 AlCl<sub>3</sub> cross-linked CMSC microspheres have shown promising results in enteric drug delivery as well as dissolution enhancement.
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 AlCl<sub>3</sub> cross-linked CMSC microspheres have shown promising results in enteric drug delivery as well as dissolution enhancement.
作者
Saravanan Muniyandy
Pushpamalar Janarthanan
Thenapakiam Sathasivam
Saravanan Muniyandy;Pushpamalar Janarthanan;Thenapakiam Sathasivam(Department of Pharmacy, Fatima College of Health Sciences, Al Ain, United Arab Emirates;School of Science, Monash University Malaysia, Selangor, Malaysia;Monash-Industry Palm Oil Education and Research Platform (MIPO), Monash University Malaysia, Selangor, Malaysia;School of Pharmacy, Monash University Malaysia, Selangor, Malaysia)