Design, synthesis, fabrication and in vitro evalution of mucoadhesive 5-amino-2-mercaptobenzimidazole chitosan as low water soluble drug carriers

作者：Kongsong Mullika; Songsurang Kultida; Sangvanich Polkit; Siralertmukul Krisana; Muangsin Nongnuj^*

来源：European Journal of Pharmaceutics and Biopharmaceutics, 2014, 88(3): 986-997.

DOI：10.1016/j.ejpb.2014.08.016

• Low water soluble drug
• Drug carrier
• Mucoadhesive chitosan
• Thiolated chitosan
• Electrospray
• Microspheres

Mucoadhesive thiolated chitosan suitable as a carrier for low water soluble drugs was designed and synthesized by conjugating 5-amino-2-mercaptobenzimidazole (MBI) using methylacrylate (MA) as the linking agent. A 14.4% degree of substitution of MA, as determined by H-1 NMR analysis, and 11.86 +/- 0.01 mu mol thiol groups/g of polymer, as determined by Ellman%26apos;s method, was obtained. The MBI-MA-chitosan had an 11-fold stronger mucoadhesive property compared to unmodified chitosan at pH 1.2, as determined by the periodic acid: Schiff colorimetric method. Chitosan, MA-chitosan and MBI-MA-chitosan were fabricated as well-formed microspheres using electrospray ionization, including an entrapment efficiency of simvastatin (SV) of over 80% for the. MBI-MA-chitosan. The mucoadhesiveness of the SV-loaded MBI-MA-CS microspheres was still higher than that for SV-loaded chitosan at pH 1.2 and 6.4. The SV-loaded MBI-MA-CS microspheres revealed a reduced burst effect and an increased release rate (more than fivefold higher than pure SV) of SV over 12 h.

• 出版日期2014-11