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https://www.selleckchem.com/ Selfmicroemulsifying properties were not impaired neither after the solidification process and nor after the compression of solid SMEDDS into tablets. This suggests that fluid-bed granulation with SMEDDS offers a perspective alternative for solidification of the SMEDDS, enabling preservation of self-microemulsifying properties, acceptable drug loading and complete drug release. AIM Development of a preactivated thiomer as sprayable excipient for mucoadhesive formulations. METHODS CG4500 (acrylic acid/acrylamide-methyl propane sulfonic acid copolymer) was thiolated by conjugation with L-cysteine and preactivated by further modification with 2-mercaptonicotinic acid (MNA) in a two-step synthesis and characterized regarding degree of modification and cytotoxicity on Caco-2 cells. The mucoadhesive properties of this novel thiomer were evaluated via rheological synergism, tensile and mucosal residence time studies. Furthermore, the sprayability of the thiomer was evaluated. RESULTS The newly synthesized derivatives CG4500-SH and CG4500-S-S-MNA showed mean coupling rates of 651 µmol thiol groups and 264 µmol MNA per gram polymer, respectively. Even for the unmodified polymer a rheological synergism was observed with isolated porcine intestinal mucus, which was 2.81-fold higher in case of the preactivated thiomer. Mucoadhesion studies on freshly excised porcine intestinal mucosa confirmed these results via a 2.43-fold higher total work of adhesion and a 2.31-fold higher mucosal residence time of the preactivated thiomer. In sprayability tests it was shown that solutions of the preactivated thiomer could be sprayed in concentrations up to 12% (m/V). CONCLUSION The novel polymer CG4500-S-S-MNA is a promising sprayable excipient for mucoadhesive formulations. In current study, it was investigated if the moisture-mediated polymorphic transition from δ- to β-mannitol during twin screw granulation (TSG) also took place in high drug loaded formulation

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