Naslov
Triclosan Complexation with Polymeric and Natural ß-cyclodextrin in Solution and in Solid State

Autori
Jug, Mario ; Mura, Paola ; Maestrelli, Francesca

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
The 15th International Cyclodextrin Symposium, Final program and Abstracts / Viernstein, Helmut ; Wolschann, Peter - Beč, 2010, P15-P15

Skup
15th International Cyclodextrin Symposium

Mjesto i datum
Beč, Austrija, 09.05.2010. - 12.05.2010

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
triklozan; ciklodekstrins; DSC; FTIR; XRPD; dissolution rate

Sažetak
Triclosan (TR), a broad spectrum antimicrobial agent, is one of the most preferred agents for routine oral hygiene due to its potential activity against dental plaque biofilm, which may provide a prevention and therapy of dental diseases such as caries and gingivitis. The clinical efficiency of TR containing formulation is often impaired by its lipophilic character and practical insolubility in water. Because of that, we have thoroughly investigated the solubilising efficiency of polymeric ß-cyclodextrin derivate (PßCD) against TR in solution and in solid state and confronted it to those of parent ß-cyclodextrin (ßCD). Phase solubility studies confirmed the formation of stabile inclusion complex between TR and ßCD with limited aqueous solubility. The addition of hydroxypropyl cellulose (HPC) increased overall TR solubility in ternary system and changed the phase solubility type from BS to AL. HPC did not increase complexation efficiency of ßCD, but acted as a solubilizer of already formed TR/ßCD complex. PCD presented superior solubilising efficiency against TR in respect to ßCD with or without HPC. The TR/PßCD solubilisation curve was linear (AL type) with slope higher than 1. This may indicate that excellent solubilising performance of PßCD may be attributed to the cooperatives between adjacent CD molecules in the polymer structure. 2D 1H-NMR studies confirmed the actual inclusion complex formation between TR and both CDs tested and indicated different binding modes of TR with ßCD and PßCD. Different binary (TR/ßCD, TR/HPC and TR/PßCD) and ternary (TR/ßCD/HPC) solid systems were prepared by co-grinding of the components in high energy mills for 80 minutes at 24 Hz. Thorough solid state analysis (DSC, FTIR and XRPD) demonstrated the formation of amorphous products in case of TR/PßCD and TR/ßCD/HPC. TR/HPC and TR/ßCD retained partial drug crystallinity, while the grinding of TR alone did not change the solid state properties of the drug. Dissolution studies in simulated saliva solution (pH 6.75) confirmed the superior performance of TR/PßCD even in solid state indicating that polymeric CDs is derivative of choice which may improve the biopharmaceutical properties of TR. Interestingly, the positive effect of HPC on the dissolution of solid TR/ßCD sample was completely absent, indicating that TR/ßCD/HPC ternary system may be useful only in development of the liquid formulations.

Izvorni jezik
Engleski

Znanstvena područja
Farmacija

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