Naslov
Development of highly soluble econazole-cyclodextrin complexes for the treatment of oral candidiadis

Autori
Jug, Mario ; Mennini, Natascia ; Vergara, Andrea ; Mura, Paola ;

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

Izvornik
Programme and Abstract / - , 2013

Skup
3rd Conference Innovation in Drug Delivery Advances in Local Drug Delivery

Mjesto i datum
Pisa, Italija, 22.09.2013. - 25.09.2013

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
econazole nitrate; cyclodextrins; buccal delivery

Sažetak
The aim of the work was to improve solubility and dissolution properties of econazole nitrate (ECO) in pH 6.7 phosphate buffer solution (simulated saliva) by cyclodextrin complexation, as a first phase in the development of a novel mucoadhesive formulation for the treatment of oral candidiasis. Phase-solubility studies of ECO with various cyclodextrin (CD) derivatives, in the presence or not of fixed amounts of a suitable third component (hydrophilic polymers, aminoacids, citric acid), were performed in simulated saliva at 37°C. Equimolar ECO-CD solid systems were prepared by co-grinding in a high-energy micro-mill, in the presence or not of the third component. Drug-carrier interactions were investigated in both liquid and solid state, by 1D and 2D H-NMR analyses, differential scanning calorimetry, X-ray powder diffractometry, dissolution rate studies. Phase-solubility studies indicated the formation of soluble 1:1 drug-CD complexes with all tested CDs. NMR studies and Job’s plots, performed on all ECO-CD systems, confirmed the results of phase-solubility studies and indicated SBEβCD as the best partner for ECO, probably due to its extended lipophilic cavity and the presence of a negative charge, that both contributed to more intense host-guest interactions. Citric acid (CA) proved to be the most effective “third component” to improve both the solubilizing and complexing efficiency of CDs towards ECO. Moreover, the simultaneous use of SBEβCD and citric acid gave rise to the highest improvement in drug solubility and dissolution rate. The combined use of SBEβCD and CA improved ECO solubility and dissolution efficiency of about 10 and 50 times, respectively. The ECO-SBEβCD-CA ternary system was then selected as the best one for drug loading into the mucoadhesive formulation.

Izvorni jezik
Engleski

Znanstvena područja
Farmacija

POVEZANOST RADA