Naslov
Novel cyclodextrin-based film formulation intended for buccal delivery of atenolol

Autori
Jug, Mario ; Bećirević-Laćan, Mira ; Bengez, Sandra

Izvornik
Drug development and industrial pharmacy (0363-9045) 35 (2009), 7; 796-807

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
atenolol ; randomly methylated ß-cyclodextrin ; polymeric films ; buccal delivery ; bioadhesion

Sažetak
A novel bioadhesive film formulation for buccal atenolol delivery containing drug/cyclodextrin inclusion compounds was developed. Interaction between atenolol and randomly methylated ß-cyclodextrin (RAMEB) in solution was studied by phase solubility studies. The results revealed formation of a stabile inclusion complex (Ks=783.4± ; 21.6 M-1) in 1:1 molar stoichiometry. The complex in solid state was prepared by the freeze-drying method and characterized by differential scanning calorimetry (DSC) and Fourieur transformed infrared spectroscopy (FTIR). The drug, free or in complex form, was incorporated into polymeric films prepared by the casting method using ethylcellulose (EC), polyvinyl alcohol (PVA) and hydroxypropyl methylcellulose (HPMC). The swelling properties of films were predominated by the type of polymer used in formulation In vitro bioadhesive properties of the films were well correlated with the swelling properties of the polymers used in the formulation. Although incorporation of the drug, free or in complex form, decreased the bioadhesion of the films, PVA and HPMC based formulations retained suitable bioadhesive properties. Higher atenolol solubility upon complexation with RAMEB increased the drug dissolution rate under conditions designed to be similar to those on the buccal mucosa, but it has decreased the drug release rate from the PVA and HPMC film formulation, leading to a sustained drug release pattern. In the case of EC based films, RAMEB promoted drug release. Other parameters that influenced the drug release rate were associated with the structure of the polymer used in the formulation, swelling characteristics of the films and the interaction between atenolol and hydrophilic polymers that was demonstrated by FTIR analysis.

Izvorni jezik
Engleski

Znanstvena područja
Farmacija

POVEZANOST RADA