Priprava i karakterizacija mukoadhezivnih flastera za bukalnu primjenu propranolol hidroklorida s kitozanom

Mucoadhesive buccal patches containing propranolol hydrochloride were prepared using the solvent casting method. Chitosan was used as bioadhesive polymer and different ratios of chitosan to PVP K-30 were used. The patches were evaluated for their physical characteristics like mass variation, drug content uniformity, folding endurance, ex vivo mucoadhesion strength, ex vivo mucoadhesion time, surface pH, in vitro drug release, and in vitro buccal permeation study. Patches exhibited controlled release for a period of 7 h. The mechanism of drug release was found to be non-Fickian diffusion and followed the first-order kinetics. Incorporation of PVP K-30 generally enhanced the release rate. Swelling index was proportional to the concentration of PVP K-30. Optimized patches (F4) showed satisfactory bioadhesive strength of 9.6 ± 2.0 g, and ex vivo mucoadhesion time of 272 minutes. The surface pH of all patches was between 5.7 and 6.3 and hence patches should not cause irritation in the buccal cavity. Patches containing 10 mg of drug had higher bioadhesive strength with sustained drug release as compared to patches containing 20 mg of drug. Good correlation was observed between the in vitro drug release and in vitro drug permeation with a correlation coefficient of 0.9364. Stability study of optimized patches was done in human saliva and it was found that both drug and buccal patches were stable.Mukoadhezivni flasteri za bukalnu primjenu s propranolol hidrokloridom pripravljeni su koristeću metodu isparavanja otapala. Kao mukoadhezivni polimer upotrebljen je kitozan u različitim omjerima u odnosu na PVP K-30. Određivana su sljedeća svojstva flastera: masa, ujednačenost količine lijeka, savitljivost, ex vivo mukooadhezivnost, ex vivo vrijeme mukoadhezije, pH na površini, in vitro oslobađanje ljekovite tvari i in vitro permeacija. Iz flastera se ljekovita tvar kontrolirano oslobađala prema kinetici prvog reda tijekom 7 h i nije slijedila Fickov zakon difuzije. Upotreba PVP K-30 produljila je vrijeme oslobađanja. Indeks bubrenja bio je proporcionalan koncentraciji PVP K-30. Snaga bioadhezije optimiranih flastera (F4) bila je 9,6 ± 2,0 g, a ex vivo vrijeme mukoadhezije 272 minute. pH na površini svih flastera bio je između 5,7 i 6,3 pa ne bi trebali iritirati bukalnu šupljinu. Flasteri sa 10 mg propranolola imali su veću bioadhezivnost, a lijek se iz njih polaganije oslobađao nego iz flastera sa 20 mg ljekovite tvari. Dobivena je dobra korelacija između in vitro oslobađanja i in vitro permeacije lijeka (koeficijent korelacije 0,9364). Ispitivanja stabilnosti pokazala su da su i propranolol i flasteri za bukalnu primjenu stabilni u ljudskoj slini