DESIGN, DEVELOPMENT AND OPTIMIZATION OF NOVEL NANOVESICLE LOADED SUBGLOSSAL FILMS FOR ENHANCED SYSTEMIC AVAILABILITY OF TACROLIMUS THROUGH SUBLINGUAL ROUTE
Tacrolimus being the drug of choice in prevention of transplanted organ from rejection suffers from low oral bioavailability and dose-dependent side effects. An attempt was made to formulate tacrolimus into subglossal (sublingual) fast dissolving films containing ethosomes using ethanol and soyalecithin to enhance systemic availability of drug with controlled delivery of drug. Ethosomes were prepared by modified mechanical dispersion method and were optimized by central composite design to arrive for best drug-loaded ethosome dispersion. Optimized formulations were characterized for vesicle size, Deformability index and entrapment efficiency. Subglossal films were prepared for best and optimized dispersion using HPMC K15M and PEG-400 as film-forming polymer and plasticizer respectively. Formulated fast dissolving subglossal films were optimized by Box benhkendesign and characterized for physical characteristics like appearance, pH, thickness, disintegration time, in-vitro release, Histopathology studies, stability and in-vivo pharmacokinetics in rats. Higher drug plasma levels were shown by optimized subglossal film when compared with that of oral pengraf capsules. These results suggests the potential of nanovesicle fast dissolving films as effective drug carriers...
Read More




