Development of ketoprofen loaded proliposomal powders for improved gastric absorption and gastric tolerance: in vitro and in situ evaluation

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Pearlitol SD 200 based proliposomes
Ketoprofen proliposome formulations using pearlitol SD 200 and different ratios of HSPC and cholesterol were prepared. HSPC (a high phase transition temperature lipid) and cholesterol (for structural rigidity) were selected because of their lower risk of oxidation and improved stability of liposomes respectively. However any variation in the composition of HSPC and cholesterol results in the deformation of vesicle, which leads to drug leakage and fusion of vesicle with gastrointestinal epithelium (32). To conquer the lipid to cholesterol composition in developing stable proliposomes varying ratios of HSPC to cholesterol (total lipid mixture of 250 µM) were investigated.
Physicochemical characterization of proliposomes
Formation of liposomes from proliposomal powders
Stepwise formation of liposomes from proliposomes upon hydration was observed under optical microscope and represented in Figure 2 A-D. Proliposomal powder (Figure 2A) upon contact with distilled water resulted in the formation of tubular structures (Figure 2B) due to instantaneous surface lipid hydration of proliposomes followed by budding off and liposome formation until the surface lipid hydration and solubility of the water soluble carrier ends. The hydrophilic nature of pearlitol might also facilitate the quick hydration of proliposomes to transform into liposomes. Under stagnant conditions (without agitation) liposomes formed are aggregates as shown in Figure 2C. Optical microscopic images of the liposomes formed upon hydration with manual agitation (Figure 2D) confirms separation of liposomes from aggregates and dispersion of spherical shape liposomes in the medium.
Micromeritics
Oral administration of proliposomal powders whi...

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...om aggregation and floating behavior of drug particles during dissolution. All proliposomal powders showed 67.5 to 91.2% drug release with following order KPL3>KPL5>KPL0>KPL4>Pure drug within 5 min which indicated improved dissolution of drug in the form of proliposomes. The improved dissolution of ketoprofen in proliposomal formulation may be due to the hydrophilic nature of pearlitol which facilitate the quick hydration of proliposomes to transform into liposomes, enhanced solubility of poorly water soluble drug by amphiphilic HSPC or altered physical state of drug entrapped in the bilayers from crystalline to amorphous state and it may be also due to increased effective surface area and wetting characteristic of unentrapped drug upon contact with dissolution medium as fine dispersion which was adsorbed over the porous water soluble carrier i.e. pearlitol SD 200.

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