We have developed a novel alpha-helical peptide antibiotic termed NK-2. It efficiently kills bacteria, but not human cells, by membrane destruction. This selectivity could be attributed to the different membrane lipid compositions of the target cells. To understand the mechanisms of selectivity and membrane destruction, we investigated the influence of NK-2 on the supramolecular aggregate structure, the phase transition behavior, the acyl chain fluidity, and the surface charges of phospholipids representative for the bacterial and the human cell cytoplasmic membranes. The cationic NK-2 binds to anionic phosphatidylglycerol liposomes, causing a thinning of the membrane and an increase in the phase transition temperature. However, this interaction is not solely of electrostatic but also of hydrophobic nature, indicated by an overcompensation of the Zeta potential. Whereas NK-2 has no effect on phosphatidylcholine liposomes, it enhances the fluidity of phosphatidylethanolamine acyl chains and lowers the phase transition enthalpy of the gel to liquid cristalline transition. The most dramatic effect, however, was observed for the lamellar/inverted hexagonal transition of phosphatidylethanolamine which was reduced by more than 10 degrees C. Thus, NK-2 promotes a negative membrane curvature which can lead to the collapse of the phosphatidylethanolamine-rich bacterial cytoplasmic membrane.

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The crystallinity of omeprazole in six film‐forming polymers, Eudragit L100, shellac, polyvinyl acetate phthalate, cellulose acetate phthalate, hydroxypropyl methylcellulose acetate phthalate and hydroxypropyl methylcellulose (HPMC) was determined. Polymer films containing omeprazole were prepared by casting and characterized using powder X‐ray diffractometry, Fourier transform infrared spectroscopy, and differential scanning calorimetry. Omeprazole powder recrystallized from all solvents studied were similar to the original powder. The drug existed as the amorphous form in the five acid polymers whereas its crystalline form appeared in nonionic polymer HPMC. No evidence of a drug‐polymer interaction was found. Omeprazole exists in amorphous form in polymers most commonly used in enteric filmcoated formulations.

The physical structure and drug-polymer interactions of theophylline in Eudragit L100, shellac, polyvinyl acetate phthalate (PVAP), cellulose acetate phthalate (CAP), hydroxypropylmethylcellulose acetate phthalate (HPMCP), and hydroxypropylmethylcellulose (HPMC) were studied. The drug-polymer films were prepared by casting and were characterized using powder X-ray diffractometry (PXRD), nuclear magnetic resonance (NMR) spectroscopy, and thin-layer chromatography (TLC). Theophylline was found to recrystallize in the modification II form in all kinds of polymers, which was the same as that recrystallized solely from the solvent system and the original powder. The PXRD and NMR results indicated a superficial drug-polymer interaction between theophylline and Eudragit L100, while there was no evidence of interaction for the others. No drug decomposition was observed by TLC for all drug-polymer mixtures.

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