TLC characterization of liposomes containingD-myo-inositol derivatives

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Abstract
The thin‐layer chromatographic (TLC) behaviour of liposomes containig inositol phosphates (IPs) was studied. The liposomes contained different concentrations of D‐myo‐inositol 1, 4, 5‐trisphosphate (IP3), D‐myo‐inositol 1, 2, 6‐trisphosphate (α‐trinositol, PP 56, a novel Perstorp Pharma derivative), D‐myo‐inositol 1, 3, 4, 5‐tetrakisphosphate (IP4), D‐myo‐inositol 1, 3, 4, 5, 6‐pentakisphosphate (IP5) and D‐myo‐inositol 1, 2, 3, 4, 5, 6‐hexakisphosphate (IP6). Migration of all liposome batches was compared to that of control liposomes (containing only triple‐distilled water), and to that of free phosphatidylcholine (PC); the same amount of lipid was used in all situations. Thin‐layer chromatography was performed on silica gel as adsorbent. As solvent we used an n‐buthanol: ethanol: water mixture in a 4:3:3 volume ratio. Significant differences were found between PC and all liposome batches, as well as between control liposomes and the ones containing IP3, α‐trinositol, IP4, or IP5, in various concentrations. Liposomes containing IP6 migrate completely differently compared not only to phosphatidylcholine and control liposomes, but also to the ones containing other IPs (−3M). Unlike the other IPs studied, liposome‐entrapped IP6 elicits dose‐independent contractions of the isolated rat aorta. This suggests that liposomes loaded with IP6 undergo, during or after their preparation, physico‐chemical alterations that eventually change their drug‐delivery capacity.

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