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• W2015217412 abstract "A liposome-gel formulation containing 1% (w/w) hydrocortisone was prepared by blending phosphatidylcholine liposomes of hydrocortisone with Carbopol 934 hydrogel. The liposome-gel was applied topically onto the normal and stratum corneum (SC)-removed skins (3.0 cm2) of hairless mice at a dose of 1 mg as hydrocortisone. Percutaneous absorption of hydrocortisone across the SC-removed skin was significantly faster than that across normal skin, suggesting that SC behaves as a penetration barrier for the liposome-bound drugs. Contrary to previous reports that have suggested enhanced percutaneous penetration of drugs by liposomes, the liposome-gel in this study reduced the skin absorption of hydrocortisone, compared with the conventional ointment formulation. The amount of hydrocortisone absorbed from the liposome-gel after 8 h into the SC-removed skin was less than one-third of that from the conventional ointment. In spite of the reduced absorption, higher and sustained skin concentrations of hydrocortisone were achieved for the liposome-gel as compared to the ointment. Drug concentration in both viable and deep skin reached its maximum within 0.5 h after application of both formulations to both skin types. Drug concentrations in both skins from the ointment declined as a function of time, while those from the liposome-gel were greatly sustained. The sustainment by the liposome-gel was more remarkable in the viable skin than in the deep skin. Drug concentration in the viable skin could be maintained at a nearly constant level for over 8 h by applying the liposome-gel. As a result, a 5-fold higher viable skin drug concentration was obtained from the liposome-gel than from the ointment at 8 h after the application to the SC-removed skin. Nevertheless, the plasma concentration of hydrocortisone at 4 h from the liposome-gel was only one-fourth (p<0.01) the value from the ointment when the drug was applied to the SC-removed skin. Thus, retarded diffusion of the drug from the skin to the systemic blood stream appears to be a potential factor in the sustained skin concentration of hydrocortisone from the liposome-gel. The retarded diffusion was supported by the lower urinary (one-third, p<0.05) and fecal (one-half, p<0.05) excretion of the drug from the liposome-gel as compared to the ointment when the drug was applied to SC-removed skin. Interaction of hydrocortisone in the skin with phosphatidylcholine, a component of the liposomes and skin, may well be a factor in retarding the diffusion of the drug in the skin." @default.
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• W2015217412 date "1997-06-02" @default.
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• W2015217412 title "Targeted and sustained delivery of hydrocortisone to normal and stratum corneum-removed skin without enhanced skin absorption using a liposome gel" @default.
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• W2015217412 doi "https://doi.org/10.1016/s0168-3659(96)01604-5" @default.
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