摘要 : A combination method of using microneedle pretreatment and elastic liposomes was developed to increase skin permeation of drugs with high molecular weight and poor water solubility Docetaxel (DTX, MW = 807.9) was chosen as a model... 展开 A combination method of using microneedle pretreatment and elastic liposomes was developed to increase skin permeation of drugs with high molecular weight and poor water solubility Docetaxel (DTX, MW = 807.9) was chosen as a model drug. DTX liposomal systems with and without elastic properties were prepared and characterized. The effect of the developed formulations on the permeation of DTX across both rat and porcine skin was investigated in vitro. The combination effect of microneedle pretreatment and elastic liposomes on the permeability of DTX was evaluated using porcine skin in vitro. The following results were obtained: (1) Elastic liposomes loaded with DTX can enhance transdermal delivery of DTX without microneedle treatment. (2) An enhanced transdermal flux (1.3-1.4 mu g/cm(2)/h) for DTX from all liposomal formulations was observed after microneedle treatment. Importantly, the lag time obtained following the application of elastic liposomes through microneedle-treated skin was decreased by nearly 70% compared with that obtained from conventional liposomes. These results suggest that the combination of elastic liposomes with microneedle pretreatment can be a useful method to increase skin permeation of drugs with high molecular weight and poor water solubility. (C) 2008 Elsevier B.V. All rights reserved. 收起