| Summary: | 碩士 === 長庚大學 === 生化與生醫工程研究所 === 98 === The lipophilic drug, curcumin, has low oral bioavailability because of its low solubility and poor stability. By using microemulsion via the transdermal route, a new delivery system was developed to improve curcumin’s delivery. Stratum corneum in skin is the main obstacle in transdermal drug delivery systems. To overcome the stratum corneum barrier, several physical and chemical means to increase the drug penetration have been studied. In this study, a variety of chemical enhancers were screened with the help of Plackett Burman design to evaluate their effects on curcumin transderaml delivery. We found that limonene, geraniol, isopropyl myristate (IPM), isopropanol (IPA), and Dimethyl dioctadecyl ammonium bromide (DDAB)、N-cetyl-N,N,N, trimethyl amoniumbromid (CTAB) had good enhance effects on the percutaneous absorption of curcumin.
Microemulsion.A (ME.A) containing limonene, geraniol, isopropyl myristate isopropanol, DDAB, CTAB, and 6 % tween 80 has a nano-scale particle size (21 nm) and a transparent appearance. Microemulsion.E (ME.E) containing limonene, geraniol, isopropyl myristate, and 6 % tween 80 has a nano-scale particle size (93 nm). By using the in vitro Franz diffusion cells, curcumin loaded Microemulsion.A (ME.A) can penetrate the pig ear skin at a flux up to 98 μg/cm2 in 24 hrs. Microemulsion.E (ME.E) can reach a 82 μg/cm2 in 24 hrs. The DSC thermogram result showed that the intracellular transport is possible mechanism of ME.A and ME.E. We also used cytoxicity irritation test and hemolysis of red blood cells to evaluate the microemulsion(ME) toxicity. These results showed that the developed ME was non-toxicity and stable. However, Oleic acid microemulsion D (OA.D) had a transdermal delivery rate of 27 μg/cm2 in 24 hrs. In our transdermal study. This new delivery system has the potential to be applied to other lipophilic durgs to enhance their solubility and delivery efficiency.
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