Awareness rate and influencing factors of elderly cancer patients in a community of Shanghai / 上海预防医学

ObjectiveTo explore the awareness rate and the influencing factors of notification in elderly cancer patients， and to improve the community health management. MethodsA total of 622 cancer patients were selected from a community health service center in Jing’an District of Shanghai， who participated in the Survey of Unified Needs Assessment of Elderly Care in Shanghai. ResultsThe overall awareness rate was 62.86%. Multivariate analysis showed that elderly patients were more likely to have disease notification than younger patients. Patients were less likely to have notification if they were without spouse， with care needs and with more diseases other than cancer. Patients with family history of cancer， living with children were more likely to have notification （P< 0.05）. Different tumor types might also influence the notification. Moreover， under the control of different factors， the influence effect on patients in specific age group may be different. （This sentence， in Chinse and English abstracts is confusing. Suggest authors to revise） ConclusionCommunity workers should develop corresponding health management strategies to improve the patients’ proper awareness， based on tumor category， of patient health status and family attitude.

Awareness rate and influencing factors of elderly cancer patients in a community of Shanghai / 上海预防医学

ObjectiveTo explore the awareness rate and the influencing factors of notification in elderly cancer patients， and to improve the community health management. MethodsA total of 622 cancer patients were selected from a community health service center in Jing’an District of Shanghai， who participated in the Survey of Unified Needs Assessment of Elderly Care in Shanghai. ResultsThe overall awareness rate was 62.86%. Multivariate analysis showed that elderly patients were more likely to have disease notification than younger patients. Patients were less likely to have notification if they were without spouse， with care needs and with more diseases other than cancer. Patients with family history of cancer， living with children were more likely to have notification （P< 0.05）. Different tumor types might also influence the notification. Moreover， under the control of different factors， the influence effect on patients in specific age group may be different. （This sentence， in Chinse and English abstracts is confusing. Suggest authors to revise） ConclusionCommunity workers should develop corresponding health management strategies to improve the patients’ proper awareness， based on tumor category， of patient health status and family attitude.

A combination of receptor mediated transcytosis and photothermal effect promotes BBB permeability and the treatment of meningitis using itraconazole.

Fungal infections of the central nervous system (CNS) may lead to life-threatening meningitis. Itraconazole (ITZ) is an effective antifungal agent that can be used to treat various fungal infections; however, its poor solubility along with poor permeability of the blood-brain barrier (BBB) prevents it from treating meningitis. Receptor mediated transcytosis (RMT) shows modest efficacy in BBB crossing, while affinity and saturability of interactions between ligands and receptors account for the limited efficacy of RMT in crossing the BBB. Mild hyperthermia could temporarily disrupt the BBB to increase its permeability. Therefore, we speculated that the combination of mild hyperthermia with RMT could potentially increase BBB permeability of ITZ leading to improved efficacy in fungal meningitis. Here, we have constructed for the first time, apolipoprotein E (Apo E) mimicked peptide COG1410 modified polydopamine (PDA)-coated bovine serum albumin nanoparticles (ApoE-PDA@ITZ-NPs). Different levels of COG1410-modified NPs were prepared and characterized. ApoE-PDA@ITZ-NPs have a superior photothermal effect under 808 nm light irradiation and exhibited favorable plasma stability and photothermal stability. Moreover, the cellular uptake of nanoparticles increased with an increase in COG1410. H-ApoE-PDA@ITZ-NPs increased cellular uptake and in vitro BBB permeability by 4.2-fold and 4.8-fold, respectively, compared to the ITZ-NPs. Live imaging implied that H-ApoE-PDA@ITZ-NPs could significantly increase the distribution of ITZ in the brain under 808 nm light irradiation. Histopathological analysis of periodic acid-Schiff-stained brain sections of the H-ApoE-PDA@ITZ-NP treated C. albicans meningitis model indicated that H-ApoE-PDA@ITZ-NPs showed superior antifungal activity after 808 nm light irradiation. Hence, we report ApoE-PDA@ITZ-NPs in tandem with 808 nm irradiation as a novel strategy of RMT combination with a photothermal effect in enhancing BBB permeability to facilitate drug accumulation in the brain region and enhance the therapeutic efficacy of ITZ in meningitis.

Effects of keto acid supplements on Chinese patients receiving maintenance hemodialysis: a prospective, randomized, controlled, single-center clinical study / 中华医学杂志(英文版)

BACKGROUND@#The effects of keto acid (KA) supplements on Chinese patients receiving maintenance hemodialysis (MHD) are unclear. This study aimed to evaluate the effects of KA supplementation on nutritional status, inflammatory markers, and bioelectric impedance analysis (BIA) parameters in a cohort of Chinese patients with MHD without malnutrition.@*METHODS@#This was a prospective, randomized, controlled, single-center clinical study conducted in 2011 till 2014. Twenty-nine patients with MHD were randomly assigned to a control (n = 14) or a KA (n = 15) group. The control group maintained a dietary protein intake of 0.9 g/kg/day. The KA group received additional KA supplement (0.1 g/kg/day). BIA was used to determine the lean tissue mass, adipose tissue mass, and body cell mass. The patients' nutritional status, dialysis adequacy, and biochemical parameters were assessed at the ends of the third and sixth months with t test or Wilcoxon rank-sum test.@*RESULTS@#The daily total energy intake for both groups was about 28 kcal/kg/day. After 6 months, the Kt/V (where K is the dialyzer clearance of urea, t is the dialysis time, and V is the volume of the distribution of urea) was 1.33 ± 0.25 in KA group, and 1.34 ± 0.25 in the control group. The median triceps skin-fold thickness in KA group was 12.00 and 9.00 mm in the control group. In addition, the median hand-grip strength in KA group was 21.10 and 25.65 kg in the control group. There were no significant differences between the groups with respect to the anthropometry parameters, dialysis adequacy, serum calcium and phosphorus levels, inflammatory markers, and amino-acid profiles, or in relation to the parameters determined by BIA. Both groups achieved dialysis adequacy and maintained nutritional status during the study.@*CONCLUSIONS@#In this cohort of Chinese patients with MHD, the patients in the control group whose dietary protein intake was 0.9 g/kg/day and total energy intake was 28 kcal/kg/day, maintained well nutritional status during study period. The KA supplement (0.1 g/kg/day) did not improve the essential amino acid/non-essential amino acid ratio, nor did it change the patients' mineral metabolism, inflammatory parameters, or body compositions.

Relationship between the APOE genotypes and the common major psychosis / 上海交通大学学报（医学版）

Apolipoprotein E (APOE) is a lipid transfer protein, which plays an important role in maintaining the stabilization of nerve and recovering. Alzheimer's disease (AD) is a neurodegenerative disorder. Most studies showed that APOE genotypes were closely related with AD. In clinical practice, AD is mainly manifested as progressive cognitive decline, and often accompanied by mental behavioral symptoms. These symptoms also exist in common severe mental illness. It is worth thinking about the correlation between APOE genotypes and these diseases. This article reviewed the relationship between the APOE genotypes and the common major psychosis.

Relationship between the APOE genotypes and the common major psychosis / 上海交通大学学报（医学版）

Apolipoprotein E (APOE) is a lipid transfer protein, which plays an important role in maintaining the stabilization of nerve and recovering. Alzheimer's disease (AD) is a neurodegenerative disorder. Most studies showed that APOE genotypes were closely related with AD. In clinical practice, AD is mainly manifested as progressive cognitive decline, and often accompanied by mental behavioral symptoms. These symptoms also exist in common severe mental illness. It is worth thinking about the correlation between APOE genotypes and these diseases. This article reviewed the relationship between the APOE genotypes and the common major psychosis.

Mitochondria-targeted drug delivery system for cancer treatment.

Mitochondria are one type of the major organelles in the cell, participating in a variety of important physiological and biochemical processes, such as tricarboxylic acid cycle, fatty acid metabolism and oxidative phosphorylation. Meanwhile, it also happens to be the key regulator of apoptosis by triggering the complex cell-death processes through a variety of mechanisms. Since it plays a pivotal role in cell-death, a mitochondria-targeted treatment strategy could be promising for cancer therapy. In this comprehensive review, we focused on the mechanisms of mitochondrial targeting and a variety of strategies to realize the purpose of mitochondrial targeting, including that based on the use of lipophilic cations, and mitochondrial targeting signal peptides (MTS) as well as cell-penetrating peptides (CPPs). Then on this basis we present some several developed strategies for multifunctional mitochondria-targeted agents so as to achieve the good anti-cancer therapeutic effects.

Conversion of mild cognitive impairment to dementia among subjects with diabetes: a population-based study of incidence and risk factors with five years of follow-up.

Type 2 diabetes mellitus (T2DM) is associated with dementia. Mild cognitive impairment (MCI) is a key determinant in this association. It is not clear whether T2DM increases the risk of conversion from MCI to dementia. We plan to explore the relationship between T2DM-MCI and dementia and identify its potential risk factors. A prospective community-based cohort study was conducted from March 2010 to March 2014, including 634 participants with T2DM-MCI, 261 T2DM participants who were cognitively intact, and 585 MCI participants without diabetes. All cohort members received detailed annual evaluations to detect dementia onset during the 5 years of follow-up. The three cohorts were compared to assess differences in dementia onset. Furthermore, Cox proportional hazards regression was used to identify risk factors for dementia onset in the T2DM-MCI cohort. During follow-up, 152 and 49 subjects developed dementia in the MCI and cognitively-intact cohorts, amounting to an adjusted hazard ratio (HR) of 1.66 (95% CI 1.07-2.26). In a survival analysis of the cohorts, MCI accelerated the median progression to dementia by 2.74 years. In a multivariable analysis of the T2DM-MCI cohort, major risk factors for dementia were age >75 years and longer durations of diabetes, while significantly reduced risks of dementia were associated with oral hypoglycemic agents and HMG-CoA reductase inhibitors. Insulin was not associated with significantly changed risk. T2DM-MCI may aggravate the clinical picture as a concomitant factor. To minimize progression to dementia, it may be worthwhile to target several modifiable diabetes-specific features, such as the duration of disease, glycemic control, and antidiabetic agents.

Pharmacokinetics of orally disintegrating tablets of perphenazine/hydroxypropyl-beta-cyclodextrin inclusion complex in rabbits.

We investigated the pharmacokinetic behavior of orally disintegrating tablets (ODTs) containing perphenazine/hydroxypropyl-beta-cyclodextrin inclusion complex (PPZ/HP-beta-CD) in rabbits and evaluated their bioequivalence with conventional tablets. In this study, a simple, sensitive and accurate high performance liquid chromatography method was developed for the determination of perphenazine concentration in rabbit plasma. The pharmacokinetic parameters were calculated by non-compartmental methods and the bioequivalence between PPZ/HP-beta-CD ODTs with conventional tablets was determined by calculating 90% confidence interval (CI) for the ratio of logarithmic transformed C(max), AUC(0-t), AUC(0-infinity) values. The pharmacokinetic parameters of test ODTs and reference tablets were as follows: C(max), 82.86 and 62.71 ng/mL; AUC(0-24), 480 and 397.56 ng/mL/h; AUC(0-infinity), 505 and 400.12 ng/mL/h; T(max), 1.04 and 3.83h. The relative bioavailabilities of two formulations for AUC(0-t) and AUC(0-infinity) were 120.77% and 126.37%, respectively. The 90% CI statistical analysis demonstrated the two formulations were not bioequivalence. In conclusion, the ODTs showed faster absorption and higher peak concentration when compared with conventional tablets, which suggests ODTs could be promising oral formulations for PPZ.

Development of brucine-loaded microsphere/thermally responsive hydrogel combination system for intra-articular administration.

Intra-articular drug delivery system could directly deliver a drug to an affected joint and offer the possibility of reaching high drug concentrations at the site of action with limited systemic toxicity. However, depending on their chemical structure, some active compounds were rapidly cleared from the joint, thus requiring numerous injections, which could cause infection or joint disability. To control the release behavior for prolonged time periods, a novel biologically based drug delivery vehicle was designed for intra-articular using microsphere/thermally responsive hydrogel combination system in this paper. And brucine was the test drug. The system was constructed by dispersing the brucine microspheres which was prepared by using a spray-drying method in a thermally responsive biopolymer hydrogel contained with chitosan-glycerol-borax. The microspheres were spherical as evidenced by the scanning electron microscopy (SEM) photographs. And the entrapment rate was 98.60% w/w with an average size range of 0.9-4.5 µm. Fourier transforms infrared (FT-IR) spectroscopy and X-ray diffraction (XRD) revealed the absence of drug-polymer interaction and amorphous nature of an entrapped drug. From the in vitro drug release study we could see that there was a burst release of microsphere, which was obviously retarded when dispersed in hydrogel. And the studies of biocompatibility with synovium showed that no apparent thickening or hyperplasia of the synovium, a small quality of phlogocyte imbibitions was observed. The results of FX imaging in rats showed that by intra-articular injection the BMH could stay in articular for over 7 days were consistent with our in vitro release. And the results of pharmacodynamics revealed the BMH could benefit OA joint by suppressing the levels of TNF-α and IL-1ß, protect the damaged joint from degradation. The novel microsphere/thermoresponsive hydrogel combination system could be a promising treatment option for OA and RA. In conclusion, the system appears to be generally biocompatible with synovium and could control the drug release for several days; hence it might be suitable for the development of treatment strategies for rheumatic diseases.

Novel materials which possess the ability to target liver cells.

INTRODUCTION: Hepatic-targeted drug delivery systems are designed to treat diseases of the liver. However, since there are several different types of liver diseases that are caused by different cells, it is important to select the proper materials to target these different cells. AREAS COVERED: This review addresses novel materials that possess the ability to target liver cells via receptor-ligand processes and offers an insight into the aspects of formulation design. It also discusses several approaches used to enhance the targeting efficiency of drug delivery systems to receptors in the liver cells. In addition, the delivery efficiency and therapeutic efficacy of these materials in the treatment of acute or chronic liver diseases is highlighted. EXPERT OPINION: Further research into the use of clinical materials and the design of smart materials for multi-drug delivery to different organelles is important for future studies on these new materials. It is hoped that these targeted therapeutics will benefit patients with liver disorders in the near future.

Effects of exogenous carnitine on function of respiratory chain and antioxidant capacity in mitochondria of myocardium after exhaustive running in rats / 中国应用生理学杂志

<p><b>OBJECTIVE</b>To investigate the effect of exogenous carnitine on function of respiratory chain and antioxidant capacity in mitochondria of myocardium in rats.</p><p><b>METHODS</b>Forty male Wistar rats were randomized to 4 groups (n = 10): static control (C), supplementation of carnitine (LC), exercise-training (T) and training with supplementation of carnitine (TLC). LC and TLC animals were perfused carnitine by the dose of 300 mg/kg bw x d. T and TLC animals were forced to performed 6-week treadmill training. Heart were prepared immediately after exhaustive running. Myocardium mitochondria was extracted by differential centrifugation. Spectrophotometric analysis was used to evaluate activities of respiratory chain complex (C) I -IV and superoxide dismutase (SOD), malondialdehyde (MDA) level in myocardium mitochondria.</p><p><b>RESULTS</b>To compare with C group, C I and C IV activity in LC, T and TLC group were increased significantly (P < 0.05, P < 0.01), CII and C III activity in T and TLC group were increased significantly (P < 0.05, P < 0.01); to compare with LC group, C I - IV activity in TLC group were increased significantly (P < 0.05, P < 0.01); to compare with T group, CI and C IV activity in TLC group increased significantly (P < 0.05). To compare with C group, SOD activity increased remarkably, MDA was remarkably lower (P < 0.05, P < 0.01) in LC, T and TLC group; To compare with LC and T group, SOD activity increased remarkably, MDA was remarkably lower (P < 0.05) in TLC group.</p><p><b>CONCLUSION</b>Carnitine and training could improve function of respiratory chain and increased antioxidant capacity in myocardium mitochondria, there was better function of cooperation between carnitine and training.</p>

[Water in oil microemulsions containing NaCl for transdermal delivery of fluorouracil].

This study is to prepare the W/O microemulsion containing NaCl and fluorouracil (5-Fu) as a model drug to investigate the transdermal characteristics and skin irritation of the microemulsion in vitro. Isopropylmyristate (IPM) acting as oil phase, Aerosol-OT (AOT) as surfactant, Tween 85 as cosurfactant, NaCl solution was added dropwise to the oil phase to prepare W/O microemulsion at room temperature using magnetic stirring, and then 5-Fu powder was added. According to the area of microemulsion based on the pseudo-tertiary phase diagrams, the optimum formulation was screened initially. And the permeation flux of fluorouracil across excised mice skin was determined in vitro using Franz diffusion cells to study the influence of the amount of water and the drug loading capacity and optimize the formulation further. Refer to 5-Fu cream, the irritation of microemulsion on the rat skin was studied. The optimum formulation was composed of 0.7% (w/v) 5-Fu, 50% NaCl solution (0.05 mol x L(-1)), 20% mix-surfactant (AOT/Tween 85, K(m) = 2) and 29.3% oil (IPM). The cumulative amount of fluorouracil permeated in 12 h was (2 013.4 +/- 41.6) microg x cm(-2), 20.23 folds and 10.38 folds more than 0.7% fluorouracil aqueous solution and 2.5% (w/w) fluorouracil cream, respectively. Microemulsion exhibited some irritation, but could be reversed after drug withdrawal. The addition of NaCl significantly increased the content of water and the drug loading in microemulsion systems. The NaCl/AOT-Tween 85/IPM microemulsion system promoted the permeation of fluorouracil greatly, which may be a promising vehicle for the transdermal delivery of fluorouracil and other hydrophilic drug.

[Study on the pharmacokinetics Oxytropis falcate total flavonoids ointment in rats].

OBJECTIVE: To study the pharmacokinetics of Oxytropis falcate total flavonoids ointment after transdermal administration in rats. METHODS: The content of 2',4'-dihydroxychalcone (TFC) in plasma was determined by high performance liquid chromatography. The concentration was determined at various time and the data was processed by 3P97. RESULTS: TFC behaved as a one-compartment and a two-compartment model after transdermal administration of total Oxytropis falcate total flavonoids ointment and solution, respectively. And the C(max) of ointment was improved about 3 times compared with that of the solution. CONCLUSION: The results show that the ointment possesses sustained release property and significantly prolong the degradation half life of TFC. The ointment is benefit to improve the analgesic and anti-inflammatory activity after transdermal administration.

The studies of anti-inflammatory and analgesic activities and pharmacokinetics of Oxytropis falcate Bunge extraction after transdermal administration in rats.

The aim of this study was to evaluate the activities of anti-inflammatory and analgesic of the total flavonoids extraction from Oxytropis falcate Bunge (FEO) after transdermal administration. The pharmacokinetics and absolute bioavailability of FEO in rat, furthermore, was studied. Firstly, the anti-inflammatory and analgesic effects of the FEO were studied by xylene-induced ear edema, adjuvant-induced joint inflammation law in rats, acetic acid-induced writhing and hot-plate tests in mice. Secondly, we developed a sensitive and specific HPLC method to analyze 2', 4'-dihydroxychalcone (TFC, the mainly ingredient of FEO) in rat plasma to study the pharmacokinetic of TEC. The results showed FEO has anti-inflammatory and analgesic property in a dose-dependent manner, and that the high dose group (90.6 mg/kg) of FEO appeared more significantly effective than the positive drug. From the pharmacokinetic studies of TFC in rats, we got the main pharmacokinetic parameters of TFC, providing a basis for the future studies in clinic.

Effect of pinocembrin on brain mitochondrial respiratory function / 药学学报

There are growing evidences that pinocembrin has better neuroprotective effect. In the present study, the effect of pinocembrin on mitochondrial respiratory function was evaluated in global brain ischemia/ reperfusion (4-vessel occlusion, 4-VO) rats. The results showed that pinocembrin improved the respiratory activity of 4-VO brain mitochondria, through increasing ADP/O, state 3 respiration state (V3), respiration control rate index (RCI) and oxidative phosphorylation rate (OPR). And then, the effect of pinocembrin on brain mitochondria was verified in vitro. The results showed that pinocembrin increased ADP/O, state 3 respiration state, respiration control rate index, oxidative phosphorylation rate in NADH/FADH2 dependent respiratory chain and decreased state 4 respiration state (V4) in NADH dependent respiratory chain. Pinocembrin improved ATP content in brain mitochondria in vitro and in SH-SY5Y cells.

Absorption dynamic characteristics of clopidogrel bisulfate polymorphs in rat / 药学学报

Four crystalline forms of clopidogrel bisulfate were characterized by analytical techniques. Aiming to research the absorption characteristics of clopidogrel bisulfate polymorphs after taken orally by rat, and to estimate the influence of crystal form to pharmacodynamic action, four crystalline forms of clopidogrel bisulfate were administered intragastrically to rats, and high performance liquid chromatography (HPLC) was used to measure the contents of clopidogrel bisulfate and its metabolite in rat plasma. The metabolite of clopidogrel bisulfate was detected in rat plasma. There were significant deviations among four crystalline forms in the areas under curve of the metabolite of clopidogrel bisulfate. We concluded that the different crystal forms of clopidogrel bisulfate showed different pharmacokinetic characteristics, which might affect pharmacodynamic action.

Comparative pharmacokinetics and bioavailability studies of quercetin, kaempferol and isorhamnetin after oral administration of Ginkgo biloba extracts, Ginkgo biloba extract phospholipid complexes and Ginkgo biloba extract solid dispersions in rats.

The aim of this study was to improve the oral bioavailability of Ginkgo biloba extract (GBE) through preparing G. biloba extract phospholipid complexes (GBP) and G. biloba extract solid dispersions (GBS). Firstly we prepared the GBP and GBS and studied their physicochemical properties by differential scanning calorimetry (DSC), powder X-ray diffraction (XRD) and dissolution. Then we studied the pharmacokinetic characteristics and bioavailability in rats. The results showed that the bioavailability of quercetin, kaempferol and isorhamnetin in rats was increased remarkably after oral administration of GBP and GBS comparing with GBE. The bioavailabilities of GBP increased more than that of GBS.

Synthesis of a novel polymer bile salts-(polyethylene glycol)2000-bile salts and its application to the liver-selective targeting of liposomal DDB.

PURPOSE: The objective of this study was to achieve a sustained and targeted delivery of liposome to the liver, by modifying the phospholipid [phosphatidylcholine (PC)/cholesterol (10 : 1) liposomes with a novel polymer bile salts-(polyethylene glycol)(2000)-bile salts (BP(2)B). METHODS: First, we generated a novel BP(2)B by N,N'-dicyclohexylcarbodiimide/4-dimethylaminopyridine esterification method and confirmed by Fourier transform infraredand (1) H-NMR spectra. Second, we prepared the BP(2)B-modified liposomes (BP(2)BL) that included BP(2)B, and the effect of the weight ratios of BP(2)B/PC on entrapment efficiency was investigated and BP(2)B/PC = 3% (w/w) was determined as the optimum ratio for the 4,4'-dimethoxy-5,6,5',6'-bi (methylenedioxy)-2,2'-bicarbomethoxybiphenyl liposomes. And then, the ability of the liver target of BP(2)BL was studied by calculating the targeted parameters. RESULTS AND DISCUSSION: All the results revealed that the introduction of polyoxyethylene chains could control interactions of bile salt moieties on liposome surfaces with the receptor compared with traditional liposomes (CL), marking BP(2)BL as a suitable carrier for hepatic parenchymal cell-specific and sustained targeting. It was suggested that liposomes containing such novel BP(2)B have great potential as drug delivery carriers for the liver-selective targeting that has targeted and sustained drug delivery.

[Microemulsion-based gel of fluorouracil for transdermal delivery].

This study is to prepare the microemulsion-based gel based on the W/O microemulsion and fluorouracil (5-Fu) as a model drug to study the transdermal characterization and observe its skin irritation of the microemulsion-based gel in vitro. IPM acted as oil phase, AOT as surfactant, Tween 85 as cosurfactant, water was added dropwise to the oil phase to prepare W/O microemulsion at room temperature using magnetic stirring, then 5-Fu powder was added. The gelatin was used as substrate to prepare 5-Fu microemulsion-based gel. The permeation flux of 5-Fu from 5-Fu microemulsion-based gel across excised mice skin was determined in vitro using Franz diffusion cell to study the influence of the amount of gelatin and the drug loading capacity. Refer to 5-Fu cream, the irritation of microemulsion and microemulsion-based gel on the rat skin was studied. Based on the water/AOT/Tween 85/IPM microemulsion, only the gelatin can form the microemulsion-based gel. At 25 degrees C, 32 degrees C and 40 degrees C, the amount of gelatin required for the formation of microemulsion-based gel were 7%, 14% and more than 17%, respectively. The 12 h transdermal cumulated permeation amount of 5-Fu from microemulsion-based gel containing 14% gelatin and 0.5% drug loading were (876.5 +/- 29.1) microg x cm(-2), 12.3 folds and 4.5 folds more than 0.5% 5-Fu aqueous solution and 2.5% (w/w) 5-Fu cream, respectively. Microemulsion-based gel exhibited some irritation, but could be subsided after drug withdrawal. Microemulsion-based gel may be a promising vehicle for transdermal delivery of 5-Fu and other hydrophilic drug.