Article

The Effect of Clove Oil on the Transdermal Delivery of Ibuprofen in the Rabbit by In Vitro and In Vivo Methods

School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China.
Drug Development and Industrial Pharmacy (Impact Factor: 2.1). 01/2008; 33(12):1369-74. DOI: 10.1080/03639040701399346
Source: PubMed

ABSTRACT

The study was designed to evaluate skin permeation enhancement effect of essential oils from Eugenia caryophyllata (clove oil) in rabbits and to compare the in vitro absorption and in vivo permeation using ibuprofen as a model drug. The in vitro results indicated a significant permeation enhancement effect of the clove oil. The group with 1% oil appeared to the flux (239 microg/cm(2)/hr), and 3% oil was 293 microg/cm(2)/hr to some extent similar with 2% azone group (327 microg/cm(2)/hr). The enhancement ratio of clove oil was 7.3. In vivo results also demonstrated that clove oil showed a significant permeation enhancement effect, but the enhancement of clove oil was relatively weak than in vitro. The group with 3% oil exhibited the higher value of area under the curve (AUC) of 80.8 microg/mL.hr, which was 2.4 times the high of control. The AUC value of 3% oil group was similar to that of 2% azone group (89.8 mug/mL.hr). The GC-MS results indicated eugenol and acetyleugenol identified from clove oil might mainly contribute to enhance in vitro and in vivo absorption of ibuprofen because of its large quantities (90.93%).

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    • "Therefore, it is indispensable to employ PE to increase the skin permeation of ibuprofen in order to maintain an effective blood level. Among the five EOs, only Clove oil had been evaluated as PE for TDD of ibuprofen hydrogel and the AUC values was increased by 2.4 times compared to the control[21]. In the present study, five analgesic EOs were compared as PE. "
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    ABSTRACT: The present study was conducted to evaluate and compare five essential oils (EOs) as penetration enhancers (PEs) to improve the transdermal drug delivery (TDD) of ibuprofen to treat dysmenorrhoea. The EOs were prepared using the steam distillation method and their chemical compositions were identified by GC-MS. The corresponding cytotoxicities were evaluated in epidermal keartinocyte HaCaT cell lines by an MTT assay. Furthermore, the percutaneous permeation studies were carried out to compare the permeation enhancement effect of EOs. Then the therapeutic efficacy of ibuprofen with EOs was evaluated using dysmenorrheal model mice. The data supports a decreasing trend of skin cell viability in which Clove oil >Angelica oil > Chuanxiong oil > Cyperus oil > Cinnamon oil > Azone. Chuanxiong oil and Angelica oil had been proved to possess a significant permeation enhancement for TDD of ibuprofen. More importantly, the pain inhibitory intensity of ibuprofen hydrogel was demonstrated to be greater with Chuanxiong oil when compared to ibuprofen without EOs (p < 0.05). The contents of calcium ion and nitric oxide (NO) were also significantly changed after the addition of Chuanxiong oil (p < 0.05). In summary, we suggest that Chuanxiong oil should be viewed as the best PE for TDD of ibuprofen to treat dysmenorrhea.
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    ABSTRACT: Eugenol, the major constituent of clove oil, has been widely used for its anesthetic and analgesic action in dentistry. Eugenol exhibits pharmacological effects on almost all systems and our aim is to review the research work that has identified these pharmacological actions. Eugenol possesses significant antioxidant, anti-inflammatory and cardiovascular properties, in addition to analgesic and local anesthetic activity. The metabolism and pharmacokinetics of the compound in humans have been studied. Eugenol has also been used as a penetration enhancer. The compound is a very promising candidate for versatile applications, and the design of new drugs based on the pharmacological effects of eugenol could be beneficial.
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    ABSTRACT: Red peppers are part of a group of 20 plant species belonging to the genus Capsicum of the botanical family Solanaceae. The recognition that capsaicin can activate the transient receptor potential ion channel of the vanilloid type (TRPV1) has led to the use of red pepper extracts, capsaicin, and its analogs in pharmacological strategies for treating various medical conditions, especially pain and other neurological conditions. Interest in red pepper and capsaicin for dietary strategies to improve health has increased. The capacity of dietary capsaicin to manage gastrointestinal distress is unclear, because of a lack of understanding of its apparent contradictory actions within various segments of the gastrointestinal tract. More promising is evidence linking capsaicin and red pepper to improving weight loss and weight maintenance as well as lessening glucose intolerance and insulin resistance. However, progress in substantiating these benefits is limited by the need for larger, well-controlled human studies that can characterize capsaicin/red pepper's actions at doses more consistent with typical human intakes. Likewise, insights into both TRPV1-associated and TRPV1-independent mechanisms related to any health benefits of dietary red pepper have only begun to be explored
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