Transdermal delivery of imipramine and doxepin from newly oil-in-water nanoemulsions for an analgesic and anti-allodynic activity: Development, characterization and in vivo evaluation

Sandig, A. Gimeno; Campmany, Ana Cristina Calpena; Campos, Francisco; Villena, María J. Martín; Naveros, Beatriz Clarés

doi:10.1016/j.colsurfb.2012.10.061

Cited by 43 publications

(17 citation statements)

References 27 publications

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“…(2). Taking into account a doxepin plasmatic clearance (Cl p ) of 1000 mL/min (Sandig et al, 2013), and using the J s previously calculated (Table 1), the median plasma concentration under steady-state conditions was calculated to be 46 ng/mL. According to these theoretical data, small amounts of the topical dose applied would be absorbed, and serum concentrations would be significantly below the therapeutic range for a potential central nervous system activity as tricyclic agent (150-250 ng/mL) (Drake et al, 1999;Demling, 2001).…”

Section: Resultsmentioning

confidence: 99%

“…The system consisted of a Waters 515 pump (Waters, Milford, MA, USA) with UV-vis 2487 detector (Waters, Milford, MA, USA) set at 235 nm. Doxepin was detected with a retention time of 4.6 min with a reverse-phase C18 Sunfire 1 column (4.6 mm Â 150 mm, Waters Associates, Milford, MA, USA) using as mobile phase methanol/ (acetate buffer pH 6.0/water (36/64, v/v)) (72/28, v/v), pumped at 1 mL/min flux rate (Sandig et al, 2013).…”

Section: Drug Assaymentioning

confidence: 99%

“…The role of antidepressant in the management of different pain syndromes has elicited considerable interest (Sandig et al, 2013). Among them, doxepin belongs to the tricyclic antidepressant family.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Transbuccal delivery of doxepin: Studies on permeation and histological investigation

Gimeno

Calpena

Sanz

et al. 2014

International Journal of Pharmaceutics

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Section: Resultsmentioning

confidence: 99%

Section: Drug Assaymentioning

confidence: 99%

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Transbuccal delivery of doxepin: Studies on permeation and histological investigation

Gimeno

Calpena

Sanz

et al. 2014

International Journal of Pharmaceutics

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“…The aliquots (1 ml) from the buffer media were withdrawn at time intervals (0.5, 1, 2, 4, 6, 8, 10, 12, 14, 16, 24 h.) and replaced immediately with a similar volume (1 ml) of fresh medium. The withdrawal samples were filtered using membrane filter (0.45 µm) and the drug content was determined using HPLC [27].…”

Section: In Vitro Permeation Ex-vivo Skin Permeation and Skin Retentmentioning

confidence: 99%

Nanoemulsion Gel of Nutraceutical Co-Enzyme Q10 as an Alternative to Conventional Topical Delivery System to Enhance Skin Permeability and Anti-Wrinkle Efficiency

Leithy

Makky

Khattab

et al. 2017

Int J Pharm Pharm Sci

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Objective: The object of our investigation was to develop and characterize nanoemulsion gel (NEG) as transdermal delivery systems for the poorly water soluble drug, Co-enzyme Q10 (Co Q10), to improve its solubility and skin permeability and thus improving its anti-wrinkle efficiency.Methods: An optimized nanoemulsion (NE) formula was chosen according to its particle size and stability and converted into nanoemulsion gel using different gelling agents, including; carbopol 934 (1%), xanthan gum (2%) and sodium carboxymethyl cellulose(NaCMC) (2%). Drug loaded nanoemulsion gels were characterized for particle size, zeta potential, viscosity and rheological behavior, conductivity, spreadability, drug content and permeation studies using Franz diffusion cell.Results: NEG containing 10% w/v isopropyl myristate (IPM) as oil, 60% w/v tween 80 and transcutol HP as surfactant/co-surfactant mixture (S/CoS), 30%w/v water, 2%w/v drug, and 1% w/v carbopol 934 as gelling gent was concluded as an optimized NEG formula. It exhibited pH, viscosity, drug content, particle size, zeta potential, polydispersity index(PDI) and spreadability, as 5.4±0.011, 27588±2034.34 cps,101.51±0.93%,120.5±1.19 nm,-29.8±1.46, 0.273 and 6.16±0.28 cm, respectively. Also, it showed significantly higher cumulative amount of drug permeated through dialysis membrane (281.71±0.97μg/cm 2 ) and through rat skin (20.73±2.5 μg/cm 2 ) than the other formulae and marketed formulation (P<0.001). In addition, its permeability parameters like drug flux (Jss), enhancement ratio (Er) and permeability coefficient (Kp) exhibited the highest values; 12.79µg/cm 2 /h, 95.92×10 -4 cm 2 /h and 57.35, respectively for in vitro permeation study and 0.968µg/cm 2 /h, 7.26×10 -4 cm 2 /h and 1.183, respectively for ex-vivo permeation study.Further histopathological evaluation test showed that CoQ10 NEG has a good anti-wrinkle efficacy compared to the conventional topical dosage form. Conclusion:These results judged NEG to be a promising alternative carrier for topical delivery of Co Q10 to enhance its solubility, skin permeability and thus anti-wrinkle efficiency.

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“…An alternative approach to this is the topical administration of analgesics. Currently, the possibility of the topical use of these drugs that have local analgesic effects has been proposed [9][10][11][12][13][14], but there is little data regarding antidepressant topical coadministration with morphine and the nature of the interaction between morphine and either doxepin or venlafaxine, two antidepressant drugs that have been recently used in neuropathic pain therapies.…”

Section: Introductionmentioning

confidence: 99%

Analgesic effects of antidepressants alone and after their local co-administration with morphine in a rat model of neuropathic pain

Jagła

Mika

Makuch

et al. 2014

Pharmacological Reports

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(2014) 'Analgesic eects of antidepressants alone and after their local co-administration with morphine in a rat model of neuropathic pain.', Pharmacological reports., 66 (3). pp. 459-465. Further information on publisher's website: Additional information: Use policyThe full-text may be used and/or reproduced, and given to third parties in any format or medium, without prior permission or charge, for personal research or study, educational, or not-for-prot purposes provided that:• a full bibliographic reference is made to the original source • a link is made to the metadata record in DRO • the full-text is not changed in any way The full-text must not be sold in any format or medium without the formal permission of the copyright holders.Please consult the full DRO policy for further details. IntroductionNeuropathic pain is defined as pain arising as a direct consequence of a lesion or disease affecting the somatosensory system [1]. The most frequent etiologic factors of neuropathic pain are trauma (including post-surgery scars), metabolic disturbances (e.g., diabetes mellitus) and ischemia. The pathological mechanism of neuropathic pain differs significantly from that of inflammatory pain; studies have shown that the changes in spinal gene expression under neuropathy and inflammations are different [2]. Thus, the response to antinociceptive drugs, especially opioids, is not the same. It has generally been accepted that neuropathic pain is somewhat resistant to morphine administration in clinical studies [3,4], and the reduced ability of morphine to attenuate allodynia and hyperalgesia in experimental models of neuropathic pain has been demonstrated [5][6][7][8]. For these reasons, it is a common clinical practice to use analgesic drug combinations. The primary approach to treat neuropathic pain is the use of coanalgesics such as tricyclic antidepressants (TCA); however, their systemic application is associated with significant side effects, which can hinder the desired analgesic effect. An alternative approach to this is the topical administration of analgesics. Currently, the possibility of the topical Background:The therapy of neuropathic pain may include the use of co-analgesics, such as antidepressants, however, their desired analgesic effect is associated with significant side effects. An alternative approach to this is their local administration which has been proposed, but there is little data regarding their local co-administration with morphine and the nature of the interaction between morphine and either doxepin or venlafaxine, two antidepressant drugs that have been recently used in neuropathic pain therapies. Methods: This study was performed on rats after chronic constriction injury (CCI) to the sciatic nerve. The von Frey and Hargreaves' tests were used to assess mechanical allodynia and thermal hyperalgesia, respectively, after intraplantar (ipl) or subcutaneous (sc) administration of amitriptyline, doxepin, or venlafaxine, or their ipl co-administration with morphine on day 12-16 after inj...

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Transdermal delivery of imipramine and doxepin from newly oil-in-water nanoemulsions for an analgesic and anti-allodynic activity: Development, characterization and in vivo evaluation

Cited by 43 publications

References 27 publications

Transbuccal delivery of doxepin: Studies on permeation and histological investigation

Transbuccal delivery of doxepin: Studies on permeation and histological investigation

Nanoemulsion Gel of Nutraceutical Co-Enzyme Q10 as an Alternative to Conventional Topical Delivery System to Enhance Skin Permeability and Anti-Wrinkle Efficiency

Analgesic effects of antidepressants alone and after their local co-administration with morphine in a rat model of neuropathic pain

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