Effect of Mixed Micelle Formulations Including Terpenes on the Transdermal Delivery of Diclofenac

Hendradi, Esti; Obata, Yasuko; Isowa, Koichi; Nagai, Tsuneji; Takayama, Kozo

doi:10.1248/bpb.26.1739

Cited by 25 publications

(16 citation statements)

References 7 publications

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“…Moreover, other physical parameters like low molecular weight (369.3) and pharmacological parameters such as poor bioavailability (40-60%), short biological half-life (2-3 h), and low dose (25-50 mg) are favorable for transdermal delivery [9]. Various transdermal delivery systems containing diclofenac have been reported, including patches [8,10], gels [11,12], mixed micelle formulations [13], microemulsion systems [11,[14][15][16][17], nanoemulsions [15] and vesicular systems [18][19][20]. Transdermal delivery of NSAIDs proved to be a convenient route of administration for a variety of clinical indications [21].…”

Section: Introductionmentioning

confidence: 99%

Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation

Ali

Kumar

Ahad

et al. 2015

Journal of Polymer Engineering

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A transdermal therapeutic system (TTS) of diclofenac diethylamine (DDE) was developed to obtain a prolonged controlled drug delivery by the solvent evaporation technique. The matrix diffusion controlled systems used various combinations of hydrophilic (polyvinylpyrrolidone K30) and lipophilic (Eudragit RL 100  and Eudragit RS 100  ) polymers containing dimethyl sulfoxide (DMSO) (0, 5 and 10% w/w) as a penetration enhancer. In vitro drug release was improved with an increased fraction of hydrophilic polymer. Formulation F8 containing Eudragit RL 100 and polyvinylpyrrolidone K30 in the ratio 40:60 presented the highest drug release (92.45%) and permeation rate (0.0988±0.010 mg/cm 2 /h) with sustained release action for 48 h. In vivo pharmacodynamic study of DDE-loaded Eudragit RL 100  transdermal system (formulation F8) showed significant higher percent inhibition of rat paw edema compared with the marketed formulation of the drug. Our results suggest that a developed formulation is an efficient system for transdermal diclofenac delivery against inflammation. The optimized formulation was found to be stable and did not show physicochemical interaction. The system is envisaged to be stable for a sufficiently long period (2.52 years) at room temperature.

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Section: Introductionmentioning

confidence: 99%

Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation

Ali

Kumar

Ahad

et al. 2015

Journal of Polymer Engineering

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“…7,8 This capability has been exploited to use MM as nanocarriers for pharmaceutical purposes. [9][10][11][12][13][14][15][16][17] In this context, we have recently employed photophysical techniques, such as time-resolved fluorescence and laser flash photolysis, to demonstrate encapsulation of several drugs within MM. 18 In a preliminary communication, we have shown that cholic acid (CA) derivatized with a 4-nitrobenzo-2-oxa-1,3-diazole (NBD) chromophore exhibits a significant stereodifferentiation in the quenching by tryptophan (Trp) upon incorporation into sodium cholate (NaCA) aggregates.…”

Section: Introductionmentioning

confidence: 99%

Two-channel dansyl/tryptophan emitters with a cholic acid bridge as reporters for local hydrophobicity within supramolecular systems based on bile salts

2014

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The aim of the present work is to develop two-channel emitters to probe local hydrophobicity by means of fluorescence quenching within different biomimetic supramolecular environments. To achieve this goal, the dansyl (Dns) and tryptophan (Trp) fluorophores have been covalently attached to cholic acid (CA) in order to ensure simultaneous incorporation of the two emitting units into the same compartment. In principle, the two fluorophores of the synthesized Dns-CA-Trp probes could either exhibit an orthogonal behavior or display excited state interactions. The fluorescence spectra of 3β-Dns-CA-Trp showed a residual Trp emission band at ca. 350 nm and an enhanced Dns maximum in the 500-550 nm region. This reveals a partial intramolecular energy transfer, which is consistent with the Dns and Trp singlet energies. Thus, the two photoactive units are not orthogonal; nevertheless, 3β-Dns-CA-Trp seems appropriate as two-channel reporter for the supramolecular systems of interest. Fluorescence quenching of 3β-Dns-CA-Trp by iodide (which remains essentially in bulk water) was examined within sodium cholate, sodium taurocholate, sodium deoxycholate and mixed micelles. Interestingly, a decrease in the emission intensity of the two bands was observed with increasing iodide concentrations. The most remarkable effect was observed for mixed micelles, where the quenching rate constants were one order of magnitude lower than in solution. As anticipated, the quenching efficiency by iodide decreased with increasing hydrophobicity of the microenvironment, a trend that can be correlated with the relative accessibility of the probe to the ionic quencher.

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“…18 Such micellar systems are usually larger and more fluid than simple micelles and hence have better solubilizing ability for lipophilic compounds. 19 Due to their good physiological compatibility and excellent solubilizing capacity, bile salt micelles and derived mixed systems have been intensively investigated as drug-carrier systems. [20][21][22] Previous investigations into bile salt/phospholipid MMs has mainly focused on the solubilization of insoluble drugs, 18,[23][24][25] structural identification, 26 physicochemical properties, 27 and transmembrane characteristics; 17 however, bile salt/ phospholipid MMs may also be good candidates for oral delivery of poorly water-soluble drugs.…”

Section: Introductionmentioning

confidence: 99%

Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating

Dong¹,

Xie²,

Qi³

et al. 2013

IJN

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Bile salt/phospholipid mixed micelles (MMs) are potent carriers used for oral absorption of drugs that are poorly soluble in water; however, there are many limitations associated with liquid formulations. In the current study, the feasibility of preparing bile salt/ phospholipid MM precursor (preMM) pellets with high oral bioavailability, using fluid-bed coating technology, was examined. In this study, fenofibrate (FB) and sodium deoxycholate (SDC) were used as the model drug and the bile salt, respectively. To prepare the MMs and to serve as the micellular carrier, a weight ratio of 4:6 was selected for the sodium deoxycholate/ phospholipids based on the ternary phase diagram. Polyethylene glycol (PEG) 6000 was selected as the dispersion matrix for precipitation of the MMs onto pellets, since it can enhance the solubilizing ability of the MMs. Coating of the MMs onto the pellets using the fluid-bed coating technology was efficient and the pellets were spherical and intact. MMs could be easily reconstituted from preMM pellets in water. Although they existed in a crystalline state in the preMM pellets, FB could be encapsulated into the reconstituted MMs, and the MMs were redispersed better than solid dispersion pellets (FB:PEG = 1:3) and Lipanthyl ® . The redispersibility of the preMM pellets increased with the increase of the FB/PEG/micellar carrier. PreMM pellets with a FB:PEG:micellar carrier ratio of 1:1.5:1.5 showed 284% and 145% bioavailability relative to Lipanthyl ® and solid dispersion pellets (FB:PEG = 1:3), respectively. Fluid-bed coating technology has considerable potential for use in preparing sodium deoxycholate/phospholipid preMM pellets, with enhanced oral bioavailability for poorly water-soluble drugs.

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Effect of Mixed Micelle Formulations Including Terpenes on the Transdermal Delivery of Diclofenac

Cited by 25 publications

References 7 publications

Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation

Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation

Two-channel dansyl/tryptophan emitters with a cholic acid bridge as reporters for local hydrophobicity within supramolecular systems based on bile salts

Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating

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Effect of Mixed Micelle Formulations Including Terpenes on the Transdermal Delivery of Diclofenac

Cited by 25 publications

References 7 publications

Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100® transdermal system against inflammation

Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100® transdermal system against inflammation

Two-channel dansyl/tryptophan emitters with a cholic acid bridge as reporters for local hydrophobicity within supramolecular systems based on bile salts

Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating

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Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation

Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation