Improved solubility and dissolution rate of piroxicam using gelucire 44/14 and labrasol

Karataş, Ayşegül; Yüksel, Nilüfer; Baykara, Tamer

doi:10.1016/j.farmac.2005.04.014

Cited by 78 publications

(43 citation statements)

References 16 publications

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“…The greatest permeation was noted for the higher hydration conditions (Test 1) applied to the higher Gelucire content FM10 films. This lipid excipient is associated with favourable solubilisation [42][43], permeation enhancement [30] and self-emulsifying [27,[44][45][46], hence while the consistency and performance need to be considered in conjunction for any system that can be used in practice, the inclusion of this excipient does appear to show particular promise as a means of achieving waterinduced release of the drug from the transdermal film.…”

Section: ) (Iv) Liquid-like Emulsion Of Hydrated Fm10 Films (20% (mentioning

confidence: 99%

Hot melt extruded transdermal films based on amorphous solid dispersions in Eudragit RS PO: The inclusion of hydrophilic additives to develop moisture-activated release systems

Albarahmieh

Craig

2016

International Journal of Pharmaceutics

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A series of Eudragit RS PO-based hot melt extruded films were evaluated as potential transdermal systems, with particular emphasis on the inclusion of hydrophilic excipients to allow water sorption, which in turn would allow drug release on application to the skin. More specifically, sucrose, methyl cellulose, xanthan gum (Xantural®75), poloxamer (Pluronic®F127), Gelucire 44/14 were added to Eudragit RS PO and assessed in terms of physical structure (modulated temperature DSC (MTDSC), thermogravimetric analysis (TGA), powder XRD (PXRD), scanning electron microscopy(SEM)) and in vitro drug release and permeation properties. In addition, the effect of prior hydration on drug permeation was studied for selected systems. Phase separation was noted for sucrose, methylcellulose (high loading), xanthan gum (high loading), poloxamer and Gelucire 44/14 (high loading) using both visual observation and MTDSC. PXRD studies indicated drug crystallization within the phase separated systems. SEM studies broadly followed the same pattern. Dissolution studies indicated that the hydrophilic excipients considerably enhanced the release rate, while Franz diffusion cell studies showed a much greater variability in effectiveness, which we ascribe to the paucity of water of hydration present which would not allow swellable additives such as xanthan to release the drug. However, films containing Gelucire 44/14 emerged as the most satisfactory systems, despite the higher additive loaded systems showing drug phase separation. This may be related to emulsification rather than swelling on contact with water, as noted for the permeation studies involving prehydration. This strategy therefore presents a promising approach for triggered transdermal drug delivery, activated by hydration from the skin itself.

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Section: ) (Iv) Liquid-like Emulsion Of Hydrated Fm10 Films (20% (mentioning

confidence: 99%

Hot melt extruded transdermal films based on amorphous solid dispersions in Eudragit RS PO: The inclusion of hydrophilic additives to develop moisture-activated release systems

Albarahmieh

Craig

2016

International Journal of Pharmaceutics

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“…The phase solubility diagram followed an A L -type system at the given range of concentrations. [19,20] Moreover, the values of DG tr also varied linearly and became more negative with increasing concentrations of Soluplus®, showing that the drug solubilisation process is spontaneous in the presence of the polymer (Figure 2). The rapid negative increase in DG tr values with the polymer concentration also indicates that the transfer of the drug from aqueous phase at the drug particle vicinity to the bulk of the carrier solution is more favourable at higher carrier concentrations.…”

Section: Phase Solubilitymentioning

confidence: 99%

Enhanced dissolution characteristics of piroxicam–Soluplus® nanosuspensions

Patnaik

Chunduri

Akilesh

et al. 2016

Journal of Experimental Nanoscience

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In the present study, we have prepared nanosuspensions of piroxicam using Soluplus® as the matrix using aqueous-based conventional ball milling. The comparative physico-chemical characteristics were assessed using PXRD (powder X-ray diffraction), DSC (differential scanning calorimetry), FESEM (field emission scanning electron microscopy) and FTIR (Fourier transform infrared spectroscopy) analysis, indicating the nanoformulations displayed lower crystallinity with no chemical interactions between the drug and polymer molecules. The cytotoxicity of the formulations was established from MTT assay performed on Caco-2 cell lines. The release rate of piroxicam from various ratios of drug/polymer nanoparticles was investigated using a USP paddle apparatus. The nanoformulations exhibited higher release of the drug in comparison with the pure drug. The enhanced dissolution characteristics of the drug in the nanoformulations could possibly increase the anti-inflammatory effects of the drug owing to superior bioavailability characteristics.

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“…It also showed a broad endothermic peak at 117.5°C that could be due to formation of hydrogen bond between the -OH group on benzothiazine ring of PX and the stabilizer used during NPs preparation. 33 PM thermogram only showed an endothermic peak at 55.4°C, representative of endothermic peak of P188.…”

Section: Scanning Electron Microscopymentioning

confidence: 99%

Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation

El-Habashy

Allam

El-Kamel

2016

IJN

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Nanoparticles (NPs) have long gained significant interest for their use in various drug formulations in order to increase bioavailability, prolong drug release, and decrease side effects of highly toxic drugs. The objective of this investigation was to evaluate the potential of ethyl cellulose-based NPs (EC-NPs) to modulate the release and reduce ulcerogenicity of piroxicam (PX) after oral administration. PX-loaded EC-NPs were prepared by solvent evaporation technique using different stabilizers at three concentration levels. Morphological examination of selected formulas confirmed the formation of spherical NPs with slightly porous surface. Formulation containing poloxamer-stabilized EC-NPs (P188/0.2), having a particle size of 240.26±29.24 nm, polydispersity index of 0.562±0.030, entrapment efficiency of 85.29%±1.57%, and modulated release of PX (88% after 12 hours), was selected as the optimum formulation. Differential scanning calorimetry demonstrated the presence of PX in an amorphous form in the NPs. Fourier-transform infrared spectroscopy revealed the possible formation of hydrogen bond and the absence of chemical interaction. In vivo study, evaluation of pharmacokinetic parameters, evaluation of gastric irritation potential, and histological examination were conducted after administration of the selected formulation. Time to reach maximum plasma concentration, t max , of poloxamer-stabilized EC-NPs was significantly higher than that of Feldene ® 20 mg capsules ( P ≤0.001). Encapsulation of the acidic, gastric offender PX into NPs managed to significantly suppress gastric ulceration potential in rats ( P ≤0.05) as compared to that of PX suspension. A reduction of 66% in mean ulcer index was observed. In conclusion, poloxamer-stabilized EC-NPs (P188/0.2) had a significant potential of offsetting deleterious side effects common in PX use.

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Improved solubility and dissolution rate of piroxicam using gelucire 44/14 and labrasol

Cited by 78 publications

References 16 publications

Hot melt extruded transdermal films based on amorphous solid dispersions in Eudragit RS PO: The inclusion of hydrophilic additives to develop moisture-activated release systems

Hot melt extruded transdermal films based on amorphous solid dispersions in Eudragit RS PO: The inclusion of hydrophilic additives to develop moisture-activated release systems

Enhanced dissolution characteristics of piroxicam–Soluplus® nanosuspensions

Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation

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