Topical liquid crystalline gel containing lornoxicam/cyclodextrin complex

Ammar, H. O.; Ghorab, Mahmoud M.; Mahmoud, Azza A.; Makram, Tarek Saad; Noshi, Shereen H.

doi:10.1007/s10847-011-0039-y

Cited by 23 publications

(9 citation statements)

References 59 publications

(65 reference statements)

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“…2-hydroxy propyl-β-CD (HP-β-CD) (Fig 1c), have also attracted growing interest due to their improved complexation efficiency, greater water solubility and less toxicity [3]. Inclusion complex formation with CDs is an approach to improve the aqueous solubility via molecular encapsulation of the drug within the cavity of the more soluble CD molecule [2,21]. Molecular weight and solubility parameters of β-CD and HP-β-CD were given in Table 1.…”

Section: Scanning Electron Microscopy (Sem) and Thickness Measurementsmentioning

confidence: 99%

Electrospun Thermoplastic Polyurethane Mats Containing Naproxen– Cyclodextrin Inclusion Complex

Akduman

Özgüney

Kumbasar

2014

Autex Research Journal

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Incorporation of cyclodextrins (CDs) into electrospun nanofibrous materials can be considered as potential candidates for functional medical textile applications. Naproxen (NAP) is a type of non-steroidal anti-inflammatory drug commonly administered for the treatment of pain, inflammation and fever. Drug-inclusion complex formation with CDs is an approach to improve the aqueous solubility via molecular encapsulation of the drug within the cavity of the more soluble CD molecule. In this study, NAP or different NAP-CD inclusion complexes loaded nanofibres were successfully produced through electrospinning and characterised. The inclusion complex loaded mats exhibited significantly faster release profiles than NAP-loaded thermoplastic polyurethane (TPU) mats. Overall, NAP-inclusion complex loaded TPU electrospun nanofibres could be used as drug delivery systems for acute pain treatments since they possess a highly porous structure that can release the drug immediately.

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Section: Scanning Electron Microscopy (Sem) and Thickness Measurementsmentioning

confidence: 99%

Electrospun Thermoplastic Polyurethane Mats Containing Naproxen– Cyclodextrin Inclusion Complex

Akduman

Özgüney

Kumbasar

2014

Autex Research Journal

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“…Additionally, NLCs can reduce the skin barrier and improve the lipid solubility of drugs, thus translating the drugs across the skin effectively, as well as protecting the active drugs from degradation 23. To our knowledge, LN can be incorporated in some carriers, such as transdermal patches,5 films,6 gels9,24,25 and NLCs8 for transdermal drug delivery. To further enhance the delivery of NLCs into deep skin layers, cell-penetrating peptides (CPPs) have been investigated for their ability to translocate nanoparticles across the cellular membrane when modified on the surface of NLCs 26.…”

Section: Introductionmentioning

confidence: 99%

<p>Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema</p>

Gao¹,

Tian²,

Han³

et al. 2019

IJN

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Background: Nanostructured lipid carriers (NLCs) are emerging as attractive drug carriers in transdermal drug delivery. The surface modification of NLCs with cell-penetrating peptides (CPPs) can enhance the skin permeation of drugs. Purpose: The objective of the current study was to evaluate the ability of the cell-penetrating peptide (CPP) polyarginine to translocate NLCs loaded with lornoxicam (LN) into the skin layers and to evaluate its anti-inflammatory effect. Methods: The NLCs were prepared using an emulsion evaporation and low temperature solidification technique using glyceryl monostearates, triglycerides, DOGS-NTA-Ni lipids and surfactants, and then six histidine-tagged polyarginine containing 11 arginine (R11) peptides was modified on the surface of NLCs. Results: The developed NLCs formulated with LN and R11 (LN-NLC-R11) were incorporated into 2% HPMC gels. NLCs were prepared with a particle size of (121.81±3.61)–(145.72±4.78) nm, and the zeta potential decreased from (−30.30±2.07) to (−14.66±0.74) mV after the modification of R11 peptides. The encapsulation efficiency and drug loading were (74.61±1.13) % and (7.92±0.33) %, respectively, regardless of the surface modification. Cellular uptake assays using HaCaT cells suggested that the NLC modified with R11 (0.02%, w/w) significantly enhanced the cell internalization of nanoparticles relative to unmodified NLCs ( P <0.05 or P <0.01). An in vitro skin permeation study showed better permeation-enhancing ability of R11 (0.02%, w/w) than that of other content (0.01% or 0.04%). In carrageenan-induced rat paw edema models, LN-NLC-R11 gels inhibited rat paw edema and the production of inflammatory cytokines compared with LN-NLC gels and LN gels ( P <0.01). Conclusion: In our investigation, it was strongly demonstrated that the surface modification of NLC with R11 enhanced the translocation of LN across the skin, thereby alleviating inflammation.

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“…LOR exhibits a short plasma elimination with half-life (3–5 hr). LOR is characterized by lipophilic nature with a poor solubility in the acidic media of the stomach which gives local toxicity on the stomach [ 6 , 7 ]. LOR has a molecular weight of 371.8, partition coefficient of 1.7, and dose of 4 to 8 mg [ 6 ], and it is available only in tablet and parenteral forms.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Skin Permeation and Analgesic Activity Effects of Carbopol Lornoxicam Topical Gels Containing Penetration Enhancer

Al‐Suwayeh

Taha

Alqahtani

et al. 2014

The Scientific World Journal

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The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also, in vitro skin permeation of LOR was conducted. The effect of hydroxypropyl β-cyclodextrin (HP β-CD), beta-cyclodextrin (β-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 μg/cm2/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HP β-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HP β-CD and may be promising in enhancing permeation.

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Topical liquid crystalline gel containing lornoxicam/cyclodextrin complex

Cited by 23 publications

References 59 publications

Electrospun Thermoplastic Polyurethane Mats Containing Naproxen– Cyclodextrin Inclusion Complex

Electrospun Thermoplastic Polyurethane Mats Containing Naproxen– Cyclodextrin Inclusion Complex

<p>Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema</p>

Evaluation of Skin Permeation and Analgesic Activity Effects of Carbopol Lornoxicam Topical Gels Containing Penetration Enhancer

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