Nanostructured lipid carriers for the topical delivery of tretinoin

Ghate, Vivek; Lewis, Shaila; Prabhu, Prabhakara; Dubey, Akhilesh; Patel, Nilkumar

doi:10.1016/j.ejpb.2016.07.026

Cited by 82 publications

(31 citation statements)

References 34 publications

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“…The oil phase studied, were IPM and OA due to their availability, low cost and applicability in topical anti-acne treatments [24,29]. Tween 80 and tween 20 were selected as surfactants (S) for IPM and OA based on the previously published microemulsion systems, respectively [30][31], while DEGEE and ethanol in the weight ratios of (20:18, w/w) and (20:27, w/w) for IPM and OA, respectively, were used as the co-surfactant (CoS).…”

Section: Construction Of Pseudo-ternary Phase Diagrammentioning

confidence: 99%

A novel hydrogel-thickened microemulsion of dapsone for acne treatment: Development, characterization, physicochemical stability and ex vivo permeation studies

Beheshti-Mall¹,

Shafaroodi²,

Jafariazar³

et al. 2018

mpj

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Acne vulgaris is a common inflammatory skin condition, which has been reclassified as a chronic disease. The spectrum of topical acne treatments has expanded substantially in recent years and various topical medications including topical dapsone are available. Dapsone has special physicochemical properties that make its topical formulation challenging. The aim of this study was preparing a hydrogel-thickened microemulsion as a topical delivery system for dapsone. The microemulsions composed of dapsone (5%), isopropyl myristate, tween 80, diethylene glycol monoethyl ether, ethanol and water were prepared. The optimum microemulsion was modified with carbomer 940. Droplet size, pH, refractive index, conductivity, rheology of the optimized formulation, and skin permeation of dapsone through rat skin were evaluated. The optimized formulation significantly increased the skin permeation of dapsone in comparison to that of control gel. Although incorporation of menthol increased the particle size, the flux of microemulgel consisting of menthol (5%) was 2.51 times higher than that of the control. However, the skin absorption of the drug was less than 3%. Six month accelerated studies proved the physicochemical stability of microemulgels. The results of this research indicate that menthol based hydrogel-thickened microemulsion system could be a promising vehicle for topical delivery of dapsone.

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Section: Construction Of Pseudo-ternary Phase Diagrammentioning

confidence: 99%

A novel hydrogel-thickened microemulsion of dapsone for acne treatment: Development, characterization, physicochemical stability and ex vivo permeation studies

Beheshti-Mall¹,

Shafaroodi²,

Jafariazar³

et al. 2018

mpj

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show abstract

“…Cytokines, including IL-1β, IL-8 and IL-6, are used as markers for the potential toxicity of drugs administered to the reproductive tract mucosa ( 20 ). NLCs can be prepared using both solid and liquid lipids, which induce minimal skin irritation ( 35 ). In the present study, the irritation caused to the cervical mucosal tissue of Tibetan mini pigs following repeated administrations of different doses of POD-NLC was evaluated.…”

Section: Discussionmentioning

confidence: 99%

Development of podophyllotoxin‑loaded nanostructured lipid carriers for the treatment of condyloma acuminatum

et al. 2018

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Condyloma acuminatum (CA) is a common sexually transmitted disease caused by human papillomavirus (HPV). Podophyllotoxin (POD), a cytotoxic compound, is able to effectively treat HPV; however, the severe irritation side effects of POD restrict its use as a treatment for CA. The aim of the present study was to construct novel POD-loaded nanostructured nanolipid carriers (POD-NLCs) and evaluate their physicochemical characteristics and cytotoxicity. POD-NLCs (0.5%) were prepared using emulsion-evaporation and low temperature-solidification methods with optimized conditions and preparations. Subsequently, the POD-NLCs were physicochemically characterized and their in vitro and in vivo release efficiencies and in vitro cytotoxicity were studied. The prepared POD-NLCs had an average particle size, ζ potential, polydispersity index and encapsulation efficacy of 178.5±20 nm, −27±0.5 mV, 0.18±0.01 and 82.9±2%, respectively. In vitro and in vivo release studies demonstrated that POD-NLCs are able to provide sustained drug delivery for 72 h in vitro and 10 h in the mucosa. Compared with a tincture formulation of POD (POD-T), POD-NLC induced less inflammatory cytokine production in the cervical mucous and led to a decreased histopathological score. In addition, a cytotoxicity assay demonstrated that inhibition of the POD-NLCs was 98.4% at 24 h and remained >98% up to 72 h. Furthermore, more cells were arrested in the G2/M phase of the cell cycle following POD-NLC treatment compared with the POD-T treatment. The present study provides evidence that POD-NLC is a promising delivery system for the treatment of CA.

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“…In pure PCL peaks at 2864 cm − 1 and 2942 cm − 1 represent stretching vibrations of CH 2 , the peak in 1722 cm − 1 attributes to stretching vibrations of C=O and band in 1000-1300 cm − 1 indicates stretching vibrations of the C-O-C group of the PCL backbone. The peak in 3438 cm − 1 depicts O-H stretching vibrations, the band in 2324 cm − 1 corresponds to C=O stretching and peaks at 960 cm − 1 shows the trans vinyl (CH=CH) groups of tretinoin molecule [14][15][16][17][18][19].…”

Section: Ftir Analysismentioning

confidence: 99%

Fabrication and characterization of tretinoin-loaded nanofiber for topical skin delivery

et al. 2020

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Background: Tretinoin or all-trans retinoic acid is used in the treatment of acne vulgaris and photo-aging. This work aims to develop tretinoin-loaded nanofibers as a potential anti-acne patch and to investigate its physicochemical characteristics. Method: Nanofibers were produced via electrospinning method and surface topography was evaluated by Field Emission Scanning Electron Microscopy (FESEM). The functional groups of polymer and the drug molecule and the possible interactions were studied by Fourier Transform Infrared Spectroscopy (FTIR). Drug release studies were carried out by total immersion method at 25°C and 32°C. Tretinoin stability was evaluated at room temperature and fridge for 45 days. The possibility of synergistic antibacterial activity of tretinoin and erythromycin combination was investigated on Staphylococcus aureus (ATCC® 25923™) and (ATCC® 29213™) by Kirby Bauer disc diffusion method. Results: Uniform fibers without drug crystals were fabricated via electrospinning. Drug-loaded nanofibers show inherent stability under various storage conditions. Electrospun nanofibers showed a prolonged release of tretinoin. The stability of formulations in FT was higher than RT. Disc diffusion tests did not show any synergism in the antibacterial activity of erythromycin when used in combination with tretinoin. Conclusion: It can be anticipated that the easy fabrication, low costs and dosing frequency of the construct reported here provide a platform that can be adapted for on-demand delivery of tretinoin.

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Nanostructured lipid carriers for the topical delivery of tretinoin

Cited by 82 publications

References 34 publications

A novel hydrogel-thickened microemulsion of dapsone for acne treatment: Development, characterization, physicochemical stability and ex vivo permeation studies

A novel hydrogel-thickened microemulsion of dapsone for acne treatment: Development, characterization, physicochemical stability and ex vivo permeation studies

Development of podophyllotoxin‑loaded nanostructured lipid carriers for the treatment of condyloma acuminatum

Fabrication and characterization of tretinoin-loaded nanofiber for topical skin delivery

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