Effect of microemulsion in topical sertaconazole hydrogel: <i>in vitro</i> and <i>in vivo</i> study

Sahoo, Susijit; Pani, Nihar Ranjan; Sahoo, Sabuj

doi:10.3109/10717544.2014.914601

Cited by 32 publications

(19 citation statements)

References 31 publications

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“…The cup-plate technique was used to evaluate the antifungal activity of the selected SLNs, as described by Barot et al, and Sahoo et al, [21,22]. The evaluation was carried out against Candida albicans ATCC 10231, which obtained from The National Research Centre, Cairo, Egypt.…”

Section: Microbiological Evaluation Of the Selected Slns Formulaementioning

confidence: 99%

FORMULATION AND OPTIMIZATION OF TERBINAFINE HCl SOLID LIPID NANOPARTICLES FOR TOPICAL ANTIFUNGAL ACTIVITY

Abobakr

Fayez

Elwazzan

et al. 2019

Int J Pharm Pharm Sci

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Objective: Solid lipid nanoparticles (SLNs) are at the forefront of the rapidly developing field of nanotechnology with several potential applications in drug delivery and research. The aim of this study was to develop and characterize SLNs formulae of Terbinafine HCl (TFH) for topical drug delivery applications.Methods: SLNs were prepared using the solvent injection technique. Glyceryl Monostearate (GMS) served as the lipid base. Three stabilizers; Tween 80, Cremophor RH40, and Poloxamer 188, were used. The effect of stabilizer type and concentration, as well as the lipid concentration, were studied, factorial design of 3 2 *2 1 was applied. The prepared SLNs were characterized regarding their particle size, zeta potential, polydispersity index (PDI), entrapment efficiency percent (EE %), and physicochemical stability. The selected formulae were subjected to further investigations such as morphological studies, in vitro release studies, and Infrared (IR) spectroscopy. They were compared with the marketed cream Lamifen ® in term of their antifungal activity against Candida albicans.Results: Lipid concentration, together with the type and concentration of stabilizer, appeared to be the main cornerstones which affect the formation of SLNs. Smaller particle size was observed when increasing the stabilizer concentration and decreasing the lipid concentration. Higher EE% was observed when increasing both the stabilizer and the lipid concentrations. Formulae (F6, F12 andF19) were selected as the most suitable SLNs with optimum particle size of 480.2±18.89, 458.6±12.45 and 246.7±10.5 nm, respectively as well as the highest EE% of 87.13±0.19, 93.69±0.7 and 95.06±0.25, respectively. In vitro microbiological screening of their antifungal activity showed significantly larger zones of inhibition of diameters 25.9±0.25, 25±0.35 and 24.67±0.36 mm, respectively in comparison with the marketed Lamifen® cream which showed a zone of 11.2±0.44 mm diameter. Conclusion:Applying SLNs containing TFH as topical antifungal preparations may be considered as a very promising option as they show good physicochemical characterization with high antifungal activity, which delineates them as a promising dosage form for topical antifungal treatment.

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Section: Microbiological Evaluation Of the Selected Slns Formulaementioning

confidence: 99%

FORMULATION AND OPTIMIZATION OF TERBINAFINE HCl SOLID LIPID NANOPARTICLES FOR TOPICAL ANTIFUNGAL ACTIVITY

Abobakr

Fayez

Elwazzan

et al. 2019

Int J Pharm Pharm Sci

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“…At each speed, dial reading on the viscometer was noted. Direct multiplication of the dial readings with factors given in the Brookfield viscometer catalogue gave the viscosity in centipoises [34][35][36][37].…”

Section: Viscositymentioning

confidence: 99%

“…From this solution, 1 ml was withdrawn and volume adjusted to 10 ml with methanol. The absorbance was taken at a λmax 264 nm by UV-Spectrophotometer [35][36][37].…”

Section: Drug Contentmentioning

confidence: 99%

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Enhancement of Skin Permeability of Econazole Nitrate Using Novel Flexisomal Nanocarriers by Implementing Quality by Design (Qbd) Approach

Mandlik

Dandgavhal

2019

Int J App Pharm

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Objective: The purpose of this study was an implementation of quality by design (QbD) for the formulation and characterization of econazole nitrate loaded flexisomal nanocarriers (EN-FS) to improve antifungal activity and to enhance skin permeability.Methods: Initially quality target product profile (QTTP) elements were identified and later critical quality attributes (CQA) elements were defined from QTPP elements. Particle size, entrapment efficiency and deformability index were defined as CQAs. Risk assessment was performed by using fishbone diagram and failure mode and effect analysis (FMEA). Design space was created by using fractional factorial design 2 5-2 as screening design and 3 2 full factorial design as optimization design to optimize two variables soya phosphatidylcholine concentration(X1) and sodium deoxycholate concentration (X2 Results:Optimized batch of EN-FS was 249.5±3.48 nm, with entrapment efficiency of 88.6±0.89 % and deformability index of 31.75±0.98. Zeta potential analysis showed value of-22.5 mV. Morphological analysis by TEM showed spherical shaped flexisomes, which confirmed the vesicular characteristics. The optimized batch of EN-FS was further made into hydrogels by using sepineo P600 as gelling agent. The % drug diffusion of EN-FS hydrogels had shown 24.68%. With higher skin deposition and higher value of zone of inhibition in antifungal study as compared to plain EN hydrogel. CLSM studies indicated deep penetration of EN-FS in skin layers. Lastly control strategy for EN-FS were developed.). Conclusion:It was concluded that EN-FS showed high flexibility and enhanced antifungal activity therefore found to be a potential nanocarriers for drug deposition in skin layers without disturbing skin integrity. I In nt te er rn na at ti io on na al l J Jo ou ur rn na al l o of f A Ap pp pl li ie ed d P Ph ha ar rm ma ac ce eu ut ti ic cs s

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“…Three wells were made in the middle of the plates with the help of sterile cork-borer, each well (6 mm internal diameter) was accurately filled with either 0.1 ml of the nPEVs formula, 0.1 ml of the control formula or an amount of Dermofix Õ cream equivalent to the sertaconazole dose in the 0.1 ml nPEVs formula. The plates were then incubated at 25 C for three days in the incubator to allow fungal growth (Barot et al, 2012;Sahoo et al, 2014).…”

Section: Microbiological Efficacy Of Npevs For the Treatment Of Onychmentioning

confidence: 99%

Novel nail penetration enhancer containing vesicles “nPEVs” for treatment of onychomycosis

et al. 2015

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Context: The systemic treatment of onychomycosis has been hampered by the reported side effects of antifungals in addition to the limited blood circulation to the affected nails. Topical ungual treatment would circumvent the limitations of systemic onychomycosis treatment. Objective: Preparation and characterization of nail penetration enhancer containing nanovesicles (nPEVs) loaded with sertaconazole for topical treatment of onychomycosis. Materials and methods: nPEVs were prepared using different nail penetration enhancers (N-acetyl-L-cysteine, thioglycolic acid, thiourea and ethanol) by the thin film hydration method, and characterized for their particle size, zeta potential, entrapment efficiency (EE%), elasticity, viscosity, physical stability and morphology. The selected nPEVs formula and the marketed Dermofix Õ cream were compared in terms of nail hydration, transungual drug uptake and antifungal activity against Trichophyton rubrum. Results: N-acetyl-L-cysteine was the optimum nail penetration enhancer for incorporation within vesicles. nPEVs showed high EE% of sertaconazole ranging from 77 to 95%, a size ranging from 38-538 nm and a zeta potential ranging from +48 to +72 mV. The selected nPEVs formula displayed spherical morphology and good storage stability. Compared to the conventional marketed cream, the selected nPEVs formula showed 1.4-folds higher hydration and drug uptake enhancement into nail clippings. Furthermore, it showed significantly higher zone of inhibition for Trichophyton rubrum (20.9 ± 0.25 mm) than the marketed cream (11.6 ± 0.44 mm). Conclusion: Nail penetration enhancer containing nanovesicles (nPEVs) present a very promising option, worthy of clinical experimentation on onychomycotic patients.

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Effect of microemulsion in topical sertaconazole hydrogel: in vitro and in vivo study

Abstract: The results of study showed that ME played a major role in permeation enhancing and skin retention effect of HSM and the concentration of STZL used for cutaneous fungal infection could be decreased by using ME based hydrogel preparation.

Cited by 32 publications

References 31 publications

FORMULATION AND OPTIMIZATION OF TERBINAFINE HCl SOLID LIPID NANOPARTICLES FOR TOPICAL ANTIFUNGAL ACTIVITY

FORMULATION AND OPTIMIZATION OF TERBINAFINE HCl SOLID LIPID NANOPARTICLES FOR TOPICAL ANTIFUNGAL ACTIVITY

Enhancement of Skin Permeability of Econazole Nitrate Using Novel Flexisomal Nanocarriers by Implementing Quality by Design (Qbd) Approach

Novel nail penetration enhancer containing vesicles “nPEVs” for treatment of onychomycosis

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