Niosomes as carriers for tretinoin. I. Preparation and properties

Manconi, Maria; Sinico, Chiara; Valenti, Donatella; Loy, Giuseppe; Fadda, Anna Maria

doi:10.1016/s0378-5173(01)00971-1

Cited by 179 publications

(91 citation statements)

References 21 publications

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“…The total run time was 35 minutes. method 24 with some modification. A range of process variables, including hydrophile-lipophile balance values for the surfactants, hydration temperature, molar ratio of surfactants, and cholesterol and weight ratio of GbE and carriers, were studied and optimized on the basis of uniformly small particle size and high entrapment efficiency.…”

Section: Hplc Analysis Of Gbe Flavonoid Glycosidesmentioning

confidence: 99%

Development of a novel niosomal system for oral delivery of Ginkgo biloba extract

Jin¹,

Wen²,

Garg³

et al. 2013

IJN

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Background:The aim of this study was to develop an optimal niosomal system to deliver Ginkgo biloba extract (GbE) with improved oral bioavailability and to replace the conventional GbE tablets. Methods: In this study, the film dispersion-homogenization method was used to prepare GbE niosomes. The resulting GbE niosome suspension was freeze-dried or spray-dried to improve the stability of the niosomes. GbE-loaded niosomes were formulated and characterized in terms of their morphology, particle size, zeta potential, entrapment efficiency, and angle of repose, and differential scanning calorimetry analysis was performed. In vitro release and in vivo distribution studies were also carried out. Results: The particle size of the optimal delivery system prepared with Tween 80, Span 80, and cholesterol was about 141 nm. There was a significant difference (P , 0.05) in drug entrapment efficiency between the spray-drying method (about 77.5%) and the freeze-drying method (about 50.1%). The stability study revealed no significant change in drug entrapment efficiency for the GbE niosomes at 4°C and 25°C after 3 months. The in vitro release study suggested that GbE niosomes can prolong the release of flavonoid glycosides in phosphate-buffered solution (pH 6.8) for up to 48 hours. The in vivo distribution study showed that the flavonoid glycoside content in the heart, lung, kidney, brain, and blood of rats treated with the GbE niosome carrier system was greater than in the rats treated with the oral GbE tablet (P , 0.01). No flavonoid glycosides were detected in the brain tissue of rats given the oral GbE tablets, but they were detected in the brain tissue of rats given the GbE niosomes. Conclusion: Niosomes are a promising oral system for delivery of GbE to the brain.

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Section: Hplc Analysis Of Gbe Flavonoid Glycosidesmentioning

confidence: 99%

Development of a novel niosomal system for oral delivery of Ginkgo biloba extract

Jin¹,

Wen²,

Garg³

et al. 2013

IJN

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“…8,[35][36][37][38][39] The different molar ratio of compounds herein reported improves the stability of NSVs and provides suitable nanocarriers for in vitro and in vivo administration. Freeze-fracture microscopy analysis demonstrated that presence of the drug does not modify the morphology or supramolecular structure of NSVs ( Figure 1).…”

mentioning

confidence: 95%

Ammonium glycyrrhizinate-loaded niosomes as a potential nanotherapeutic system for anti-inflammatory activity in murine models

Marianecci¹,

Rinaldi²,

Marzio³

et al. 2014

IJN

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Background: Liquorice extracts demonstrate therapeutic efficacy in treating dermatitis, eczema, and psoriasis when compared with corticosteroids. In this work, nonionic surfactant vesicles (niosomes, NSVs) containing polysorbate 20 (Tween 20), cholesterol, and cholesteryl hemisuccinate at different molar concentrations were used to prepare monoammonium glycyrrhizinate (AG)-loaded NSVs. The anti-inflammatory properties of AG-loaded NSVs were investigated in murine models. Methods: The physicochemical properties of the NSVs were characterized using dynamic light scattering. The fluidity of the lipid bilayer was evaluated by measuring the fluorescence intensity of diphenylhexatriene. The drug entrapment efficiency of AG was assessed using high-performance liquid chromatography. The physicochemical stability of the NSVs was evaluated as a function of time using dynamic light scattering combined with Turbiscan Lab(R) Expert analysis. Serum stability was determined by incubating the NSVs with 10% v/v fetal bovine serum. The cytotoxic effects of the NSVs were investigated in human dermal fibroblasts using the Trypan blue dye exclusion assay (for cell mortality) and an MTT assay (for cell viability). Release profiles for the AG-loaded NSVs were studied in vitro using cellulose membranes. NSVs showing the most desirable physicochemical properties were selected to test for in vivo anti-inflammatory activity in murine models. The anti-inflammatory activity of the NSVs was investigated by measuring edema and nociception in mice stimulated with chemical agents. Results: NSVs showed favorable physicochemical properties for in vitro and in vivo administration. In addition, they demonstrated long-term stability based on Turbiscan Lab Expert analysis. The membrane fluidity of the NSVs was not affected by self-assembling of the surfactants into colloidal structures. Fluorescence anisotropy was found to be independent of the molar ratios of cholesteryl hemisuccinate and/or cholesterol during preparation of the NSVs. The anti-inflammatory AG drug showed no effect on the stability of the NSVs. In vivo experiments demonstrated that AG-loaded NSVs decreased edema and nociceptive responses when compared with AG alone and empty NSVs. In vitro and in vivo results demonstrated that pH sensitive and neutral NSVs show no statistical significant difference. Conclusion: NSVs were nontoxic and showed features favorable for potential administration in vivo. In addition, neutral NSVs showed signs of increased anti-inflammatory and anti-nociceptive responses when compared with AG

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“…On the other hand, vesicles can protect compounds, like vitamins, from oxidation. Encapsulation of TRT into vesicular carriers as liposomes and ethosomes and nanoparticulate carriers as Solid lipid nanoparticles and, nanostructured lipid carriers (NLCs) offered enhanced photostability, skin transport and anti-psoriatic activity (Manconi et al, 2002(Manconi et al, , 2003Razaa et al, 2013). …”

Section: Introductionmentioning

confidence: 99%

Formulation of tretinoin-loaded topical proniosomes for treatment of acne:in-vitrocharacterization, skin irritation test and comparative clinical study

et al. 2014

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Tretinoin (TRT) is a widely used retinoid for the topical treatment of acne, photo-aged skin, psoriasis and skin cancer which makes it a good candidate for topical formulation. Yet side effects, like redness, swelling, peeling, blistering and, erythema, in addition to its high lipophilicity make this challenging. Therefore, the aim of this study was the development of TRT-loaded proniosomes to improve the drug efficacy and to increase user acceptability and compliance by reducing its side effects. Nine formulae were prepared according to 3 2 factorial design and were evaluated for their morphology, vesicle size, entrapment efficiency (EE %), and% of drug released after 5 h. Hydrogel of the candidate formula, N8G (proniosomes prepared with 0.025% TRT, and Span60: cholesterol molar ratio of 3:1 and incorporated in 1% carbopol gel) was developed and evaluated for skin irritation test and clinical study in acne patients compared to marketed product. Candidate formula showed higher efficacy and very low irritation potential when compared to marketed product in human volunteers.

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Niosomes as carriers for tretinoin. I. Preparation and properties

Cited by 179 publications

References 21 publications

Development of a novel niosomal system for oral delivery of Ginkgo biloba extract

Development of a novel niosomal system for oral delivery of Ginkgo biloba extract

Ammonium glycyrrhizinate-loaded niosomes as a potential nanotherapeutic system for anti-inflammatory activity in murine models

Formulation of tretinoin-loaded topical proniosomes for treatment of acne:in-vitrocharacterization, skin irritation test and comparative clinical study

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