<i>In vitro</i> assessment of non-irritant microemulsified voriconazole hydrogel system

Y, Prasanna Raju; Hyndavi, N; Chowdary, Harini; Nair, Rajesh Sreedharan; D, Jamal Basha; Tejeswari, N

doi:10.1080/21691401.2016.1260579

Cited by 12 publications

(6 citation statements)

References 34 publications

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“…However, the oral administration of voriconazole is compromised by complicated pharmacokinetics, notable drug interactions, and relatively significant adverse events [ 5 ]. Furthermore, its intravenous administration is reported to cause heart rhythm problems [ 6 ]. Therefore, a need exists for a topical delivery system to overcome the limitations and enhance the antifungal effect of voriconazole against cutaneous candidiasis [ 7 ].…”

Section: Introductionmentioning

confidence: 99%

Formulation Development, Characterization and Antifungal Evaluation of Chitosan NPs for Topical Delivery of Voriconazole In Vitro and Ex Vivo

et al. 2021

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This study aims to develop chitosan-based voriconazole nanoparticles (NPs) using spray-drying technique. The effect of surfactants and polymers on the physicochemical properties, in vitro release, and permeation of NPs was investigated. The prepared NPs containing various surfactants and polymers (e.g., Tween 20 (T20), Tween 80 (T80), sodium lauryl sulfate (SLS), propylene glycol (PG), and Polyethylene glycol-4000 (PEG-4000)) were physiochemically evaluated for size, zeta potential, drug content, percent entrapment efficiency, in vitro release, and permeation across rats’ skin. A Franz diffusion cell was used for evaluating the in vitro release and permeation profile. The voriconazole-loaded NPs were investigated for antifungal activity against Candida albicans (C. albicans). The prepared NPs were in the nano range (i.e., 160–500 nm) and positively charged. Images taken by a scanning electron microscope showed that all prepared NPs were spherical and smooth. The drug content of NPs ranged from 75% to 90%. Nanoparticle formulations exhibited a good in vitro release profile and transport voriconazole across the rat’s skin in a slow control release manner. The NPs containing SLS, T80, and PG exhibited the best penetration and skin retention profile. In addition, the formulation exhibited a potential antifungal effect against C. albicans. It was concluded that the development of chitosan NPs has a great potential for the topical delivery of voriconazole against fungal infection.

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Section: Introductionmentioning

confidence: 99%

Formulation Development, Characterization and Antifungal Evaluation of Chitosan NPs for Topical Delivery of Voriconazole In Vitro and Ex Vivo

et al. 2021

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“…This high degree of chemical instability and low solubility of curcumin hinders its oral administration. Although curcumin has a favourable molecular weight (368 Da) for transdermal delivery, other parameters such as its low aqueous solubility and relatively high log P of 3.2 require additional enhancement techniques for skin penetration (10)(11)(12)(13). Numerous studies have aimed at improving curcumin bioavailability and stability by a variety of different approaches including formulation into nanoparticles (14), nanogels (15), microemulsions (16,17), nanofibre transdermal patches (18)(19)(20), micelles (21,22), polymeric conjugates (23,24) or lipid vesicles (25,26).…”

Section: Introductionmentioning

confidence: 99%

An Evaluation of Curcumin-Encapsulated Chitosan Nanoparticles for Transdermal Delivery

et al. 2019

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Curcumin-loaded chitosan nanoparticles were synthesised and evaluated in vitro for enhanced transdermal delivery. Zetasizer® characterisation of three different formulations of curcumin nanoparticles (Cu-NPs) showed the size ranged from 167.3 ± 3.8 nm to 251.5 ± 5.8 nm, the polydispersity index (PDI) values were between 0.26 and 0.46 and the zeta potential values were positive (+ 18.1 to + 20.2 mV). Scanning electron microscopy (SEM) images supported this size data and confirmed the spherical shape of the nanoparticles. All the formulations showed excellent entrapment efficiency above 80%. FTIR results demonstrate the interaction between chitosan and sodium tripolyphosphate (TPP) and confirm the presence of curcumin in the nanoparticle. Differential scanning calorimetry (DSC) studies of Cu-NPs indicate the presence of curcumin in a disordered crystalline or amorphous state, suggesting the interaction between the drug and the polymer. Drug release studies showed an improved drug release at pH 5.0 than in pH 7.4 and followed a zero order kinetics. The in vitro permeation studies through Strat-M® membrane demonstrated an enhanced permeation of Cu-NPs compared to aqueous curcumin solution (p 0.05) having a flux of 0.54 ± 0.03 μg cm −2 h −1 and 0.44 ± 0.03 μg cm −2 h −1 corresponding to formulations 5:1 and 3:1, respectively. The cytotoxicity assay on human keratinocyte (HaCat) cells showed enhanced percentage cell viability of Cu-NPs compared to curcumin solution. Cu-NPs developed in this study exhibit superior drug release and enhanced transdermal permeation of curcumin and superior percentage cell viability. Further ex vivo and in vivo evaluations will be conducted to support these findings.

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“…These results proved that microemulsions had superior fungicidal efficacies due to considerable penetration of the drug into fungal cell membranes. 26 Jadhav et al 27 observed greater activity of fluconazole-loaded microemulsions than of conventional gel formulations and this was attributed to the better diffusion of the drug provided by the presence of surfactants and oil phase. Similarly, El-Hadidy et al 28…”

Section: Atr-ftir Spectroscopymentioning

confidence: 99%

<i>In Vitro</i> Skin Permeation and Antifungal Activity of Naftifine Microemulsions

Erdal¹,

Gürbüz²,

Tan³

et al. 2020

tjps

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Amaç: Mikroemülsiyonlar, ilaç taşıyıcı sistemler olarak çok çalışılan; sıvı, izotropik, kolloidal sistemlerdir. Aktif maddelerin mikroemülsiyonlardan perkütan absorpsiyonu konvansiyonel formülasyona göre iyileşebilmektedir. Bu çalışmanın amacı, naftifin yüklü mikroemülsiyonların, ilacın deriden permeasyonunun iyileştirilmesine yönelik olarak değerlendirilmesidir. Gereç ve Yöntemler: Oleik asit (yağ fazı), Kolliphor EL veya Kolliphor RH40 (surfaktan), Transcutol (ko-surfaktan) ve sudan oluşan mikroemülsiyonlar hazırlanarak fizikokimyasal karakterizasyonları gerçekleştirilmiştir. Naftifinin in vitro deriden permeasyonu çalışılmış ve konvansiyonel ticari preparatı ile karşılaştırılmıştır. Zayıflatılmış toplam yansıma-Fourier dönüşümü (ATR-FTIR) spektroskopisi, mikroemülsiyonlar ile stratum corneum lipitleri arasındaki etkileşimin araştırılması için kullanılmıştır. Naftifin yüklü mikroemülsiyonların antifungal aktiviteleri Candida albicans Amerikan Tip Kültür Koleksiyonu (ATCC) 10231 ve Candida parapsilosis kullanılarak değerlendirilmiştir. Bulgular: Ko-surfaktan olarak Kolliphor RH40 içeren mikroemülsiyon formülasyonu, naftifinin topikal ticari formülasyonu ile karşılaştırıldığında, domuz derisinden naftifin permeasyonunu istatistiksel olarak anlamlı derecede arttırmıştır (p<0,05). ATR-FTIR spektroskopisi, mikroemülsiyonların stratum corneum lipit çifte tabakalarının akışkanlığını arttırdığını göstermiştir. İlaç yüklü mikromülsiyonlar, Candida albicans ATCC 10231 ve Candida parapsilosis türlerine karşı yüksek antifungal aktivite göstermişlerdir. Sonuç: Sonuç olarak, bu çalışmada mikroemülsiyonların, naftifinin deriden permeasyonunun iyileştirilmesinde alternatif topikal taşıyıcılar olarak kabul edilebilecekleri gösterilmiştir. Anahtar kelimeler: Naftifin, mikroemülsiyon, kolloidal ilaç taşıyıcı sistem, topikal antifungal Objectives: Microemulsions are fluid, isotropic, colloidal systems that have been widely studied as drug delivery systems. The percutaneous transport of active agents can be enhanced by their microemulsion formulation when compared to conventional formulations. The purpose of this study was to evaluate naftifine-loaded microemulsions with the objective of improving the skin permeation of the drug. Materials and Methods: Microemulsions comprising oleic acid (oil phase), Kolliphor EL or Kolliphor RH40 (surfactant), Transcutol (co-surfactant), and water were prepared and physicochemical characterization was performed. In vitro skin permeation of naftifine from microemulsions was investigated and compared with that of its conventional commercial formulation. Attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy was used to evaluate the interaction between the microemulsions and the stratum corneum lipids. Candida albicans American Type Culture Collection (ATCC) 10231 and Candida parapsilosis were used to evaluate the antifungal susceptibility of the naftifine-loaded microemulsions. Results: The microemulsion formulation containing Kolliphor RH40 as co-surfactant increased nafti...

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In vitro assessment of non-irritant microemulsified voriconazole hydrogel system

Cited by 12 publications

References 34 publications

Formulation Development, Characterization and Antifungal Evaluation of Chitosan NPs for Topical Delivery of Voriconazole In Vitro and Ex Vivo

Formulation Development, Characterization and Antifungal Evaluation of Chitosan NPs for Topical Delivery of Voriconazole In Vitro and Ex Vivo

An Evaluation of Curcumin-Encapsulated Chitosan Nanoparticles for Transdermal Delivery

<i>In Vitro</i> Skin Permeation and Antifungal Activity of Naftifine Microemulsions

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