Itraconazole lipid nanocapsules gel for dermatological applications: In vitro characteristics and treatment of induced cutaneous candidiasis

El-Sheridy, Nabila A.; Ramadan, Alyaa; Eid, Abulfotooh M.; El-Khordagui, Labiba K.

doi:10.1016/j.colsurfb.2019.05.057

Cited by 39 publications

(14 citation statements)

References 57 publications

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“…The development of M-ITC-LNC <100 nm in diameter and having high EE% and relatively high ITC payload was guided by earlier studies involving different applications (Eissa et al., 2015 ; El-Sheridy et al., 2019 ). LNC are conventionally formulated with Labrafac as the main oil core component and Kolliphor ® HS 15 as the pegylated surfactant forming the tensioactive shell (Heurtault et al., 2002; Huynh et al., 2009 ).…”

Section: Resultsmentioning

confidence: 99%

“…Entrapment efficiency was calculated based on the difference between the amounts of entrapped and un-entrapped ITC. LNC were separated using an ultrafiltration/centrifugation technique and ITC was assayed in the ultrafiltrate by an isocratic reverse phase HPLC method with UV detection at 225 nm (El-Sheridy et al., 2019 ). Briefly, separation was performed on Inertsil C-18 column (ODS, 250 × 4.6 mm, 5 μ).…”

Section: Methodsmentioning

confidence: 99%

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Enhancing the in vitro and in vivo activity of itraconazole against breast cancer using miltefosine-modified lipid nanocapsules

et al. 2021

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Itraconazole (ITC), a well-tolerated antifungal drug, exerts multiple anticancer effects which justified its preclinical and clinical investigation as potential anti-cancer agent with reduced side effects. Enhancement of ITC anti-cancer efficacy would bring valuable benefits to patients. We propose herein lipid nanocapsules (LNCs) modified with a subtherapeutic dose of miltefosine (MFS) as a membrane bioactive amphiphilic additive (M-ITC-LNC) for the development of an ITC nanoformulation with enhanced anticancer activity compared with ITC solution (ITC-sol) and unmodified ITC-LNC. Both LNC formulations showed a relatively small size (43–46 nm) and high entrapment efficiency (>97%), though ITC release was more sustained by M-ITC-LNC. Cytotoxicity studies revealed significantly greater anticancer activity and selectivity of M-ITC-LNC for MCF-7 breast cancer cells compared with ITC-sol and ITC-LNC. This trend was substantiated by in vivo findings following a 14 day-treatment of murine mammary pad Ehrlich tumors. M-ITC-LNC showed the greatest enhancement of the ITC-induced tumor growth inhibition, proliferation, and necrosis. At the molecular level, the tumor content of Gli 1, caspase-3, and vascular endothelial growth factor verified superiority of M-ITC-LNC in enhancing the ITC antiangiogenic, apoptotic, and Hedgehog pathway inhibitory effects. Finally, histopathological and biochemical analysis indicated greater reduction of ITC systemic toxicity by M-ITC-LNC. Superior performance of M-ITC-LNC was attributed to the effect of MFS on the structural and release properties of LNC coupled with its distinct bioactivities. In conclusion, MFS-modified LNC provides a simple nanoplatform integrating the potentials of LNC and MFS for enhancing the chemotherapeutic efficacy of ITC and possibly other oncology drugs.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Enhancing the in vitro and in vivo activity of itraconazole against breast cancer using miltefosine-modified lipid nanocapsules

et al. 2021

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“…İtrakonazol (ITC) yüklü jel bazlı LNC'lerin topikal uygulamasına yönelik gerçekleştirilen bir çalışmada, ITC yüklü NLC'ler ile karşılaştırıldığında artmış antifungal aktivite sağlanmıştır [84].…”

Section: Dermal Ve Transdermal Uygulamaunclassified

Yeni̇ Nesi̇l Li̇pi̇t Bazli İlaç Taşiyici Si̇stemler: Li̇pi̇t Nanokapsüller

Demirtaş¹,

Sengel-Türk²

2022

Ankara Universitesi Eczacilik Fakultesi Dergisi

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Amaç: Nanopartiküler ilaç taşıyıcı sistemler, boyuta bağlı özelliklerinden dolayı giderek artan şekilde ilgi görmektedir. Bu sistemler arasında polimerik nanopartiküller ve lipozomlar en popüler nanotaşıyıcılardandır; ancak bu sistemlerde görülen düşük stabilite, kısa raf ömrü, hazırlanmasında organik çözücü kullanımı, ölçek büyütmenin zor olması gibi dezavantajların üstesinden gelmek için araştırmacılar lipit bazlı nanotaşıyıcılara yönelmiştir. Yeni nesil lipidik taşıyıcılardan olan lipid nanokapsüller (LNC), hidrofilik ve lipofilik sert bir surfaktan kabuk ile çevrelenmiş yağlı sıvı çekirdekten oluşan sistemlerdir ve polimerik nanokapsüller ile lipozomlar arasında yer alan hibrit bir yapıya sahiptirler. Bu derleme kapsamında LNC'ler hakkında genel bilgiler, hazırlama yöntemi ve uygulama yollarına ilişkin bilimsel çalışmalar sunulmuştur.Sonuç ve Tartışma: Tüm bileşenleri FDA onaylı olan LNC'ler, organik çözücü içermeyen, düşük enerji tüketimli ve ölçek büyütmeye elverişli patentli bir üretim teknolojisi olan faz inversiyon yöntemiyle kolayca hazırlanabilmektedir. Bu yöntem ile 20-100 nm partikül büyüklüklerinde ve dar bir dağılım aralığında elde edilen LNC'ler yüksek etkin madde yükleme kapasitesine sahip olmaları, yüzey modifikasyonuna elverişli olmaları, yüzeyindeki polietilen glikol zincirleri sayesinde uzun süre kan dolaşımında kalabilmeleri ve fiziksel stabilitelerinin yüksek olması (18 aya kadar) gibi çok sayıda avantaja sahiptirler. LNC'lerin, lipofilik, amfifilik ve hidrofilik özellikteki pek çok etkin madde için oral, parenteral, topikal, pulmuner yollar gibi çeşitli uygulama yolları kullanılarak farklı farmasötik uygulamalarda kullanılması onların potansiyel ilaç taşıyıcı sistemler olduğunu göstermektedir. Sahip oldukları bu üstün özellikler sayesinde LNC'ler başta lipozomlar ve polimerik nanokapsüller olmak üzere ilaç taşıyıcı sistemlerde gözlenen dezavantajların üstesinden gelerek umut verici alternatif yeni nesil ilaç taşıyıcı sistemler olarak karşımıza çıkmaktadır.

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“…The prepared potato dextrose agar medium was poured into the sterile petri plate and thereafter this petri plate was allowed to cool at room temperature (25-28 °C). After the medium was solidified, the fungal strain of Candida albicans was dispersed in the medium [36,37]. After that, with the help of a sterile stainless steel borer 10 mm wells cut in the solidified medium.…”

Section: Antifungal Activitymentioning

confidence: 99%

Formulation and Development of Curcumin Based Emulgel in Treatment and Recurrence of Vaginal Candidiasis

Bairagi

Patel

2021

Int J Curr Pharm Sci

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Objective: The main causative agent of vaginal candidiasis is Candida albicans and it develops resistance against several synthetic antifungal drugs and it has a high rate of infection in women. According to WHO report, around 75% of women are infected by Candida albicans and 50 % are infected a second time by Candida albicans. Therefore, we choose Curcumin an antifungal agent that had reported antifungal properties against the various fungal species. The Curcumin-containing emulgel based microemulsion system was prepared for greater retention time and penetration across the vaginal mucosa. Methods: The screening of oil phase, surfactant, and cosurfactant for microemulsion formulation was selected based on the solubility study and followed by the construction of the pseudoternary phase diagram. The oil phase, surfactant and co-surfactant are selected from the pseudoternary phase diagram for the formulation of a stable microemulsion. The prepared Curcumin-loaded microemulsion was characterized by globule size, polydispersity index, Zeta potential, accelerated stability study, drug content, percent transmittance and antifungal assay by broth microdilution technique. The formulated microemulsion was converted into a vaginal emulgel by using Pluronic@F127. The formulated curcumin-loaded emulgel was characterized by different evaluation parameters and antifungal study by agar well diffusion method. Results: The result showed that the average globule size of emulgel was 286.3 nm, polydispersity index was 0.241, Zeta potential was+19.20 mv, conductivity was 0.0390 mS/cm, and drug content was found to be 95.58%. The texture of formulated emulgel was found to be soft and smooth, with shear-thinning, pseudoplastic behavior, and easily spreadable. The in vitro permeability study of emulgel shows slow and complete release of curcumin in 10 h. The microemulsion and developed emulgel showed promising antifungal activity against Candida albicans. Conclusion: The developed curcumin-loaded emulgel showed promising antifungal activity against Candida albicans as compared to the Fluconazole as an standard antifungal antibiotic. Our formulated Curcumin-containing emulgel can be a potential alternative as compared to the conventional dosage form for the treatment of vaginal candidiasis.

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Itraconazole lipid nanocapsules gel for dermatological applications: In vitro characteristics and treatment of induced cutaneous candidiasis

Cited by 39 publications

References 57 publications

Enhancing the in vitro and in vivo activity of itraconazole against breast cancer using miltefosine-modified lipid nanocapsules

Enhancing the in vitro and in vivo activity of itraconazole against breast cancer using miltefosine-modified lipid nanocapsules

Yeni̇ Nesi̇l Li̇pi̇t Bazli İlaç Taşiyici Si̇stemler: Li̇pi̇t Nanokapsüller

Formulation and Development of Curcumin Based Emulgel in Treatment and Recurrence of Vaginal Candidiasis

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