Comparison of LNS-AmB, a novel low-dose formulation of amphotericin B with lipid nano-sphere (LNS®), with commercial lipid-based formulations

Fukui, Hiroshi; Koike, Tomohiro; Nakagawa, Takashi; Saheki, Akira; Sonoke, Satoru; Tomii, Yoshifumi; Seki, Junzo

doi:10.1016/j.ijpharm.2003.08.002

Cited by 53 publications

(24 citation statements)

References 29 publications

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“…If the nanoemulsions induce hemolysis and adsorb to hemoglobin or cell debris, they are rapidly cleared by macrophages (97). Likewise, due to longer plasma half-life of nanoemulsions, there is a greater tendency of them to interact with blood components which increases the likelihood of inducing thrombogenicity which can lead to partial or complete occlusion of blood vessels (98,99). Further to this, the uptake of nanoemulsions by immune cells and macrophages can be facilitated by the adsorption of opsonins to the surface of the nanoemulsions which can redirect the delivery systems to endogenous clearance mechanisms reducing drug delivery and efficacy at the target site (100).…”

Section: In Vivo Fate Of Nanoemulsions Interactions With Blood Componmentioning

confidence: 99%

Nanoemulsions in Translational Research—Opportunities and Challenges in Targeted Cancer Therapy

et al. 2014

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Abstract. Nanoemulsion dosage form serves as a vehicle for the delivery of active pharmaceutical ingredients and has attracted great attention in drug delivery and pharmacotherapy. In particular, nanoemulsions act as an excellent vehicle for poorly aqueous soluble drugs, which are otherwise difficult to formulate in conventional dosage forms. Nanoemulsions are submicron emulsions composed of generally regarded as safe grade excipients. Particle size at the nanoscale and larger surface area lead to some very interesting physical properties that can be exploited to overcome anatomical and physiological barriers associated in drug delivery to the complex diseases such as cancer. Along these lines, nanoemulsions have been engineered with specific attributes such as size, surface charge, prolonged blood circulation, target specific binding ability, and imaging capability. These attributes can be tuned to assist in delivering drug/imaging agents to the specific site of interest, based on active and passive targeting mechanisms. This review focuses on the current state of nanoemulsions in the translational research and its role in targeted cancer therapy. In addition, the production, physico-chemical characterization, and regulatory aspects of nanoemulsion are addressed.

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Section: In Vivo Fate Of Nanoemulsions Interactions With Blood Componmentioning

confidence: 99%

Nanoemulsions in Translational Research—Opportunities and Challenges in Targeted Cancer Therapy

et al. 2014

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“…Moreover, in some literature, it has been reported that liposomal AmB and free AmB had comparable antifungal activities against various fungi such as Candida spp., Aspergillus spp. and Fusarium spp [Fukui et al, 2003a). The transfer mechanism of AmB from lipidic carriers to fungal cells was not fully understood.…”

Section: Sem Of Erythrocytementioning

confidence: 99%

Nanoemulsion gel-based topical delivery of an antifungal drug:in vitroactivity andin vivoevaluation

Samad²,

et al. 2014

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Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard University, New Delhi, India AbstractObjective: In this study, attempt has been focused to prepare a nanoemulsion (NE) gel for topical delivery of amphotericin B (AmB) for enhanced as well as sustained skin permeation, in vitro antifungal activity and in vivo toxicity assessment. Materials and methods: A series of NE were prepared using sefsol-218 oil, Tween 80 and Transcutol-P by slow spontaneous titration method. Carbopol gel (0.5% w/w) was prepared containing 0.1% w/w AmB. Furthermore, NE gel (AmB-NE gel) was characterized for size, charge, pH, rheological behavior, drug release profile, skin permeability, hemolytic studies and ex vivo rat skin interaction with rat skin using differential scanning calorimeter. The drug permeability and skin irritation ability were examined with confocal laser scanning microscopy and Draize test, respectively. The in vitro antifungal activity was investigated against three fungal strains using the well agar diffusion method. Histopathological assessment was performed in rats to investigate their toxicological potential.Results and discussion: The AmB-NE gel (18.09 ± 0.6 mg/cm 2 /h) and NE (15.74 ± 0.4 mg/cm 2 /h) demonstrated the highest skin percutaneous permeation flux rate as compared to drug solution (4.59 ± 0.01 mg/cm 2 /h) suggesting better alternative to painful and nephrotoxic intravenous administration. Hemolytic and histopathological results revealed safe delivery of the drug. Based on combined results, NE and AmB-NE gel could be considered as an efficient, stable and safe carrier for enhanced and sustained topical delivery for AmB in local skin fungal infection. Conclusion: Topical delivery of AmB is suitable delivery system in NE gel carrier for skin fungal infection.

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“…This drug's mechanism of action can lead to systemic toxicity, including renal, hepatic, cardiac, and blood dyscrasia and death [1,18]. Concentrations of amphotericin in the blood and renal system are highly dependent on their formulation and delivery mechanism [6]. The recommended dosing regimen to minimize the risk of systemic toxicity is 1.0 mg/kg/day or less [7].…”

Section: Introductionmentioning

confidence: 99%

Amphotericin B Is Cytotoxic at Locally Delivered Concentrations

Harmsen

McLaren

Pauken

et al. 2011

Clinical Orthopaedics &Amp; Related Research

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Comparison of LNS-AmB, a novel low-dose formulation of amphotericin B with lipid nano-sphere (LNS®), with commercial lipid-based formulations

Cited by 53 publications

References 29 publications

Nanoemulsions in Translational Research—Opportunities and Challenges in Targeted Cancer Therapy

Nanoemulsions in Translational Research—Opportunities and Challenges in Targeted Cancer Therapy

Nanoemulsion gel-based topical delivery of an antifungal drug:in vitroactivity andin vivoevaluation

Amphotericin B Is Cytotoxic at Locally Delivered Concentrations

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