Development of ciclopirox olamine topical formulations: evaluation of drug release, penetration and cutaneous retention

Pinheiro, Vanessa Alves; Serikaku, Daniela; Baby, André Rolim; Velasco, Maria Valéria Robles; Kaneko, Telma Mary; Consiglieri, Vladi Olga

doi:10.3109/10837450.2013.860544

Cited by 4 publications

(4 citation statements)

References 22 publications

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“…The topical use of terbinafine and ketoconazole cause allergy to the skin and histopathological alternations in the stratum corneum [ 19 , 65 ]. Moreover, the topical treatment of dermatophytic onychomycosis with ciclopirox olamine has resulted in nail disorder, pruritus, rash, and contact dermatitis [ 66 ]. In this context, compound 5 is a promising candidate for the development of new topic formulations against superficial and cutaneous dermatophytosis.…”

Section: Resultsmentioning

confidence: 99%

Quinolines derivatives as promising new antifungal candidates for the treatment of candidiasis and dermatophytosis

et al. 2020

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Fungal infections have emerged as a current serious global public health problem. The main problem involving these infections is the expansion of multidrug resistance. Therefore, the prospection of new compounds with efficacy antifungal becomes necessary. Thus, this study evaluated the antifungal profile and toxicological parameters of quinolines derivatives against Candida spp. and dermatophyte strains. As a result, a selective anti-dermatophytic action was demonstrated by compound 5 (geometric means (GM = 19.14 μg ml −1 )). However, compounds 2 (GM = 50 μg ml −1 ) and 3 (GM = 47.19 μg ml −1 ) have presented only anti- Candida action. Compounds 3 and 5 did not present cytotoxic action. Compound 5 did not produce dermal and mucosal toxicity. In addition, this compound showed the absence of genotoxic potential, suggesting safety for topical and systemic use. Quinolines demonstrated a potent anti-dermatophytic and anti-yeast action. Moreover, compound 5 presented an excellent toxicological profile, acting as a strong candidate for the development of a new effective and safe compound against dermatophytosis of difficult treatment. Electronic supplementary material The online version of this article (10.1007/s42770-020-00348-4) contains supplementary material, which is available to authorized users.

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Section: Resultsmentioning

confidence: 99%

Quinolines derivatives as promising new antifungal candidates for the treatment of candidiasis and dermatophytosis

et al. 2020

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“…Additionally, previous studies formulated indomethacin in various dosage forms like gels, cream, microparticles, nanospheres and nanoparticles. All these formulations utilized certain types of additives, either as co-solvent [propylene glycol (PG)] (Pinheiro et al, 2015), co-polymer [e.g. methoxy poly(ethylene glycol) in poly(ε-caprolactone)] (Kim et al, 2001), co-solubiliser (e.g.…”

Section: Introduction:-mentioning

confidence: 99%

Topical Co-Delivery of Indomethacin and Nigella Sativa L. Essential Oil in Poly- -Caprolactone Nanoparticles: In Vivo Study of Anti-Inflammatory Activity.

Badri¹,

Mohamed²,

Affendi³

et al. 2018

IJAR

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Indomethacin is a potent, nonselective Non-steroidal Antiinflammatory Drug (NSAID) but its low water-solubility precludes its use as topical dosage form. As with other NSAIDs, the systemic delivery is associated with high risk of serious gastrointestinal adverse events including bleeding, ulceration and perforation of stomach and intestines. Here we demonstrate a safer way of administration i.e via topical demonstrating synergistic effects when co-delivered with Nigella sativa L. seeds essential oil (NSSEO) in the form of coencapsulated particles (~200 nm) of poly--caprolactone. The particles showed penetrability across stratum corneum to dermis layer in ex-vivo human skin. Further study in the xyline-induced ear edema in mice was performed, and co-encapsulated particles demonstrated highest antiinflammatory effect compared to indomethacin particles and indomethacin gels. Despite slower onset compared to indomethacin gels, the inflamed ear continued to show reduction in thickness over 8 hours of observation demonstrating synergistic and pro-longed effect contributed by NSSEO. In immunohistochemistry study of CD45+, the mice ears treated with co-encapsulated particles showed considerable reduction in lesions, epidermal-dermal separation and inflammatory cells (lymphocytes and neutrophils) infiltration as compared to other formulation. Based on microscopic evaluation, the anti-inflammatory inhibition effect of co-encapsulated particles is the highest (90%) followed by indomethacin particles (79%) and indomethacin gel (49%). The findings suggest not only skin permeability of indomethacin significantly improved but also the therapeutic effects, all provided by the presence of NSSEO in the particles. This study paves the way to

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“…Drug concentrations in the skin during skin permeation experiments using Franz cells are indicators of topical distribution, whereas drug concentrations in the receptor phase are indicators of transdermal delivery. 24 Due to greater drug retention in the skin and minimal drug quantification in the receptor solution. Thus, it was determined that mupirocin's created emulgel was more effective when applied topically.…”

Section: Discussionmentioning

confidence: 99%

Development and Characterization of Mupirocin Emulgel for the Treatment of Primary and Secondary Infections in Dry Skin Conditions

Kausdikar¹,

Kondawr²,

Sayyad³

2022

Int J. Pharm. Investigation

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The general public frequently has dry skin. Erythema, edoema, exudation, and crusting are signs of an inflammatory reaction when dry skin is present together with chapping or underlying dermatoses. The most common skin conditions where dry skin may be a symptom include ichthyosis, psoriasis, and dermatitis/eczema. Primary and secondary infections can occur in these conditions. Therapeutically, secondary skin infections, such as dermatoses in atopic dermatitis, psoriasis, and infected wounds, are more problematic than original skin infections. 1,2 One of the dermatitis kinds in which primary and secondary infections are likely to occur is atopic dermatitis (AD). Due to skin sores that were damaged by scratching and became vulnerable to bacterial infections, impetigo became prevalent in AD. 3 Pustules and crusts are the first symptoms of secondarily infected atopic dermatitis. because secondary symptoms of AD are associated with increased stratum corneum Staphylococcus aureus colonization, alteration of the epidermal barrier, and faulty innate immunological responses. 4 When a person has pustular psoriasis (PP), Staphylococcus aureus can cause secondary infections that can arise from pustules and, in rare cases, blood cultures. 5 Topical fusidic acid, topical mupirocin, oral penicillins that are resistant to penicillinase, including oxacillin, and oral cephalosporin are the antibiotics prescribed for secondary infections of AD. It is recommended for the topical treatment of primary and secondary skin infections in primary pyodermas like impetigo, folliculitis, furunculosis, and ecthyma, as well as secondary infected dermatoses like eczema, psoriasis, and AD. Mupirocin is a novel topical antibacterial agent and metabolite of Pseudomonas fluorescens fermentation. In order to effectively block bacterial protein synthesis, mupirocin forms a link with the enzyme isoleucyl-t-RNA synthetase. This prevents isoleucine from being incorporated into protein chains. Mupirocin exhibits activity against gram-positive cocci in vitro, including Streptococcus pyogenes, Staphylococcus aureus, and other b-hemolytic streptococci. Due to its fast break down into an inactive metabolite in the plasma when administered systemically, mupirozin is only utilized as a topical agent. 6,7 To directly treat cutaneous problems, a topical administration device applies a drug-containing formulation to any external body surface by injunction, spraying, dusting, or injection. Topical gel is suitable for the treatment of dermatological conditions, including in scalp conditions like psoriasis, because it is simple to apply and wash off, easy to apply on hair-bearing areas, and nongreasy. The hydrophobic drug delivery is more difficult and results in a nonocclusive film, which restricts their usefulness as an occlusive emolliating vehicle. 8 In essence, emulgels, also known as emulsified gels, are biphasic systems that have an aqueous gel mixed with a lipid phase, closely resembling a cream. Greaseless, calming, protecting, thixotropic, readily spreadabl...

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Development of ciclopirox olamine topical formulations: evaluation of drug release, penetration and cutaneous retention

Cited by 4 publications

References 22 publications

Quinolines derivatives as promising new antifungal candidates for the treatment of candidiasis and dermatophytosis

Quinolines derivatives as promising new antifungal candidates for the treatment of candidiasis and dermatophytosis

Topical Co-Delivery of Indomethacin and Nigella Sativa L. Essential Oil in Poly- -Caprolactone Nanoparticles: In Vivo Study of Anti-Inflammatory Activity.

Development and Characterization of Mupirocin Emulgel for the Treatment of Primary and Secondary Infections in Dry Skin Conditions

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