Delivery of amphotericin B for effective treatment of Candida albicans induced dermal mycosis in rats via emulgel system: Formulation and evaluation

Ganeshpurkar, Aditya; Vaishya, Pooja; Jain, Sumeet; Pandey, Vikas; Bansal, Divya; Dubey, Nazneen

doi:10.4103/0019-5154.135489

Cited by 14 publications

(9 citation statements)

References 17 publications

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“…No erythema= 0, slight erythema (barely-light pink) = 1, moderate erythema (dark pink) = 2, moderate-to-severe erythema (light red)= 3 and severe erythema (extreme redness)= 4 [35][36][37] .…”

Section: Erythemal Scoring System and Visual Observationmentioning

confidence: 99%

Formulation and Evaluation of Cubosomes as Skin Retentive System for Topical Delivery of Clotrimazole

Omar

Ismail

Hassanin

et al. 2019

Journal of Advanced Pharmacy Research

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Objectives: Clotrimazole is a broad-spectrum antimycotic that widely used to treat fungal infections topically. However, poor water solubility of clotrimazole and low skin retention of its topical products present a hindrance for local availability and effectiveness of this drug. This study aimed to formulate and evaluate cubosomes as skin retentive system for topical delivery of clotrimazole. Methods: Six clotrimazole cubosomal dispersions (F1-F6) were prepared by emulsification of glyceryl monoloeate (GMO) and poloxamer 407 at different compositions in water with and without polyvinyl alcohol (PVA).The dispersions were examined under polarizing microscope and transmission electron microscope (TEM) for confirming cubosomes formation. The four cubosomal dispersions (F3-F6) that found to be successfully developed were evaluated in terms of pH, particle size, zeta potential, rheological behavior, entrapment efficiency and in vitro drug release. The formulae F3 (without PVA) and F6 (with PVA) comprising the highest concentration of poloxamer in the disperse phase (15%w/w) provided the highest clotrimazole cumulative percentage release and subjected to comparative ex vivo skin retention and permeation studies with marketed clotrimazole cream. Results: Both F3and F6 showed significantly lower clotrimazole permeation compared to the cream. Moreover, F6achieved the highest skin retention for clotrimazole. The F6 was compared with the cream for its irritation potential in rats and also for antifungal activity in rats inducted with candida albicans. The investigations showed that F6 was well tolerated as the cream. Also,F6 showed superior antifungal activity compared to the available marketed cream. Conclusions: The developed F6 cubosomes is a promising dosage form for safe and effective topical delivery of clotrimazole.

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Section: Erythemal Scoring System and Visual Observationmentioning

confidence: 99%

Formulation and Evaluation of Cubosomes as Skin Retentive System for Topical Delivery of Clotrimazole

Omar

Ismail

Hassanin

et al. 2019

Journal of Advanced Pharmacy Research

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“…Skin irritation test was used on experimental rat to evaluate the irritation potential of tadalafil gel formulations (Bachhav & Pratravale, 2010;Ganeshpurkar et al, 2014). The back of the rat was shaved 24 h prior to the formulation application.…”

Section: Skin Irritation Testmentioning

confidence: 99%

Transdermal delivery of tadalafil using a novel formulation

Baek

Cho

2015

Drug Delivery

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The aim of this work was to investigate the transdermal gel loaded with tadalafil, a practically insoluble selective phosphodiesterase-5 inhibitor (PDE5) in order to improve the solubility and bioavailability. The solubility of tadalafil in mixed solution of hydroxypropyl-b-cyclodextrin (HPCD), polyethylene glycol (PEG) 400 and tween 80 (T2 solution) was 260.8 ± 4.3 mg/mL and that of tadalafil in modified T2 (M-T2) solution, which tadalafil was dissolved in 20% (w/v) HPCD at first and then mixture solutions of PEG 400 and tween 80 were added, was increased to 344.9 ± 30.6 mg/mL. Four gel formulae were prepared, subsequently in vitro and in vivo skin permeation studies were carried out. Interestingly, tadalafil gel in M-T2 and oleic acid (OA) (F3) could promote the percutaneous absorption of tadalafil by 179.4% in vitro and increase AUC by 223% in vivo compared with tadalafil gel in the absence of M-T2 and OA (F1). Also, there was a finding that tadalafil gel in M-T2 and OA did not cause dermal irritations in an experimental animal.

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“…[ 11 ] Due to the low solubility of AmpB in water, it is usually administered as a liposomal or gel formulation to allow higher concentrations to be used intravenously. [ 12,13 ] This approach does not guarantee AmpB will reach the site of infection in a wound. [ 14 ] Another approach is to apply AmpB topically, therefore circumventing systemic cytotoxicity.…”

Section: Introductionmentioning

confidence: 99%

Superenhanced Removal of Fungal Biofilms by Protease‐Functionalized Amphotericin B Nanocarriers

Weldrick

Hardman

Paunov

2021

Advanced NanoBiomed Research

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A strong enhancement in the antifungal activity of amphotericin B (AmpB) encapsulated into shellac nanoparticles (NPs) surface functionalized with protease is reported. These AmpB‐loaded shellac NPs are fabricated by pH‐induced nucleation of aqueous solutions of shellac and AmpB in the presence of Poloxamer 407 (P407) as a steric stabilizer. The AmpB‐loaded shellac NPs are surface coated with the cationic protease Alcalase 2.4L FG. The performance of the AmpB‐encapsulated NPs against Candida albicans is evaluated. The AmpB‐loaded shellac NPs show a remarkable boost of their antifungal action compared to free AmpB when applied to C. albicans in both planktonic and biofilm forms. The surface functionalization with a cationic protease allows the NPs to adhere to the fungal cell walls, delivering AmpB directly to their membranes. Additionally, the hydrolyzing activity of the protease coating degrades the biofilm matrix, thus increasing the effectiveness of the encapsulated AmpB compared to free AmpB at the same concentration. The protease‐coated AmpB‐loaded shellac NPs show no greater toxicity to human adult keratinocyte cells (HaCaT) compared to the free AmpB. These AmpB nanocarriers demonstrat increased efficacy against C. albicans and can be potentially used to treat fungal biofilm infection in the clinic, for example, in recalcitrant chronic wounds.

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Delivery of amphotericin B for effective treatment of Candida albicans induced dermal mycosis in rats via emulgel system: Formulation and evaluation

Cited by 14 publications

References 17 publications

Formulation and Evaluation of Cubosomes as Skin Retentive System for Topical Delivery of Clotrimazole

Formulation and Evaluation of Cubosomes as Skin Retentive System for Topical Delivery of Clotrimazole

Transdermal delivery of tadalafil using a novel formulation

Superenhanced Removal of Fungal Biofilms by Protease‐Functionalized Amphotericin B Nanocarriers

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