Amphotericin B-Loaded Emulgel: Effect of Chemical Enhancers on the Release Profile and Antileishmanial Activity In Vitro

Pinheiro, Iluska Martins; Carvalho, Ivana Pereira Santos; Neto, José Alves Terceiro; Lopes, Gláucia Laís Nunes; Coêlho, Elvilene de Sousa; Sobrinho-Júnior, Enoque Pereira Costa; Alves, Michel Muálem de Moraes; Carvalho, Fernando Aécio de Amorim; Carvalho, André Luís Menezes

doi:10.1208/s12249-019-1323-1

Cited by 8 publications

(3 citation statements)

References 25 publications

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“…Gel forming agents in hydrogels exhibit multiple functions such as thickeners (increase the viscosity of formulation) and as emulsifiers (decrease the interfacial tension) to enhance the stability of emulgels (Bonacucina et al., 2009; Javed et al., 2018; Sohail et al., 2018). Thus, emulgels have been researched for the delivery of hydrophobic drug such as propolis, cyclosporine A, and amphotericin B (Shen et al., 2015; Balata et al., 2018; Pinheiro et al., 2019). From various experimental finding regarding emulgel delivery system, it was found that nanosized (generally range from 20 to 500 nm) emulsion gained the advantages of large surface area which allows rapid penetration through the pores to reach the systemic circulation.…”

Section: Introductionmentioning

confidence: 99%

Eprinomectin nanoemulgel for transdermal delivery against endoparasites and ectoparasites: preparation, in vitro and in vivo evaluation

Mao

Chen

et al. 2019

Drug Delivery

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Nanoemulgels are composed of O/W nanoemulsion and hydrogels and are considered as ideal carriers for the transdermal drug delivery because these have high affinity to load hydrophobic drugs. The stable formulation of eprinomectin (EPR) is very challenging because of it is high hydrophobic nature. In this work, we have prepared EPR loaded nanoemulgel for the treatment of endo-and ectoparasites. The surface morphology of optimized formulations was characterized by scanning electron microscopy. Additionally, skin permeability and irritation tests were conducted for in vitro safety and in vivo skin retention and pearmeation test of EPR nanoemulgel were conducted for efficacy study. Obtained results indicated that the optimized formulation had good shear-thinning behavior, bioadhesiveness properties, and are nanosized droplets with porous internal structure, which are required for topical application. Furthermore, this formulation has showed good skin permeability in comparison to suspension and has no skin irritating property. Overall, the obtained results proved that nanoemulgel is a promising carrier for transdermal drug delivery and EPR nanoemulgel is a promising formulation for the treatment of endo-and ectoparasites.

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Section: Introductionmentioning

confidence: 99%

Eprinomectin nanoemulgel for transdermal delivery against endoparasites and ectoparasites: preparation, in vitro and in vivo evaluation

Mao

Chen

et al. 2019

Drug Delivery

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“…According to USP, the apparent viscosity of semi-solid pharmaceutical products should be evaluated at the beginning of production and during shelf life since viscosity is the critical factor in drug release from formulation [30]. There is an inverse relationship between viscosity and drug release rate, and as the viscosity increases, the drug diffusion decreases [31].…”

Section: Viscosity and Rheological Propertiesmentioning

confidence: 99%

Formulation and evaluation of emulgel containing Sucralfate and Dimethicone; A novel transdermal pharmaceutical dosage form

Ghanbarveisi¹,

Pourmanouchehri²,

Khaledian³

et al. 2022

jrp

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Considering the lack of oxygen, prolonged pressure, and infection are common features of most chronic wounds, especially in pressure ulcers, finding a way to heal the wounds at the early stages is essential. Various pharmaceutical dosage forms are used to act against the infection and prevent the development of this painful condition. The present study aimed to prepare and evaluate topical emulgel formulation for use in the treatment of patients with grade I and II bedsore. The formulation was prepared through the oil in water (o/w) emulsion of organic and aqueous parts to prepare a depot for the transfer of the hydrophobic drug. Emulgel contains sucralfate (Suc), as the epidermal growth factor (EGF) and basic fibroblast growth factor (bFGF) could increase the wound healing rate in these patients. The results showed that the emulgel was stable, homogenous non-discolored, and had a constant pH. In terms of microbial content, it was within the acceptable range of pharmacopeia, and the preservatives had a suitable performance. The product had good spreadability. Rheological studies demonstrated that the prepared formulation had thixotropic properties, which is one of the most critical indicators in the design of semi-solid pharmaceutical forms. Topical emulgel containing Suc can be used as an effective pharmaceutical dosage form to treat grade I and II bedsore due to its innovative pharmacological form and the benefits of this drug form along with the moisturizing, softening, and protecting properties of dimethicone and unique properties of Suc.

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“…[ 1 , 3 ]. The drug of first choice for the treatment of leishmaniasis is N-methyl glucamine antimoniate, known commercially as Glucantime®, and Amphotericin B is the second choice [ 4 , 5 ]. However, the currently available treatment requires continuous clinical and laboratory monitoring, exhibits severe side effects, leads to intolerance, sometimes causes treatment dropout, and is expensive [ 6 ].…”

Section: Introductionmentioning

confidence: 99%

Biflavones from Platonia insignis Mart. Flowers Promote In Vitro Antileishmanial and Immunomodulatory Effects against Internalized Amastigote Forms of Leishmania amazonensis

et al. 2021

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Leishmaniasis is an infectious disease that affects millions of people worldwide, making the search essential for more accessible treatments. The species Platonia insignis Mart. (Clusiaceae) has been extensively studied and has gained prominence for its pharmacological potential. The objective of this work was to evaluate the antileishmania activity, cytotoxic effect and activation patterns of macrophages of hydroalcoholic extract (EHPi), ethyl acetate fractions (FAcOEt) and morelloflavone/volkensiflavone mixture (MB) from P. insignis flowers. EHPi, FAcOEt and MB demonstrated concentration-dependent antileishmania activity, with inhibition of parasite growth in all analyzed concentrations. EHPi exhibited maximum effect at 800 μg/mL, while FAcOEt and MB reduced the growth of the parasite by 94.62% at 800 μg/mL. EHPi, FAcOEt and MB showed low cytotoxic effects for macrophages at 81.78, 159.67 and 134.28 μg/mL, respectively. EHPi (11.25 µg/mL), FAcOEt (11.25 and 22.5 µg/mL) and MB (22.5 µg/mL) characterized the increase in lysosomal activity, suggesting a possible modulating effect. These findings open for the application of flowers from a P. insignis flowers and biflavones mixture thereof in the promising treatment of leishmaniasis.

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Amphotericin B-Loaded Emulgel: Effect of Chemical Enhancers on the Release Profile and Antileishmanial Activity In Vitro

Cited by 8 publications

References 25 publications

Eprinomectin nanoemulgel for transdermal delivery against endoparasites and ectoparasites: preparation, in vitro and in vivo evaluation

Eprinomectin nanoemulgel for transdermal delivery against endoparasites and ectoparasites: preparation, in vitro and in vivo evaluation

Formulation and evaluation of emulgel containing Sucralfate and Dimethicone; A novel transdermal pharmaceutical dosage form

Biflavones from Platonia insignis Mart. Flowers Promote In Vitro Antileishmanial and Immunomodulatory Effects against Internalized Amastigote Forms of Leishmania amazonensis

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