Clotrimazole-loaded Eudragit® RS100 nanocapsules: Preparation, characterization and in vitro evaluation of antifungal activity against Candida species

Santos, Sara S.; Lorenzoni, Alessandra Scherer; Ferreira, Luana Mota; Mattiazzi, Juliane; Adams, Andréa Inês Horn; Denardi, Laura Bedin; Alves, Sydney Hartz; Schaffazick, Scheila Rezende; Cruz, Letícia

doi:10.1016/j.msec.2012.12.040

Cited by 71 publications

(29 citation statements)

References 32 publications

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“…Thus, improving CLT's solubility and rate of release is essential to achieve rapid antimycotic activity. Previous studies to improve the solubility of clotrimazole show the possibility of preparing liposomes, microcapsules, suspensions with a polymer, nanoemulsion, nanospheres, cyclodextrin inclusion complex and solid dispersions with a substance [3,7,8]. Systemic delivery of inclusion complex of clotrimazole with cyclodextrins for oral administration and for rectal administration in suppositories on the basis poloxamer-propylene glycol are characterized by low drug loading and incomplete drug dissolution [9].…”

Section: Clotrimazolementioning

confidence: 99%

Physicochemical Characterization and Dissolution Studies of Solid Dispersions of Clotrimazole with Pluronic F127

Karolewicz¹,

Gajda

Owczarek³

et al. 2014

Trop. J. Pharm Res

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Purpose: To evaluate the physicochemical properties of clotrimazole (CLT) solid dispersion with Pluronic F127 (PLU). Methods: Solid dispersions of the antifungal drug, clotrimazole, were prepared with Pluronic F127 using grinding (PM) and fusion (FUS) methods. Physicochemical characterization of the dispersions were performed using differential scanning calorimetry (DSC), x-ray powder diffraction (XRPD) and Fourier transform infrared spectroscopy (FTIR

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Section: Clotrimazolementioning

confidence: 99%

Physicochemical Characterization and Dissolution Studies of Solid Dispersions of Clotrimazole with Pluronic F127

Karolewicz¹,

Gajda

Owczarek³

et al. 2014

Trop. J. Pharm Res

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“…24 The formulation has shown high skin adhesion 17 and no skin irritation in humans. 13 In addition to cutaneous administration, use of Eudragit RS 100 nanocapsules has been described for ocular 25 and vaginal 26 routes of administration. The aim of this work was to evaluate the performance of chitosan hydrogels containing cationic and anionic acrylicbased nanocapsules (Eudragit RS 100 and Eudragit ® S 100 [Evonik Industries AG], respectively), with Nile red (NR) as a model lipophilic substance, for vaginal administration, as measured by increased residence time and penetration of these formulations.…”

Section: Introductionmentioning

confidence: 99%

Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery

Frank¹,

Sandri²,

D’Autilia³

et al. 2014

IJN

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The vaginal route of administration is an alternative for several treatments for either local or systemic pharmacological effects. However, the permanence of a drug in this route represents a challenge for formulation development that can be overcome by using nanoencapsulation and chitosan gel. Thus, this work aimed to evaluate the performance of chitosan hydrogels containing cationic and anionic acrylic-based nanocapsules (Eudragit ® RS 100 and Eudragit ® S 100, respectively) with Nile red as a model of lipophilic substance in the vaginal route of administration, as measured by increases in the residence time and the penetration of these formulations. Several formulations were prepared with increasing chitosan concentrations, and were analyzed in terms of pH and rheological behavior so that the most suitable formulation could be selected. The enhancement of the adhesion (tensile stress test and washability profile) and penetration (confocal laser scanning microscopy and extraction followed by quantification) properties of the formulations, when applied to porcine vaginal mucosa, were evaluated. The nanocapsule suspensions produced presented adequate properties: size of approximately 200 nm (polydispersity index of ≤v0.2); zeta potential around +10 mV for the cationic formulation and -10 mV for the anionic formulation; and pH values of 6.1±0.1 (Eudragit RS 100), 5.3±0.2 (Eudragit S 100), 6.2±0.1 (Nile red loaded Eudragit RS 100), and 5.1±0.1 (Nile red loaded Eudragit S 100). The chitosan formulation presented suitable viscosity for vaginal application and acidic pH (approximately 4.5). The tensile stress test showed that both formulations containing polymeric nanocapsules presented higher mucoadhesion when compared with the formulation without nanocapsules. In the washability experiment, no significant differences were found between formulations. Confocal microscopy and fluorescence quantification after extraction from the mucosa showed higher penetration of Nile red when it was nanoencapsulated, particularly in cationic nanocapsules. The formulations developed based on chitosan gel vehicle at 2.5% weight/weight containing polymeric nanocapsules, especially the cationic nanocapsules, demonstrated applicability for the vaginal delivery of hydrophobic substances.

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“…Por sua vez, os valores de potencial zeta foram determinados por microeletroforese, após diluição das amostras em NaCl (10 mM) no mesmo equipamento [20][21][22][23][24][25][26] .…”

Section: Ne-a Ne-b Nc-pcl-a Nc-pcl-b Nc-eud-a Nc-eud-b Fase Aquosaunclassified

“…Os filmes foram cuidadosamente retirados do contato com o OL, secos com papel e pesados em balança analítica calibrada após 1, 3, 5, 7, 11, 28 e 60 dias de imersão. O ensaio foi realizado em triplicata [20][21] .…”

Section: Introductionunclassified

Sistemas Nanoestruturados Contendo Óleo De Linhaça: Desenvolvimento Tecnológico E Caracterização Físico-Química De Nanoemulsões E Nanocápsulas Poliméricas

Rigon¹,

Giuliani²,

Stangarlin³

et al. 2017

Saúde (Sta. Maria)

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Objetivo: O óleo de linhaça apresenta diversas propriedades terapêuticas, principalmente devido à presença de ácidos poli-insaturados em sua composição. Para melhor eficácia e/ou aumento da estabilidade de óleos vegetais farmacologicamente ativos, sistemas nanoestruturados são desenvolvidos para veiculação deste tipo de substância. Este estudo objetivou desenvolver e caracterizar sistemas nanoestruturados contendo óleo de linhaça. Foram preparadas nanocápsulas poliméricas e nanoemulsões, avaliando-se duas concentrações de óleo (1,5% e 3,0%) em ambas as formulações e dois polímeros, Poli(ε-caprolactona) e Eudragit ® RL100, no desenvolvimento das nanocápsulas. Ambas as formulações apresentaram características adequadas para sistemas coloidais. Em relação às nanoemulsões, houve diferença significativa das características entre as quantidades de óleo, sendo que 1,5% de óleo de linhaça foi a concentração mais satisfatória. Em relação à presença dos polímeros, houve variação apenas dos valores de potencial zeta e pH. Concluindo, as formulações foram consideradas adequadas para o encapsulamento do óleo de linhaça, sendo carreadores promissores para outras substâncias ativas.Descritores: Óleos Vegetais; Óleo de Linhaça; Nanoemulsões: Nanocápsulas Poliméricas. Cristina ABSTRACTObjective: Linseed oil has several therapeutic properties, mainly due to the presence of polyunsaturated acids in its composition. For best efficiency and/or increasing the stability of vegetable oils pharmacologically active, nanoestructured systems are developed to vehicle this type of substance. This study aimed to develop and characterize nanostructured systems containing linseed oil. Polymeric nanocapsules, and nanoemulsions were prepared, evaluating two oil concentrations (1.5% and 3.0%) in both formulations and two polymers, Poli(ε-caprolactona) e Eudragit ® RL100, of the nanocapsules development. Both formulations showed appropriate properties for colloidal systems. Regarding the nanoemulsions, there was a significant difference in characteristics between the amounts of oil, while 1.5% linseed oil was the most satisfying concentration. About presence of polymers, there was variation only of zeta potential and pH values. In conclusion, the formulations were considered suitable for the encapsulation of the linseed oil, being promising carriers for other active substances.

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Clotrimazole-loaded Eudragit® RS100 nanocapsules: Preparation, characterization and in vitro evaluation of antifungal activity against Candida species

Cited by 71 publications

References 32 publications

Physicochemical Characterization and Dissolution Studies of Solid Dispersions of Clotrimazole with Pluronic F127

Physicochemical Characterization and Dissolution Studies of Solid Dispersions of Clotrimazole with Pluronic F127

Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery

Sistemas Nanoestruturados Contendo Óleo De Linhaça: Desenvolvimento Tecnológico E Caracterização Físico-Química De Nanoemulsões E Nanocápsulas Poliméricas

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