Formulation and Optimization of Itraconazole Proniosomes Using Box Behnken Design

Samy, Ahmed M.; Ramadan, Afaf A.; El-Enin, Amal S M Abu; Mortagi, Yasmin

doi:10.22159/ijap.2018v10i2.23382

Cited by 5 publications

(5 citation statements)

References 8 publications

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“…Zeta potential is a measure of the net charge of niosomes. This high charge on the vesicle surface produces repulsion between the vesicles that make them stable without agglomeration providing a uniformly distributed suspension [10]. The positive value of zeta potential could be attributed to the presence of the nitrogen atom in the structure of cationic clopidogrel bisulphate [47].…”

Section: Fig 4: Particle Size Distribution Curve Of Clopidogrel Pronmentioning

confidence: 99%

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Enhancement of Dissolution Characteristics of Clopidogrel Bisulphate by Proniosomes

Mazyed

Zakaria

2019

Int J App Pharm

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Objective: The present investigation aims to formulate and evaluate proniosomes of clopidogrel bisulphate for improving its dissolution characteristics. Methods:The slurry method was used for the preparation of proniosomes of clopidogrel using cholesterol, sorbitan monostearate (Span 60) and maltodextrin as a carrier. Clopidogrel proniosomes were evaluated for their entrapment efficiency and in vitro drug release. The best formula (F1) that achieved maximum drug release was further evaluated by measurement of the angle of repose, morphological examination, determination of vesicle size, determination of zeta potential, Fourier transform infrared spectroscopy and differential thermal analysis. The in vivo behavior of the selected proniosomal formula (F1) was studied by measuring the antiplatelet activity in adult male mice. Results:The entrapment efficiency of clopidogrel proniosomes was in the range of 83.04±1.99 to 90.14±0.30. % drug released from proniosomal formulations was in the range of 79.73±0.35 to 97.70±1.10 % within 4 h. Clopidogrel proniosomes significantly enhanced the in vitro release of clopidogrel compared with the plain drug that achieved 61.77±2.22 % drug release. F1 significantly (p ≤ 0.001) increased the bleeding time and bleeding volume and significantly (p ≤ 0.05) prolonged prothrombin time and decreased prothrombin activity and increased the international normalized ratio (INR) compared to plain clopidogrel. Conclusion:The present investigation introduced proniosomes as a promising carrier for clopidogrel that could enhance its dissolution and pharmacological effect. I In nt te er rn na at ti io on na al l J Jo ou ur rn na al l o of f A Ap pp pl li ie ed d P Ph ha ar rm ma ac ce eu ut ti ic cs s

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Section: Fig 4: Particle Size Distribution Curve Of Clopidogrel Pronmentioning

confidence: 99%

“…Proniosomes could overcome physical instability problems of niosomes [8] and offer better convenience of storage and transportation. Following hydration, proniosomes are converted to niosomes [9,10].…”

Section: Introductionmentioning

confidence: 99%

Enhancement of Dissolution Characteristics of Clopidogrel Bisulphate by Proniosomes

Mazyed

Zakaria

2019

Int J App Pharm

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“…Kumar et al succeeded in obtaining an optimized formulation of itraconazole niosomes with EE% of 73.03 ± 2.39%, a particle size of 272.3 nm, and a zeta potential of −47.2 ± 0.2 [ 47 ]. Samy et al developed itraconazole as proniosomes and were able to obtain an optimized formulation with 94.9 ± 0.36 % regarding the EE%, −30.15 ± 0.41 mV regarding zeta potential, and 340.48 ± 0.581 nm regarding the particle size [ 48 ].…”

Section: Resultsmentioning

confidence: 99%

Preparation and Optimization of Itraconazole Transferosomes-Loaded HPMC Hydrogel for Enhancing Its Antifungal Activity: 2^3 Full Factorial Design

et al. 2023

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Itraconazole (ITZ) is a triazole antifungal agent characterized by broad-spectrum activity against fungal infections. The main drawback of ITZ, when applied topically, is the low skin permeability due to the stratum corneum, the outermost layer of the skin, which represents the main barrier for drug penetration. Therefore, this study aimed to prepare itraconazole as transferosomes (ITZ-TFS) to overcome the barrier function of the skin. ITZ-TFSs were prepared by thin lipid film hydration technique using different surfactants, sodium lauryl sulfate (SLS) and sodium deoxycholate (SDC). The prepared ITZ-TFS were evaluated for entrapment efficiency (EE) %, particle size, polydispersity index (PDI), zeta potential, and in vitro drug release to obtain an optimized formula. The surface morphology of the optimized formula of ITZ-TFS was determined by transmission electron microscope (TEM). The optimized formulation was prepared in the form of gel using hydroxyl propyl methyl cellulose (HPMC) gel base. The prepared ITZ-TFS gel was evaluated for homogeneity, drug content, spreadability, pH, and in vitro antifungal activity in comparison with the free ITZ- gel. The prepared ITZ-TFS formulations exhibited high EE% ranging from 89.02 ± 1.65% to 98.17 ± 1.28% with particle size ranging from 132.6 ± 2.15 nm to 384.1 ± 3.46. The PDI for all ITZ-TFSs was less than 0.5 and had a negative zeta potential. The TEM image for the optimized formulation (ITZ-TFS4) showed spherical vesicles with a smooth surface. The prepared gels had good spreadability, pH, and acceptable drug content. ITZ-TFS gel showed higher antifungal activity than free ITZ gel as determined by zone of inhibition. ITZ was successfully prepared in form of TFSs with higher antifungal activity than the free drug.

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“…Where A and B are emulsifiers, HLB Low is the HLB of lipophilic surfactant, and HLB High is the HLB of hydrophilic surfactant [50,51].…”

Section: Calculating Required Hlbmentioning

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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Formulation and Optimization of Itraconazole Proniosomes Using Box Behnken Design

Cited by 5 publications

References 8 publications

Enhancement of Dissolution Characteristics of Clopidogrel Bisulphate by Proniosomes

Enhancement of Dissolution Characteristics of Clopidogrel Bisulphate by Proniosomes

Preparation and Optimization of Itraconazole Transferosomes-Loaded HPMC Hydrogel for Enhancing Its Antifungal Activity: 2^3 Full Factorial Design

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

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