Formulation and optimization of long acting dual niosomes using Box-Behnken experimental design method for combinative delivery of Ethionamide and D-cycloserine in Tuberculosis treatment

Kulkarni, Pratik; Rawtani, Deepak; Barot, Tejas

doi:10.1016/j.colsurfa.2019.01.004

Cited by 49 publications

(21 citation statements)

References 42 publications

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“…This was followed by a slow diffusion from the bilayer of the membrane forming the niosomes, showing significant statistical difference in quercetin release when compared to ethanolic quercetin solution (p < 0.01). In addition, the presence of cholesterol, as well as the long hydrophobic alkyl chains (C12) of the tested surfactant, leads to the formation of compact niosomes, which retard the rate of drug release [42]. Finally, the quercetin-release kinetic model from niosomes was best fitted by Higuchi, with an R 2 value of 0.9389, indicating that the release mechanism is diffusion controlled.…”

Section: Preparation and Characterization Of Quercetin Loaded Niosomesmentioning

confidence: 94%

Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay

et al. 2020

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Flavonoids possess different interesting biological properties, including antibacterial, antiviral, anti-inflammatory and antioxidant activities. However, unfortunately, these molecules present different bottlenecks, such as low aqueous solubility, photo and oxidative degradability, high first-pass effect, poor intestinal absorption and, hence, low systemic bioavailability. A variety of delivery systems have been developed to circumvent these drawbacks, and among them, in this work niosomes have been selected to encapsulate the hepatoprotective natural flavonoid quercetin. The aim of this study was to prepare nanosized quercetin-loaded niosomes, formulated with different monolaurate sugar esters (i.e., sorbitan C12; glucose C12; trehalose C12; sucrose C12) that act as non-ionic surfactants and with cholesterol as stabilizer (1:1 and 2:1 ratio). Niosomes were characterized under the physicochemical, thermal and morphological points of view. Moreover, after the analyses of the in vitro biocompatibility and the drug-release profile, the hepatoprotective activity of the selected niosomes was evaluated in vivo, using the carbon tetrachloride (CCl 4 )-induced hepatotoxicity in rats. Furthermore, the levels of glutathione and glutathione peroxidase (GSH and GPX) were measured. Based on results, the best formulation selected was glucose laurate/cholesterol at molar ratio of 1:1, presenting spherical shape and a particle size (PS) of 161 ± 4.6 nm, with a drug encapsulation efficiency (EE%) as high as 83.6 ± 3.7% and sustained quercetin release. These niosomes showed higher hepatoprotective effect compared to free quercetin in vivo, measuring serum biomarker enzymes (i.e., alanine and aspartate transaminases (ALT and AST)) and serum biochemical parameters (i.e., alkaline phosphatase (ALP) and total proteins), while following the histopathological investigation. This study confirms the ability of quercetin loaded niosomes to reverse CCl 4 intoxication and to carry out an antioxidant effect.Pharmaceutics 2020, 12, 143 2 of 18 and anticancer activities [1][2][3]. These intrinsic properties, together with their biocompatibility and remarkable antioxidant activity, have attracted researchers' attention to explore potential therapeutic applications [4,5].Quercetin (3, 30, 4, 5, 7-pentahydroxyflavone) is probably the most studied bioflavonoid, belonging to the family of flavonols; its therapeutic applications include hepatoprotection [6], prevention of neural cell apoptosis [7] and cancer chemo-prevention and treatment [8].Quercetin acts as strong antioxidant by scavenging free radicals and transition metal ions, thus decreasing the process of lipid peroxidation, which is responsible for the development of many diseases, e.g., cardiovascular and neurodegenerative diseases, as well as liver damage [9][10][11].However, quercetin therapeutic applications present challenges due to (i) low aqueous solubility, (ii) photo and oxidative degradability, (iii) high first-pass effect, (iv) poor intestinal absorption and, hence, low systemic...

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Section: Preparation and Characterization Of Quercetin Loaded Niosomesmentioning

confidence: 94%

Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay

et al. 2020

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“…The material used when preparing the drug delivery system The method used when preparing the drug delivery system . antitubercular, 149,150 . immunomodulatory, 151 and .…”

Section: Oral Drug Delivery Systemmentioning

confidence: 99%

Nano Spray-Dried Drugs for Oral Administration: A Review

Öztürk

Arpagaus

2021

ASSAY and Drug Development Technologies

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Spray drying is an important technology that is fast, simple, reproducible, and scalable. It has a wide application range, that is, in food, chemicals, and encapsulation of pharmaceuticals. The technology can be divided into conventional spray drying and nano spray drying. The key advantage of nano spray drying is the production of drug-loaded nanosized particles for various drug delivery applications. The recent developments in nano spray dryer technology and the market launch of the Nano Spray Dryer B-90 by Bu ¨chi Labortechnik AG in 2009 enabled the production of submicron spray-dried particles. This review focuses on nanosized drug delivery systems intended for oral administration produced by nano spray drying. First, the nano spray drying concept, the basic technologies implemented in the equipment, and the effects of the various process parameters on the final dry submicron powder properties are presented. Then, the topics of new formulation strategies of oral drugs are highlighted with examples that have entered the research literature in recent years. Next, the subjects of direct conversion of poorly watersoluble drugs, encapsulation of drugs, and drying of preformed nanoparticles are considered. Finally, topics such as morphology, particle size, size distribution, surface analysis, bioavailability, drug release, release kinetics, and solid-state characterization (by differential scanning calorimetry, X-ray diffraction, Fourier transform infrared spectroscopy, nuclear magnetic resonance) of oral drug delivery systems produced by nano spray drying are discussed. The review attempts to provide a comprehensive knowledge base with current literature and foresight to researchers working in the field of pharmaceutical technology and nanotechnology and especially in the field of nano spray drying.

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“…Ethanol injection (EI) method was used for the preparation of farnesol loaded niosomes [16,17,18]. The Span 20 (non-ionic surfactant) and the cholesterol (lipid) were dissolved in ethanol in a ratio of 1:1 (36.4: 36.4 mg).…”

Section: Preparation and Optimization Of Farnesol Loaded Niosomesmentioning

confidence: 99%

“…Niosomes as a nano-carrier have offered various benefits such as economical fabrication, high stability for nano drug delivery, low systemic toxicity etc. [14,15,16,17]. Niosomes have also shown improved bioavailability, high biocompatibility, reduction in dose concentration, and a sustained drug release [16].…”

Section: Introductionmentioning

confidence: 99%

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Development, characterization and in vitro–in vivo evaluation of Farnesol loaded niosomal gel for applications in oral candidiasis treatment

Barot

Rawtani

Kulkarni

2021

Heliyon

Self Cite

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The aim of the study was to formulate and characterize the farnesol loaded niosomes comprising gel formulation and perform their in vitro-in vivo evaluation for applications in the treatment of oral candidiasis infections. Methods: Various gelling systems were evaluated for their rheological and stability properties. The formulation was statistically optimized using experimental design method (Box-Behnken). Transmission electron microscopy (TEM) and Atomic force microscopy (AFM) were used to observe the niosomal surface morphology. Centrifugation method and dialysis method were used to find out the % entrapment efficiency (%EE) and in-vitro release of Farnesol, respectively. In-vitro antifungal effect and cell biocompatibility of the Farnesol loaded niosomal gel was also performed using Candida albicans (C. albicans) as the model organism and epithelial cell line (SW480) by MTT cytotoxicity assay. In-vivo skin irritation test was performed on rabbit skin. Key findings: Farnesol loaded niosomes were integrated into polymeric gel solution. The optimized formulation demonstrated acceptable % EE (>80%) and an optimum particle size (168.8 nm) along with a sustained release and a long-term storage stability for up to a period of 6 months. TEM and AFM observations displayed a spherical niosome morphology. Farnesol niosomal gel showed a higher antifungal efficacy, ex-vivo skin permeation and deposition in comparison to plain farnesol solution. The niosomal gel also showed negligible cytotoxicity to normal cells citing biocompatibility and was found to be non-toxic and non-irritant to rabbit skin. Conclusions: This novel niosome loaded gel-based formulation could make the oral candidiasis healing process more efficient while improving patient compliance. With the optimized methodology used in this work, such formulation approaches can become an efficient, industrially scalable, and cost-effective alternatives to the existing conventional formulations.

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Formulation and optimization of long acting dual niosomes using Box-Behnken experimental design method for combinative delivery of Ethionamide and D-cycloserine in Tuberculosis treatment

Cited by 49 publications

References 42 publications

Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay

Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay

Nano Spray-Dried Drugs for Oral Administration: A Review

Development, characterization and in vitro–in vivo evaluation of Farnesol loaded niosomal gel for applications in oral candidiasis treatment

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