Implementing Central Composite Design for Developing Transdermal Diacerein-Loaded Niosomes: Ex vivo Permeation and In vivo Deposition

Aziz, Diana; Abdelbary, Ahmed; Elassasy, Abdelhalim I.

doi:10.2174/1567201815666180619105419

Cited by 43 publications

(25 citation statements)

References 54 publications

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“…The adjusted R 2 is the modified version of R 2 that designates the goodness of fit of the chosen model to the observed data. The values of adjusted and predicted R 2 statistics should be within about 0.20 of each other in order to be in reasonable harmony [ 35 ]. Table 2 demonstrates that the values of R 2 , predicted R 2 and adjusted R 2 for different responses are relatively high.…”

Section: Resultsmentioning

confidence: 99%

“…The higher permeation of EGCG-loaded SNVs could be explained on the basis of the higher deformability of spanlastic vesicles due to the presence of the EAs that increase the permeability of the SNVs across different biological membranes by squeezing through their narrow pores without rupture [ 55 ]. Additionally, the SNVs act as permeation enhancers that increase the drug permeability through biological membranes [ 35 ].…”

Section: Resultsmentioning

confidence: 99%

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Formulation and Optimization of Nanospanlastics for Improving the Bioavailability of Green Tea Epigallocatechin Gallate

et al. 2021

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The present study aimed to investigate the potential of nanospanlastics for boosting the bioavailability of epigallocatechin gallate (EGCG). EGCG has valuable effects like anti-inflammation, anti-oxidation, and anti-tumorigenesis. Unfortunately, it has a low oral bioavailability due to its limited permeation and poor stability. To overcome these pitfalls, EGCG was fabricated as a nanospanlastic. Nanospanlastics are flexible nanovesicles that are composed of surfactants and edge activators (EAs). EAs improve the deformability of spanlastics by acting as a destabilizing factor of their vesicular membranes. EGCG-loaded spanlastics were prepared by an ethanol injection method, according to 23 factorial design, to explore the impact of different independent variables on entrapment efficiency (EE%), % drug released after 12 h (Q12h), and particle size (PS). In vitro characterization, ex vivo intestinal permeation test, and pharmacokinetic study of the optimized formula were performed. A newly developed RP-HPLC technique was adopted for the estimation of EGCG. The optimized formula (F4) demonstrated more prolonged drug release and a significant improvement in the EE%, permeability, deformability and stability than the corresponding niosomes. The pharmacokinetic study investigated that F4 had a more sustained drug release and a higher bioavailability than the conventional niosomes and free drugs. Nanospanlastics could be a promising approach for improving the bioavailability of EGCG.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Formulation and Optimization of Nanospanlastics for Improving the Bioavailability of Green Tea Epigallocatechin Gallate

et al. 2021

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“…The optimal DCN-loaded niosomes (optimized using central composite design) were prepared in hydration medium with no salt and with a lipid:surfactant ratio of 150 mg:5 parts. The optimal niosomes composition was regulated using edge activators to give elastic vesicles for comparing with optimal niosomes [ 113 ]. The optimal niosomes enhanced the skin permeation of DCN ex vivo with up to four times better than the drug suspension.…”

Section: Cholesterol-based Compounds In Transdermal Drug Deliverymentioning

confidence: 99%

“…The elastic vesicle was more effective than the optimal niosomes and improved drug retention and deposition within the skin [ 114 ]. The optimized niosomes proved their ability to transdermally deliver DCN, avoiding problems associated with oral administration [ 113 ].…”

Section: Cholesterol-based Compounds In Transdermal Drug Deliverymentioning

confidence: 99%

The Efficacy of Cholesterol-Based Carriers in Drug Delivery

Ruwizhi

Aderibigbe

2020

Molecules

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Several researchers have reported the use of cholesterol-based carriers in drug delivery. The presence of cholesterol in cell membranes and its wide distribution in the body has led to it being used in preparing carriers for the delivery of a variety of therapeutic agents such as anticancer, antimalarials and antivirals. These cholesterol-based carriers were designed as micelles, nanoparticles, copolymers, liposomes, etc. and their routes of administration include oral, intravenous and transdermal. The biocompatibility, good bioavailability and biological activity of cholesterol-based carriers make them potent prodrugs. Several in vitro and in vivo studies revealed cholesterol-based carriers potentials in delivering bioactive agents. In this manuscript, a critical review of the efficacy of cholesterol-based carriers is reported.

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“…Span60's long saturated alkyl chain resulted in more preamble niosomes as an influential factor, resulting in multiplied drug encapsulation(39). Besides, Span60 surfactant has a lipophilic balance of 4.7 which is lower than that of Span40 (6.7), resulting in the formation of smaller vesicles(40).Therefore, the F1 formulation was revealed to have a more suitable size and morphological features compared to other formulations. The Span40 used in F2, F3, and F4 formulations resulted in larger vesicles compared to that of F1 due to their high hydrophilic-lipophilic balance.…”

mentioning

confidence: 99%

Encapsulation and Characterization of Meropenem in Niosome Nanoparticles and Inhibitory Effects of Antibiofilm and Antibacterial on Methicillin and Vancomycin Resistant Strains of Staphylococcus Aureus

Shirin

Gharaghie

Beiranvand

et al. 2021

Preprint

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Background: We aim to assess the antibacterial and anti-biofilm properties of niosome-encapsulated meropenem. Methods: After isolating S. aureus isolates and determining their microbial sensitivity, their ability to form biofilms was examined using plate microtiter assay. Various formulations of niosome-encapsulated meropenem were prepared using the thin-film hydration method, Minimum Biofilm Inhibitory Concentration (MBIC) and Minimum Inhibitory Concentration (MIC) were determined, and biofilm genes expression was examined. Drug formulations’ toxicity effect on HDF cells were determined using MTT assay.Results: Out of the 162 separated Staphylococcus aureus, 106 were resistant to methicillin. 87 MRSA isolates were vancomycin-resistant, all of which could form biofilms. The F1 formulation of neoplastic meropenem with a size of 51.3 ± 5.84 and an encapsulation index of 84.86 ± 3.14 was detected, which prevented biofilm growth with a BDI index of 69% and reduced icaD, FnbA, Ebps biofilms’ expression with p ≤0.05 in addition to reducing MBIC and MIC by 4-6 times. Interestingly, F1 formulation of neoplastic meropenem indicated cell viability over 90% at all tested concentrations. Conclusions: Results of the present study indicate that niosome-encapsulated meropenem reduces the resistance of Staphylococcus aureus MRSA to antibiotics in addition to increasing its anti-biofilm and antibiotic activity, and could prove useful as a new strategy for drug delivery.

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Implementing Central Composite Design for Developing Transdermal Diacerein-Loaded Niosomes: Ex vivo Permeation and In vivo Deposition

Abstract: Results revealed that a transdermal niosomal system was successfully prepared and evaluated using central composite design which will result in delivering diacerein efficiently, avoiding its oral problems.

Cited by 43 publications

References 54 publications

Formulation and Optimization of Nanospanlastics for Improving the Bioavailability of Green Tea Epigallocatechin Gallate

Formulation and Optimization of Nanospanlastics for Improving the Bioavailability of Green Tea Epigallocatechin Gallate

The Efficacy of Cholesterol-Based Carriers in Drug Delivery

Encapsulation and Characterization of Meropenem in Niosome Nanoparticles and Inhibitory Effects of Antibiofilm and Antibacterial on Methicillin and Vancomycin Resistant Strains of Staphylococcus Aureus

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