Co-polymer mixed micelles enhanced transdermal transport of Lornoxicam: in vitro characterization, and in vivo assessment of anti-inflammatory effect and antinociceptive activity

Ahmed, Sadek; Kassem, Mohamed A.; Sayed, Sinar

doi:10.1016/j.jddst.2021.102365

Cited by 17 publications

(14 citation statements)

References 59 publications

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“…The effects of stearic acid concentration (g%) (A), span 80: drug ratio (B) and cholesterol amount (mg) (C) as the independent variables on the different responses of the prepared FTN-loaded novasomes were determined using central composite design (Ahmed et al, 2021 ). Testing of each response was done exclusively and fitted to the model having highest prediction R 2 (Zhang et al, 2010 ).…”

Section: Resultsmentioning

confidence: 99%

“…It is critical to justify the biphasic release profile of the novasomal system as the early burst phase might be due to the desorption of the unentrapped FTN that presents between the large hydrocarbon chains in the lipid bilayer of novasomal system. After that, a slower phase due to the reduced fluidity of the novasomal system by stearic acid and cholesterol (Ahmed et al, 2021 ). Higuchi-diffusion model is the best model to justify the release profiles (highest r-square).…”

Section: Resultsmentioning

confidence: 99%

“…All release profiles were fitted to zero, first, and Higuchi diffusion models. The largest coefficient (R 2 ) suggests the appropriate model (Ahmed et al, 2021 ).…”

Section: Methodsmentioning

confidence: 99%

“…Analysis of central composite design was performed using Design-Expert software version 7 (Stat- Ease Inc., Minneapolis, USA) (Ahmed et al, 2021 ). All measurements were done in triplicates.…”

Section: Methodsmentioning

confidence: 99%

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Corneal targeted fenticonazole nitrate-loaded novasomes for the management of ocular candidiasis: Preparation, in vitro characterization, ex vivo and in vivo assessments

et al. 2022

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The purpose of this manuscript was to develop and optimize Fenticonazole Nitrate (FTN)-loaded novasomes aiming to enhance drug corneal penetration and to improve its antifungal activity. Ethanol injection was used to formulate FTN-loaded novasomes adopting a central composite design. The researched factors were: stearic acid concentration (g%) (A), span 80: drug ratio (B) and cholesterol amount (mg) (C), and their effects on percent entrapment efficiency (EE%), particle size (PS), poly-dispersity index (PDI), zeta potential (ZP), and in vitro drug release after 8 hours (Q8h) were studied. Numerical optimization by Design-Expert® software was employed to select the optimum formula in respect to highest EE%, ZP (as absolute value), and Q8h >80% and lowest PS and PDI. Additional evaluation of the optimum formula was accomplished by short term stability study, effect of gamma sterilization, determination of Minimal Inhibitory Concentration and ex vivo corneal permeation study. The in vivo evaluation of the optimum formula was done to ensure its safety via in vivo ocular irritancy and in vivo corneal tolerance studies. Also, the efficacy was confirmed through in vivo corneal uptake study and susceptibility test. The optimum formula with the highest desirability value (0.738) showed EE% (94.31%), PS (197.05 nm), ZP (-66.95 mV) and Q8h (85.33%). It revealed to be safe, with augmented corneal permeation (527.98 µg/cm 2 ) that leads to higher antifungal activity. The above results confirmed the validity of novasomes to improve the corneal permeation and antifungal activity of Fenticonazole Nitrate.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

“…All release profiles were fitted to zero, first, and Higuchi diffusion models. The largest coefficient (R 2 ) suggests the appropriate model (Ahmed et al, 2021 ).…”

Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Corneal targeted fenticonazole nitrate-loaded novasomes for the management of ocular candidiasis: Preparation, in vitro characterization, ex vivo and in vivo assessments

et al. 2022

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“…Recently, binary mixed micelles replaced monomicellar systems, to avoid low drug loading, large PS, and low stability (Kulthe et al, 2011 ; Ahmed et al, 2021 ). HLB (hydrophilic/lipophilic balance) and CMC (the critical micelle concentration) have an important role regarding the kinetic and thermodynamic stability of the micelles.…”

Section: Resultsmentioning

confidence: 99%

Brain targeting efficiency of intranasal clozapine-loaded mixed micelles following radio labeling with Technetium-99m

Sayed

Elsharkawy²,

Amin

et al. 2021

Drug Delivery

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The research objective is to design intranasal (IN) brain targeted CLZ-loaded polymeric nanomicellar systems (PNMS) aiming to improve central systemic CLZ bioavailability. Direct equilibrium method was used to prepare CLZ-PNMS using two hydrophobic poloxamines; Tetronic V R 904 (T904) and Tetronic V R 701 (T701) and one hydrophilic poloxamer; Synperonic V R PE/F127 (F127). Optimization is based on higher percent transmittance, solubilizing efficiency, and in vitro release after 24 h with smaller particle size was achieved using Design-Expert V R software. The optimized formula was further evaluated via TEM, ex vivo nasal permeation in addition to in vivo biodistribution using radiolabeling technique of the optimized formula by Technetium-99m ( 99m Tc). The optimized formula M5 has small size (217 nm) with relative high percentage of transmittance (97.72%) and high solubilization efficacy of 60.15-fold following 92.79% of CLZ released after 24 h. Ex vivo nasal permeation showed higher flux of 36.62 lg/ cm 2 .h compared to 7.324 lg/cm 2 .h for CLZ suspension with no histological irritation. In vivo biodistribution results showed higher values of radioactivity percentage of the labeled optimized formula ( 99m Tc-M5) in brain and brain/blood ratio following IN administration of 99m Tc-M5 complex which were greater than their corresponding values following intravenous route. It is obvious that nasal delivery of CLZ-PNMS could be a promising way to improve central systemic CLZ bioavailability.

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Polymeric Nanomaterials: Fundamentals and Therapeutic Applications

Maji

Mahajan

Sriram

et al. 2023

Nanomaterial-Based Drug Delivery Systems

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Co-polymer mixed micelles enhanced transdermal transport of Lornoxicam: in vitro characterization, and in vivo assessment of anti-inflammatory effect and antinociceptive activity

Cited by 17 publications

References 59 publications

Corneal targeted fenticonazole nitrate-loaded novasomes for the management of ocular candidiasis: Preparation, in vitro characterization, ex vivo and in vivo assessments

Corneal targeted fenticonazole nitrate-loaded novasomes for the management of ocular candidiasis: Preparation, in vitro characterization, ex vivo and in vivo assessments

Brain targeting efficiency of intranasal clozapine-loaded mixed micelles following radio labeling with Technetium-99m

Polymeric Nanomaterials: Fundamentals and Therapeutic Applications

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