In vitro and in vivo characterization of pharmaceutical topical nanocarriers containing anticancer drugs for skin cancer treatment

Gupta, Vandana; Trivedi, Piyush

doi:10.1016/b978-0-12-813687-4.00015-3

Cited by 59 publications

(32 citation statements)

References 228 publications

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“…The present results showed that all formulations follow non-Fickian release mechanism except NG6, which represent that the release of naringenin from the NG1 to NG5 will be through diffusion and erosion, whereas release kinetics from NG6 will follow completely diffusion. Further, this can be correlated with the highest viscosity of NG6, which is in congruent to the literature where it had been mentioned high viscous formulation led to high diffusion rates compared to low viscous formulation ( Gupta and Trivedi, 2018 ).…”

Section: Resultssupporting

confidence: 88%

Tocotrienols-rich naringenin nanoemulgel for the management of diabetic wound: Fabrication, characterization and comparative in vitro evaluations

Yeo

Chieng

Choudhury

et al. 2021

Current Research in Pharmacology and Drug Discovery

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The present research had been attempted to formulate and characterize tocotrienols-rich naringenin nanoemulgel for topical application in chronic wound conditions associated with diabetes. In due course, different phases of the nanoemulsion were chosen based on the solubility study, where combination of Capryol 90 and tocotrienols, Solutol HS15, and Transcutol P were selected as oil, surfactant, and cosurfactant, respectively. The nanoemulsions were formulated using the spontaneous emulsification method. Subsequently, Carbopols were incorporated to develop corresponding nanoemulgels of the optimized nanoemulsions. Thermodynamically stable optimized nanoemulgels were evaluated for their globule size, polydispersity index (PDI), surface charge, viscosity, mucoadhesive property, spreadability, in vitro release and release mechanism. Further, increasing polymer concentration in the nanoemulgels was reflected with the increased mucoadhesive property with corresponding decrease in the release rate of the drug. The optimized nanoemulgel (NG1) consisted of uniform dispersion (PDI, 0.452 ± 0.03) of the nanometric globules (145.58 ± 12.5) of the dispersed phase, and negative surface charge (−21.1 ± 3.32 mV) with viscosity 297,600 cP and good spreadability. In vitro release of naringenin in phosphate buffer saline revealed a sustained release profile up to a maximum of 74.62 ± 4.54% from the formulated nanoemulgel (NG1) within the time-frame of 24 h. Alternatively, the release from the nanoemulsion was much higher (89.17 ± 2.87%), which might be due to lack of polymer coating on the dispersed oil droplets. Moreover, the in vitro release kinetics from the nanoemulgel followed the first-order release and Higuchi model with non-Fickian diffusion. Therefore, encouraging results in this research is evident in bringing a promising future in wound management, particularly associated with diabetes complications.

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Section: Resultssupporting

confidence: 88%

Tocotrienols-rich naringenin nanoemulgel for the management of diabetic wound: Fabrication, characterization and comparative in vitro evaluations

Yeo

Chieng

Choudhury

et al. 2021

Current Research in Pharmacology and Drug Discovery

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“…It is known that increasingly negative or positive zeta-potential values (i.e., >30 mV or ˂−30 mV) signify increased electrostatic repulsion between droplets, and are therefore considered favorable as coagulation is circumvented [ 68 ]. Nevertheless, a minute deviation is allowed as research recognized that emulsions stabilized by both steric and combined electrostatic forces, as enabled by Tween ® 80, with a minimum zeta-potential value of −20 mV, can be contemplated acceptable [ 69 , 70 ]. The negatively charged zeta-potential values obtained ( Table 3 ) are initiated by the presence of free fatty acids within the oil phase [ 71 ].…”

Section: Resultsmentioning

confidence: 99%

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

2020

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A quality-by-design and characterization approach was followed to ensure development of self-emulsifying drug delivery systems (SEDDSs) destined for topical delivery of the highly lipophilic clofazimine. Solubility and water-titration experiments identified spontaneous emulsification capacity of different excipient combinations and clofazimine. After identifying self-emulsification regions, check-point formulations were selected within the self-emulsification region by considering characteristics required to achieve optimized topical drug delivery. Check-point formulations, able to withstand phase separation after 24 h at an ambient temperature, were subjected to characterization studies. Experiments involved droplet size evaluation; size distribution; zeta-potential; self-emulsification time and efficacy; viscosity and pH measurement; cloud point assessment; and thermodynamic stability studies. SEDDSs with favorable properties, i.e., topical drug delivery, were subjected to dermal diffusion studies. Successful in vitro topical clofazimine delivery was observed. Olive oil facilitated the highest topical delivery of clofazimine probably due to increased oleic acid levels that enhanced stratum corneum lipid disruption, followed by improved dermal clofazimine delivery. Finally, isothermal microcalometric experiments studied the compatibility of excipients. Potential interactions were depicted between argan oil and clofazimine as well as between Span®60 and argan-, macadamia- and olive oil, respectively. However, despite some mundane incompatibilities, successful development of topical SEDDSs achieved enhanced topical clofazimine delivery.

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“…The particle dispersed in an emulsion has a surface charge due to its attraction to a layer of oppositely charged particle; an electric double layer is thus generated [ 24 ]. An absolute value of zeta potential greater than 25 mV generally indicates a stable emulsion [ 21 , 37 , 38 , 39 ]. The zeta potentials of all nanoemulsions tested in this study were in the range –32.0 mV to –38.2 mV ( Table 1 ), which means that the w/o emulsion droplets were negatively charged.…”

Section: Resultsmentioning

confidence: 99%

Water-in-Oil-in-Water Nanoemulsions Containing Temulawak (Curcuma xanthorriza Roxb) and Red Dragon Fruit (Hylocereus polyrhizus) Extracts

2021

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Hydrophobic curcumin in temulawak extract and hydrophilic betacyanin in red dragon fruit extract are high-value bioactive compounds with extensive applications in functional food. In this study, these extracts were encapsulated in water-in-oil-in-water (w/o/w) nanoemulsions as a delivery system using a two-step high-energy emulsification method. PGPR and Span 20 were used as lipophilic emulsifiers for the primary w/o emulsion. The most stable w/o/w formulation with the least oil phase separation of 5% v/v consisted of w/o emulsion (15% w/w) and Tween 80 (1.5% w/w) as hydrophilic emulsifier. The formulation was characterized by a 189-nm mean droplet diameter, 0.16 polydispersity index, and –32 mV zeta potential. The freeze–thaw stability may be attributed to the combination of low w/o emulsion content and high Tween 80 concentration in the outer water phase of the w/o/w nanoemulsions used in this study. The IC50 values of the nanoemulsion and the red dragon fruit extract were similar. It means that the higher concentration of curcumin in the nanoemulsions and the lower IC50 value of temulawak extract ensured sufficient antioxidant activities of the w/o/w nanoemulsions.

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In vitro and in vivo characterization of pharmaceutical topical nanocarriers containing anticancer drugs for skin cancer treatment

Cited by 59 publications

References 228 publications

Tocotrienols-rich naringenin nanoemulgel for the management of diabetic wound: Fabrication, characterization and comparative in vitro evaluations

Tocotrienols-rich naringenin nanoemulgel for the management of diabetic wound: Fabrication, characterization and comparative in vitro evaluations

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

Water-in-Oil-in-Water Nanoemulsions Containing Temulawak (Curcuma xanthorriza Roxb) and Red Dragon Fruit (Hylocereus polyrhizus) Extracts

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