Brucine-loaded transliposomes nanogel for topical delivery in skin cancer: statistical optimization, in vitro and dermatokinetic evaluation

Alhakamy, Nabil A.; Aldawsari, Hibah M; Ali, Javed; Gupta, Dipak Kumar; Warsi, Musarrat Husain; Bilgrami, Anwar L.; Asfour, Hani Z.; Noor, Adeeb; Shadab,

doi:10.1007/s13205-021-02841-5

Cited by 27 publications

(27 citation statements)

References 40 publications

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“…Upon shifting the level of X2 from low to high value, %RE increases from 44.62±1.36% to 66.39±1.24% which indicates a positive correlation between X2 and X3 (verified by the+sign of the coefficient of estimates). As stated previously, VS of TEs decreases with increased SAA concentration and hence increases surface area resulting in higher %RE [34]. A similar pattern also occurs in the case of X3 where the vesicles prepared via labrafil attain %RE of 44.62±1.36% when compared to cremophore 56.72±2.38% and this is in harmony with the outcomes as per Albash et al [1] where SAA with low HLB value slows down the drug release.…”

Section: Influence Of Formulation Variables On Release Efficiencysupporting

confidence: 83%

“…For given levels of each variable, the coded equation yields an estimate of the response (Y2) where the coefficient of estimates for X1 has a positive sign indicating a positive correlation between lipoid S100 concentration and TE vesicle size which means that increasing the level of X1 from 1% (89.97±2.11 nm) to 4% (133.2±1.62 nm) resulted in larger vesicle size. Phospholipid concentration (Lipoid S100) has been demonstrated to alter the vesicular size, with increasing phospholipid concentration increasing the vesicular size by continuing to increase bilayer width [33,34]. On the contrary, X2 and X3 presented a negative correlation with VS based on the sign of the coefficient of estimates (-15.48 and-14.81).…”

Section: Influence Of Formulation Variables On Vesicle Sizementioning

confidence: 99%

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Transethosomes as Breakthrough Tool for Controlled Transdermal Delivery of Dexketoprofen Trometamol: Design, Fabrication, Statistical Optimization, in Vitro, and Ex Vivo Characterization

Soliman

RASHWAN²,

Teaima³

et al. 2022

Int J App Pharm

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Objective: Transethosomes (TEs) have introduced an emerging avenue of interest in vesicular research for transdermal delivery of drugs and can be a proper delivery system for painkillers like NSAIDS. This study aimed to formulate and characterize the potential of TE to enhance the transdermal transport of Dexketoprofen trometamol (DKT) to achieve controlled pain management compared to DKT solution. Methods: Factorial design (23) was adopted to appraise the influence of independent variables, namely, Lipoid S100 and surfactant concentrations and surfactant type (X3) on the % solubilization efficiency (% SE), vesicle size (VS), and % release efficiency (% RE). Thin film hydration was the preferred approach for preparing TEs where vesicle size, zeta potential, polydispersity index, %SE and %RE were investigated. The optimized formula was nominated and subjected to several studies. For the permeation study, optimum TE was incorporated into carbapol gel base for comparison with DKT solution. Also, an accelerated stability study was assessed for optimized formula. Results: All the prepared DKT-loaded TEs revealed acceptable VS, PDI, and ZP. The highest %SE (86.08±1.05 %) and lowest %RE (44.62±1.36 %) were observed in case of F1. The optimized formula (F1) displayed VS of 133.2±1.62 nm, PDI of 0.342±0.03 and ZP of-21.6±2.45 mV. F1 revealed enhanced skin permeation of a 2.6-fold increase compared with DKT solution. Moreover, F1 was stable upon storage and a non-significant change (P>0.05) was observed. Conclusion: DKT was successfully incorporated into vesicle carrier and can signify an alternative option for providing this therapy, bypassing the poor bioavailability and considerable adverse consequences of using the oral route besides improved patient compliance.

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Section: Influence Of Formulation Variables On Release Efficiencysupporting

confidence: 83%

Section: Influence Of Formulation Variables On Vesicle Sizementioning

confidence: 99%

Transethosomes as Breakthrough Tool for Controlled Transdermal Delivery of Dexketoprofen Trometamol: Design, Fabrication, Statistical Optimization, in Vitro, and Ex Vivo Characterization

Soliman

RASHWAN²,

Teaima³

et al. 2022

Int J App Pharm

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“…Developing liposomes for topical drug delivery system could face certain difficulties related to their low viscosities and improper application to the skin [ 13 ]. Integrating liposomes into emulgel formulation could possibly increase the viscosity of the formulation and facilitate its application over the affected area [ 14 ].…”

Section: Introductionmentioning

confidence: 99%

Quality by Design for Optimizing a Novel Liposomal Jojoba Oil-Based Emulgel to Ameliorate the Anti-Inflammatory Effect of Brucine

Abdallah

Elsewedy

Lila

et al. 2021

Gels

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One of the recent advancements in research is the application of natural products in developing newly effective formulations that have few drawbacks and that boost therapeutic effects. The goal of the current exploration is to investigate the effect of jojoba oil in augmenting the anti-inflammatory effect of Brucine natural alkaloid. This is first development of a formulation that applies Brucine and jojoba oil int a PEGylated liposomal emulgel proposed for topical application. Initially, various PEGylated Brucine liposomal formulations were fabricated using a thin-film hydration method. (22) Factorial design was assembled using two factors (egg Phosphatidylcholine and cholesterol concentrations) and three responses (particle size, encapsulation efficiency and in vitro release). The optimized formula was incorporated within jojoba oil emulgel. The PEGylated liposomal emulgel was inspected for its characteristics, in vitro, ex vivo and anti-inflammatory behaviors. Liposomal emulgel showed a pH of 6.63, a spreadability of 48.8 mm and a viscosity of 9310 cP. As much as 40.57% of Brucine was released after 6 h, and drug permeability exhibited a flux of 0.47 µg/cm2·h. Lastly, % of inflammation was lowered to 47.7, which was significant effect compared to other formulations. In conclusion, the anti-inflammatory influence of jojoba oil and Brucine was confirmed, supporting their integration into liposomal emulgel as a potential nanocarrier.

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“…Skin cancer activates the excessive growth of cells in the outermost layer, i.e., the epidermis, initiated by unrepaired DNA impairment in cells, resulting in mutations. Such modified epidermal cells propagate rapidly and generate malignant tumors [ 2 ]. In this way, abnormal dermis layers synchronize with the physiological alterations and prompt abnormal environments, leading to different types of cancer.…”

Section: Introductionmentioning

confidence: 99%

Formulation, Characterization, Anti-Inflammatory and Cytotoxicity Study of Sesamol-Laden Nanosponges

et al. 2022

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Sesamol (SES) possesses remarkable chemotherapeutic activity, owing to its anti-inflammatory and antioxidant potential. However, the activity of SES is mainly hampered by its poor physicochemical properties and stability issues. Hence, to improve the efficacy of this natural anti-inflammatory and cytotoxic agent, it was loaded into β-cyclodextrin nanosponges (NS) prepared using different molar ratios of polymer and crosslinker (diphenyl carbonate). The particle size of SES-laden NS (SES-NS) was shown to be in the nano range (200 to 500 nm), with a low polydispersity index, an adequate charge (−17 to −26 mV), and a high payload. Field emission scanning electron microscopy, thermogravimetric analysis, and Fourier transform infrared spectroscopy were used to characterize the bioactive-loaded selected batch (SES-NS6). This batch of nanoformulations showed improved solubilization efficacy (701.88 µg/mL) in comparison to bare SES (244.36 µg/mL), polymer (β-CD) (261.43 µg/mL), and other fabricated batches. The drug release data displayed the controlled release behavior of SES from NS. The findings of the egg albumin denaturation assay revealed the enhanced anti-inflammatory potential of SES-NS as compared to bare SES. Further, the cytotoxicity assay showed that SES-NS was more effective against B16F12 melanoma cell lines than the bioactive alone. The findings of this assay demonstrated a reduction in the IC50 values of SES-NS (67.38 μg/mL) in comparison to SES (106 μg/mL). The present investigation demonstrated the in vitro controlled release pattern and the enhanced anti-inflammatory and cytotoxic activity of SES-NS, suggesting its potential as a promising drug delivery carrier for topical delivery.

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Brucine-loaded transliposomes nanogel for topical delivery in skin cancer: statistical optimization, in vitro and dermatokinetic evaluation

Cited by 27 publications

References 40 publications

Transethosomes as Breakthrough Tool for Controlled Transdermal Delivery of Dexketoprofen Trometamol: Design, Fabrication, Statistical Optimization, in Vitro, and Ex Vivo Characterization

Transethosomes as Breakthrough Tool for Controlled Transdermal Delivery of Dexketoprofen Trometamol: Design, Fabrication, Statistical Optimization, in Vitro, and Ex Vivo Characterization

Quality by Design for Optimizing a Novel Liposomal Jojoba Oil-Based Emulgel to Ameliorate the Anti-Inflammatory Effect of Brucine

Formulation, Characterization, Anti-Inflammatory and Cytotoxicity Study of Sesamol-Laden Nanosponges

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