Improved anti-melanoma effect of a transdermal mitoxantrone ethosome gel

Yu, Xiang; Du, Lina; Yu, Li; Fu, Guiying; Jin, Yiguang

doi:10.1016/j.biopha.2015.05.002

Cited by 68 publications

(31 citation statements)

References 30 publications

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“…Ethanol has a fluidizing effect on phospholipid bilayers, producing compact, soft, deformable vesicles, along with the interaction between ethanol and the polar head group region of the lipid molecule resulting in a decrease in transition temperature of stratum corneum lipids with a consequent increase in membrane fluidity and BDH ethosomes partitioning. 21 , 43 – 47 …”

Section: Resultsmentioning

confidence: 99%

A novel transdermal nanoethosomal gel of betahistine dihydrochloride for weight gain control: in-vitro and in-vivo characterization

El-Menshawe¹,

Ali²,

Halawa³

et al. 2017

DDDT

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BackgroundBetahistine dihydrochloride (BDH) is a histamine analog used to control weight gain, with short elimination half-life and gastric irritation as side effects.ObjectiveThe aim of the current investigation is to formulate and optimize a topical BDH ethosomal gel for weight gain control.Materials and methodsBox–Behnken design was applied to study the effect of independent variables: phosphatidylcholine (PC), propylene glycol (PG), and ethanol on vesicle size; entrapment efficiency; % drug release; and flux. The morphology and zeta potential of the optimized formulation were evaluated. The % drug release, flux, and pharmacodynamics of the optimized formulation gel were studied.ResultsThe size and entrapment efficiency percent had a direct positive relationship with the concentration of PC and negative relationship with ethanol and PG. The % drug release and flux decreased with increasing PC and PG, while ethanol enhanced both responses. Regression modeling indicated a good correlation between dependent and independent variables, where F16 was chosen as the optimized formulation. F16 showed well-defined spherical vesicles and zeta potential of −24 mV, and % release from the gel exceeded 99.5% over 16 h with the flux of 0.28 mg/cm2/h. Food intake and weight gain of rats were significantly decreased after transdermal application of the BDH ethosomal gel when compared with control, placebo, and BDH gel. The histopathological findings proved the absence of inflammation and decrease in adipose tissue.ConclusionResults obtained showed a significant, sustained transdermal absorption of BDH ethosomal gel and, consequently, a decrease in food intake and weight gain.

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Section: Resultsmentioning

confidence: 99%

A novel transdermal nanoethosomal gel of betahistine dihydrochloride for weight gain control: in-vitro and in-vivo characterization

El-Menshawe¹,

Ali²,

Halawa³

et al. 2017

DDDT

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“…[29][30][31] In terms of possible mechanisms for ethosomes to promote percutaneous permeation of drugs, two viewpoints have been presented: the first one is that ethanol is a known penetration enhancer, which can disturb the multilamellar and ordered lipid domain, lower the structure density, and enhance the fluidity of the stratum corneum, thus providing the vesicles with flexible characteristics that allow them to penetrate easily into deeper layers of the skin; 32,33 the second one is that phospholipids between the stratum corneum and ethosomal vesicle fuse easily, thus changing the transition temperature, leading to enhanced drug penetration. 34 In our research, we interestingly found that even though the lipid content in the liposomes and the ethanol content in the hydroethanolic solution were equal with those in the ethosomes, after percutaneous penetration, a greater fluorescence intensity in the skin of the ethosomal system was observed, compared with that in the hydroethanolic solution and liposomes (P,0.05; Figure 2B). These results further confirmed that alcohol or phospholipid content was not the only driving force for promoting effective drug penetration into the skin; therefore, we speculate that there is a synergistic mechanism among lipids, ethanol, and the skin, by which skin penetration of drugs can be obviously promoted.…”

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confidence: 56%

Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes

Yang

et al. 2017

IJN

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Ethosomes can promote the penetration of lipophilic drugs into the skin, but the underlying mechanism is still unknown. The purpose of this study was to investigate the mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes. The formulation of ethosomes was optimized using the Box–Behnken experimental design, in which Rhodamine B and 1-palmitoyl-2-{12-[(7-nitro-2-1,3-benzoxadiazol-4-yl)amino]dodecanoyl}- sn -glycero-3-phosphocholine were used to simulate a model lipophilic drug and act as a fluorescent tracer of ethosomal phospholipids, respectively. Liposomes with the same phospholipid concentration and a hydroethanolic solution with the same ethanol concentration were also prepared as controls. The percutaneous progression of the above fluorescent preparations was observed by confocal laser scanning microscopy, and the fluorescence intensity of the images was analyzed. The optimized ethosome formulation consisted of 2.45% yolk phospholipids, 30% ethanol, and 67.55% distilled water. The percutaneous permeation of Rhodamine B in the optimized ethosomes was superior to that in hydroethanolic solution ( P <0.05) and liposomes ( P <0.05). The ethosomes could penetrate the skin via the percutaneous pathway of the hair follicle and stratum corneum, while during the process of penetration, the vesicles were broken and the phospholipids were retained in the upper epidermis, with the test compounds penetrating gradually. The superior percutaneous penetration of ethosomes was linked to the synergistic effects of their ingredients. The percutaneous pathways of ethosomes included open hair follicles and stratum corneum pathways. In addition, the vesicles might break up during percutaneous penetration in the superficial layer of the skin, allowing the test compounds to keep permeating into the deeper layer alone, while the phospholipid was retained in the upper epidermis.

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“…In another study, the surface modification of liposomes encapsulating doxorubicin with anti-HER2/neu peptide (AHNP) improved the in vivo therapeutic index and anticancer activity of the drug against breast cancer when compared with non-targeted liposomes such as Caelyx ® (Figure 11) 236 . The encapsulation of mitoxantrone into ethosomes improved its anticancer activity against melanoma tumors by a reduction in the tumor size and an induction of an in vivo anticancer immune response 246 . In another study, 5fluorouracil intended for dermal application was encapsulated into liposomes, transfersomes and niosomes.…”

Section: Biomedical Applications Of Nanovesicles Nanovesicles For Delmentioning

confidence: 99%

Lipid-based nanovesicles for nanomedicine

et al. 2016

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Molecular self-assembly has enabled the fabrication of biologically inspired, advanced nanostructures as lipid-based nanovesicles (L-NVs). The oldest L-NVs, liposomes, have been widely proposed as potential candidates for drug delivery, diagnostic and/or theranostic applications and some liposome-based drug products have already stepped from the lab-bench to the market. This success is attributed to their ability to encapsulate both hydrophobic and/or hydrophilic molecules, efficiently carry and protect them within the body and finally deliver them at the target site. These positive features are also coupled with high biocompatibility. However, liposomes still present some unsolved drawbacks, such as poor colloidal stability, short shelf-life, restricted and expensive conditions of preparation because of the inherent nature of their fundamental constituents (phospholipids). The new tools available in the self-assembly of controlled molecules have significantly advanced the field of L-NV design and synthesis, and non-liposomal L-NVs have been recently developed; this new generation of nanovesicles can represent a paradigm shift in nanomedicine: they may complement liposomes, showing their advantages and overcoming most of their drawbacks. Clearly, being still young, their rocky way to the clinic first and then to the market has just started and it is still long, but they have all the potentialities to reach their objective target. The purpose of this review is to first present the large plethora of L-NVs available, focusing on this new generation of non-liposomal L-NVs and showing their similarities and differences with respect to their ancestors (liposomes). Since the overspread of a nanomaterial to the market is also strongly dependent on the availability of technological-scale preparation methods, we will also extensively review the current approaches exploited for L-NV production. The most cutting-edge approaches based on compressed fluid (CF) technologies will be highlighted here since they show the potential to represent a game-change in the production of L-NVs, favouring their step from the bench to the market. Finally, we will briefly discuss L-NV applications in nanomedicine, looking also for their future perspectives.

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Improved anti-melanoma effect of a transdermal mitoxantrone ethosome gel

Cited by 68 publications

References 30 publications

A novel transdermal nanoethosomal gel of betahistine dihydrochloride for weight gain control: in-vitro and in-vivo characterization

A novel transdermal nanoethosomal gel of betahistine dihydrochloride for weight gain control: in-vitro and in-vivo characterization

Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes

Lipid-based nanovesicles for nanomedicine

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