Ultradeformable liposomes as multidrug carrier of resveratrol and 5-fluorouracil for their topical delivery

Cosco, Donato; Paolino, Donatella; Maiuolo, Jessica; Marzio, Luisa Di; Carafa, Maria; Ventura, Cinzia Anna; Fresta, Massimo

doi:10.1016/j.ijpharm.2015.04.056

Cited by 136 publications

(93 citation statements)

References 39 publications

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“…The values of flux and ER were found to be higher with ELA-3 and EL-S80 as compared to the DS respectively due to facilitated permeation across the SC. A similar finding was reported in the human SC with 6.2-fold higher flux when co-administered with resveratrol (Cosco et al, 2015). Limited permeation of 5-FU solution might be owing to hydrophilicity, polarity and low intercalating ability of 5-FU in lipid bilayer of EL across the SC (Tsukada et al, 1984;Singh et al, 2005).…”

Section: In Vitro Skin Permeation and Drug Deposition Studiessupporting

confidence: 82%

Optimized permeation enhancer for topical delivery of 5-fluorouracil-loaded elastic liposome using Design Expert: part II

et al. 2015

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Objective: To prepare and optimize the topical elastic liposome (EL)-loaded carbopol-980 gel of 5-Fluorouracil (5-FU) containing permeation enhancers (azone, propylene glycol (PG) and lauryl alcohol (LA)) and further evaluation for permeation flux of 5-FU, the activation energy and irritation in the rat skin. Methods: EL formulations were prepared using phosphatidylcholine and varied surfactants (Span 60, Span 80 and Tween-80) by rotator evaporation method and optimized by experimental design. In vitro characterizations dictated the EL containing Span 80 (lipid:surfactant ¼ 7:3) (EL3-S80) for further optimization of gel. Different gel formulations (5% w/w) with varying concentration (1-3%) of permeation enhancers were prepared and evaluated for viscosity, spreadability, the 5-FU permeation and deposition. The activation energy using the Franz diffusion cell and the plausible irritation using the Draize test were assessed on the albino rat and rabbit, respectively. Results and discussion: EL3-S80 was selected as an optimized EL owing to maximum desirability (0.99) and enhanced 5-FU flux (187.86 ± 14.1 mg/cm 2 /h). EL3-S80 suspension loaded gels (0.5%) revealed reduced viscosity leading to higher spreadability than blank gel. EL containing 3% azone in gel, EL containing 3% LA in gel and EL containing 3% PG in gel portrayed 187.86 ± 14.1, 117.7 ± 13.4 and 106.7 ± 7.3 mg/cm 2 /h as enhanced 5-FU flux values, respectively as compared to drug solution (8.8 ± 0.76 mg/cm 2 /h). Furthermore, reduced value of activation energy (2.63-folds) and the non-irritancy of gel could be effective and safe. Conclusion: ELA-3 gel formulation could be used as an effective and economic gel in cutaneous cancer and skin-related keratoses.

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Section: In Vitro Skin Permeation and Drug Deposition Studiessupporting

confidence: 82%

Optimized permeation enhancer for topical delivery of 5-fluorouracil-loaded elastic liposome using Design Expert: part II

et al. 2015

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“…32 As shown in Figure 1, the TSI results for the various surfactant-free zein nanoparticles at 20°C are very similar, thus evidencing the absence of destabilizing phenomena, eg, sedimentation, migration, and/or flocculation. 27 When the temperature was increased to 37°C, a significant variation in the TSI showed on the sample prepared with 5 mg of zein, probably as a consequence of the specific rearrangement of the protein; on the contrary, the formulation prepared with 10 mg of protein showed suitable stability.…”

Section: Physico-chemical Characterizationmentioning

confidence: 60%

Sodium deoxycholate-decorated zein nanoparticles for a stable colloidal drug delivery system

Gagliardi¹,

Paolino²,

Iannone³

et al. 2018

IJN

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Background The use of biopolymers is increasing in drug delivery, thanks to the peculiar properties of these compounds such as their biodegradability, availability, and the possibility of modulating their physico-chemical characteristics. In particular, protein-based systems such as albumin are able to interact with many active compounds, modulating their biopharmaceutical properties. Zein is a protein of 20–40 kDa made up of many hydrophobic amino acids, generally regarded as safe (GRAS) and used as a coating material. Methods In this investigation, zein was combined with various surfactants in order to obtain stable nanosystems by means of the nanoprecipitation technique. Specific parameters, eg, temperature, pH value, Turbiscan Stability Index, serum stability, in vitro cytotoxicity and entrapment efficiency of various model compounds were investigated, in order to identify the nanoformulation most useful for a systemic drug delivery application. Results The use of non-ionic and ionic surfactants such as Tween 80, poloxamer 188, and sodium deoxycholate allowed us to obtain nanoparticles characterized by a mean diameter of 100–200 nm when a protein concentration of 2 mg/mL was used. The surface charge was modulated by means of the protein concentration and the nature of the stabilizer. The most suitable nanoparticle formulation to be proposed as a colloidal drug delivery system was obtained using sodium deoxycholate (1.25% w/v) because it was characterized by a narrow size distribution, a good storage stability after freeze-drying and significant feature of retaining lipophilic and hydrophilic compounds. Conclusion The sodium deoxycholate-coated zein nanoparticles are stable biocompatible colloidal carriers to be used as useful drug delivery systems.

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“…Innovative DDSs of resveratrol, such as polymeric nanoparticles, cyclodextrins, colloidal mesoporous silica nanoparticles and liposomes, have been fabricated to enhance aqueous solubility and bioavailability, improve physicochemical stability and achieve targeted or controlled drug release. [5][6][7] Recently, different classical and successful nanotherapeutics used to transport anticancer drugs into tumors have been fabricated and applied in order to improve the anticancer effect of chemotherapeutic drugs, the most prominent among which include polymeric nanocarriers such as liposomes, supramolecular derivatives and ultradeformable vesicles. [8][9][10] As one of the promising nanoparticular approaches, the mixed micelle carriers formed by triblock copolymers for delivery of anticancer drugs have been basically exploited in various clinical applications for the merits of smaller size, self-assembling ability, solubilization and protection against unstable drugs.…”

Section: Introductionmentioning

confidence: 99%

Folic acid-functionalized drug delivery platform of resveratrol based on Pluronic 127/D-α-tocopheryl polyethylene glycol 1000 succinate mixed micelles

Hao¹,

Tong²,

Jin³

et al. 2017

IJN

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A folic acid (FA)-functionalized drug vehicle platform based on Pluronic 127 (P127)/D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) mixed micelles was orchestrated for an effective delivery of the model drug resveratrol in order to address the problem of poor water solubility and rapid metabolism of resveratrol and improve its targeted accumulation at tumor site. The FA-decorated mixed micelles were prepared using thin-film hydration method and optimized by central composite design approach. The micelles were also characterized in terms of size and morphology, drug entrapment efficiency and in vitro release profile. In addition, the cytotoxicity and cell uptake of the micelles were evaluated in folate receptor-overexpressing MCF-7 cell line. In vivo pharmacokinetic and biodistribution studies were also performed. The average size of the micelles was ~20 nm with a spherical shape and high encapsulation efficiency (99.67%). The results of fluorescence microscopy confirmed the targeting capability of FA-conjugated micelles in MCF-7 cells. FA-modified micelles exhibited superior pharmacokinetics in comparison with that of solution. Further, the low accumulation of resveratrol-loaded FA micelles formulation in the heart and kidney avoided toxicity of these vital organs. It could be concluded that folate-modified P127/TPGS mixed micelles might serve as a potential delivery platform for resveratrol.

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Ultradeformable liposomes as multidrug carrier of resveratrol and 5-fluorouracil for their topical delivery

Cited by 136 publications

References 39 publications

Optimized permeation enhancer for topical delivery of 5-fluorouracil-loaded elastic liposome using Design Expert: part II

Optimized permeation enhancer for topical delivery of 5-fluorouracil-loaded elastic liposome using Design Expert: part II

Sodium deoxycholate-decorated zein nanoparticles for a stable colloidal drug delivery system

Folic acid-functionalized drug delivery platform of resveratrol based on Pluronic 127/D-α-tocopheryl polyethylene glycol 1000 succinate mixed micelles

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Ultradeformable liposomes as multidrug carrier of resveratrol and 5-fluorouracil for their topical delivery

Cited by 136 publications

References 39 publications

Optimized permeation enhancer for topical delivery of 5-fluorouracil-loaded elastic liposome using Design Expert: part II

Optimized permeation enhancer for topical delivery of 5-fluorouracil-loaded elastic liposome using Design Expert: part II

Sodium deoxycholate-decorated zein nanoparticles for a stable colloidal drug delivery system

Folic acid-functionalized drug delivery platform of resveratrol based on Pluronic 127/D-&alpha;-tocopheryl polyethylene glycol 1000 succinate mixed micelles

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Folic acid-functionalized drug delivery platform of resveratrol based on Pluronic 127/D-α-tocopheryl polyethylene glycol 1000 succinate mixed micelles