Cubosome Dispersions as Delivery Systems for Percutaneous Administration of Indomethacin

Esposito, Elisabetta; Cortesi, Rita; Drechsler, Markus; Paccamiccio, Lydia; Mariani, Paolo; Contado, Catia; Stellin, Elisa; Menegatti, Enea; Bonina, Francesco; Puglia, Carmelo

doi:10.1007/s11095-005-8176-x

Cited by 242 publications

(81 citation statements)

References 35 publications

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“…In this context, Table 2 displays representative examples from literature on studies conducted on the possibility of utilizing cubosomes and hexosomes as drug nanocarriers [52,53,[108][109][110]. These nanostructured fluids show potential as drug nanocarriers since they are composed of naturally occurring biodegradable lipids and tailored for solubilizing higher amounts of amphiphilic, hydrophobic, and hydrophilic drugs in their highly ordered self-assembled interiors as opposed to liposomes.…”

Section: Cubosomes and Hexosomes As Drug Nanocarriersmentioning

confidence: 99%

Characterization and potential applications of nanostructured aqueous dispersions

Yaghmur

Glatter

2009

Advances in Colloid and Interface Science

349

270

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Section: Cubosomes and Hexosomes As Drug Nanocarriersmentioning

confidence: 99%

Characterization and potential applications of nanostructured aqueous dispersions

Yaghmur

Glatter

2009

Advances in Colloid and Interface Science

349

270

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“…The feasibility of cubosomes as carriers for parenteral, topical, and buccal delivery of drugs has been reported in the literature (14)(15)(16)(17)(18)(19). Formulations based on this technology have been reported to have improved tolerance and drug bioavailability (20).…”

Section: Introductionmentioning

confidence: 99%

Nanostructured Cubosomes in a Thermoresponsive Depot System: An Alternative Approach for the Controlled Delivery of Docetaxel

et al. 2015

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Abstract. The aim of the present study was to develop and evaluate a thermoresponsive depot system comprising of docetaxel-loaded cubosomes. The cubosomes were dispersed within a thermoreversible gelling system for controlled drug delivery. The cubosome dispersion was prepared by dilution method, followed by homogenization using glyceryl monooleate, ethanol and Pluronic ® F127 in distilled water. The cubosome dispersion was then incorporated into a gelling system prepared with Pluronic ® F127 and Pluronic ® F68 in various ratios to formulate a thermoresponsive depot system. The thermoresponsive depot formulations undergo a thermoreversible gelation process i.e., they exists as free flowing liquids at room temperature, and transforms into gels at higher temperatures e.g., body temperature, to form a stable depot in aqueous environment. The mean particle size of the cubosomes in the dispersion prepared with Pluronic ® F127, with and without the drug was found to be 170 and 280 nm, respectively. The prepared thermoresponsive depot system was evaluated by assessing various parameters like time for gelation, injectability, gel erosion, and in-vitro drug release. The drug-release studies of the cubosome dispersion before incorporation into the gelling system revealed that a majority (∼97%) of the drug was released within 12 h. This formulation also showed a short lag time (∼3 min). However, when incorporated into a thermoresponsive depot system, the formulation exhibited an initial burst release of ∼21%, and released only ∼39% drug over a period of 12 h, thus indicating its potential as a controlled drug delivery system.

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“…In cubosome system, it was speculated that cubic structure with similar nano-structure as the skin, increase the interaction between skin and formulation and enhances the skin permeation. 5,20) Lopes et al reported that hexagonal phase may facilitate the fusion of the LCNs with stratum corneum and deeper skin layers and thereby may improve drug delivery to the skin. 14) Moreover, they speculated that the larger surface area of the hexosome system might have resulted in enhanced contact with the porcine ear skin that improved vitamin K permeation.…”

Section: F-nmr (Right Side) Spectra Of Glyceryl Monooleyl Ether (Gme)mentioning

confidence: 99%

“…4) Among these LLC systems, some of liquid crystal structures form a liquid crystalline nanoparticles (LCNs) by dispersing in an aqueous environment and the LCNs of reverse hexagonal phase and bicontinuous cubic phase are called "hexosomes (H II )" and "cubosomes," respectively. 3,5) Glycerol monoolate (GMO) has been widely studied as an additive to form LLCs and their LCNs.6,7) Effect of the additives such as block copolymer formation and electrostatic interaction were also investigated.8-11) Cohen-Avrahami et al reported transdermal delivery of sodium diclofenac with hexosomes of GMO in combination with cell-penetrating peptides. 3,12) Lopes et al showed improved skin permeation for vitamin K and cyclosporine A with hexosomes of GMO.…”

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confidence: 99%

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confidence: 99%

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Glyceryl Monooleyl Ether-Based Liquid Crystalline Nanoparticles as a Transdermal Delivery System of Flurbiprofen: Characterization and <i>in Vitro</i> Transport

et al. 2015

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Liquid crystalline nanoparticles (LCNs) were prepared using glyceryl monooleyl ether (GME) by the modified film rehydration method. Hydrogenated lecithin (HL), 1,3-butylene glycol (1,3-BG), and Poloxamer 407 were used as additives. The prepared LCN formulations were evaluated based on particle size, smallangle X-ray diffraction (SAXS) analysis, 1 H-and 19F-NMR spectra, and in vitro skin permeation across Yucatan micropig skin. The composition (weight percent) of the LCN formulations were GME-HL-1,3-BG (4 : 1 : 15), 4% GME-based LCN and GME-HL-1,3-BG (8 : 1 : 15), 8% GME-based LCN and their mean particle sizes were 130-175 nm. Flurbiprofen 5 and 10 mg was loaded into 4% GME-based LCN and 8% GMEbased LCN systems, respectively. The results of SAXS and NMR suggested that both flurbiprofen-loaded formulations consist of particles with reverse type hexagonal phase (formation of hexosome) and flurbiprofen molecules were localized in the lipid domain through interaction of flurbiprofen with the lipid components. Flurbiprofen transport from the LCN systems across the Yucatan micropig skin was increased compared to flurbiprofen in citric buffer (pH 3.0). The 8% GME-based LCN systems was superior to the 4% GME-based LCN for flurbiprofen transport. Since the internal hexagonal phase in the 8% GME-based LCN systems had a higher degree of order compared to the 4% GME-based LCN in SAXS patterns, the 8% GME-based LCN system had a larger surface area, which might influence flurbiprofen permeation. These results indicated that the GME-based LCN system is effective in improving the skin permeation of flurbiprofen across the skin.Key words lyotropic liquid crystal; liquid crystalline nanoparticle; hexosome; skin permeation; flurbiprofen; NMR Under some circumstances, transdermal delivery may be superior to other routes of delivery due to advantages such as avoidance of first pass elimination and a lack of invasiveness. However, relatively few transdermal drugs have been commercialized owing to the efficient barrier function of the stratum corneum, which is located on the outer layer of the skin. To overcome the barrier function of the stratum corneum, several physical and chemical methods have been developed. 1)Recently, lyotropic liquid crystal (LLC) systems have been developed as a chemical method to overcome the stratum corneum barrier.2,3) LLCs are usually composed of amphiphilic molecules and solvents that can form a variety of structures, including lamellar (L α ), hexagonal (normal, or reverse) and inverted cubic (bicontinuous and micellar) structures. 4) Among these LLC systems, some of liquid crystal structures form a liquid crystalline nanoparticles (LCNs) by dispersing in an aqueous environment and the LCNs of reverse hexagonal phase and bicontinuous cubic phase are called "hexosomes (H II )" and "cubosomes," respectively. 3,5) Glycerol monoolate (GMO) has been widely studied as an additive to form LLCs and their LCNs.6,7) Effect of the additives such as block copolymer formation and electrostatic interaction were also i...

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Cubosome Dispersions as Delivery Systems for Percutaneous Administration of Indomethacin

Abstract: MO dispersions can be proposed as nanoparticulate systems able to control the percutaneous absorption of indomethacin.

Cited by 242 publications

References 35 publications

Characterization and potential applications of nanostructured aqueous dispersions

Characterization and potential applications of nanostructured aqueous dispersions

Nanostructured Cubosomes in a Thermoresponsive Depot System: An Alternative Approach for the Controlled Delivery of Docetaxel

Glyceryl Monooleyl Ether-Based Liquid Crystalline Nanoparticles as a Transdermal Delivery System of Flurbiprofen: Characterization and <i>in Vitro</i> Transport

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