In vitro skin permeation of monoolein nanoparticles containing hydroxypropyl β-cyclodextrin/minoxidil complex

Kwon, Teak Kwan; Kim, Jin Chul

doi:10.1016/j.ijpharm.2010.03.049

Cited by 40 publications

(12 citation statements)

References 23 publications

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“…24 In the case of cubic phase gel, glyceryl monooleate could intercalate with the extracellular lipid matrix of the skin, and disrupt its well organized compact structure. 30 Some studies have reported that enhanced transdermal delivery of drugs may depend on a disordered state, or depend on a different order of lipids, given that intercellular lipids can rearrange into a cubic phase under specific circumstances. 31 In both the in vitro permeability and in vivo bioavailability experiments, a correlation was obtained between the outcomes of the in vitro permeability model and the in vivo bioavailability data.…”

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confidence: 99%

Transdermal delivery of paeonol using cubic gel and microemulsion gel

Luo¹,

Shen²,

Chen³

2011

IJN

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Background The aim of this study was to develop new systems for transdermal delivery of paeonol, in particular microemulsion gel and cubic gel formulations. Methods Various microemulsion vehicles were prepared using isopropyl myristate as an oil phase, polyoxyethylated castor oil (Cremophor ® EL) as a surfactant, and polyethylene glycol 400 as a cosurfactant. In the optimum microemulsion gel formulation, carbomer 940 was selected as the gel matrix, and consisted of 1% paeonol, 4% isopropyl myristate, 28% Cremophor EL/polyethylene glycol 400 (1:1), and 67% water. The cubic gel was prepared containing 3% paeonol, 30% water, and 67% glyceryl monooleate. Results A skin permeability test using excised rat skins indicated that both the cubic gel and microemulsion gel formulations had higher permeability than did the paeonol solution. An in vivo pharmacokinetic study done in rats showed that the relative bioavailability of the cubic gel and microemulsion gel was enhanced by about 1.51-fold and 1.28-fold, respectively, compared with orally administered paeonol suspension. Conclusion Both the cubic gel and microemulsion gel formulations are promising delivery systems to enhance the skin permeability of paeonol, in particular the cubic gel.

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confidence: 99%

Transdermal delivery of paeonol using cubic gel and microemulsion gel

Luo¹,

Shen²,

Chen³

2011

IJN

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“…SPC in the nanoparticulate surface also played an important role for enhancing follicular targeting. Previous studies (30,31) have suggested that liposomes, which are organized by phospholipids, can deposit minoxidil in follicles. That is why minoxidil showed greater follicular uptake enhancement by squarticles than DPCP.…”

Section: Discussionmentioning

confidence: 94%

“…PG not only solubilized minoxidil, but it also increased the flux across the skin. According to previous studies (29,30), the PG-rich medium could act as penetration enhancers to increase minoxidil receptor penetration. It is reported that minoxidil absorption into systemic circulation leads to unwanted cardiovascular effects (8,31).…”

Section: Discussionmentioning

confidence: 95%

Squarticles as a Lipid Nanocarrier for Delivering Diphencyprone and Minoxidil to Hair Follicles and Human Dermal Papilla Cells

Aljuffali

Sung

Shen

et al. 2013

AAPS J

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Abstract. Delivery of diphencyprone (DPCP) and minoxidil to hair follicles and related cells is important in the treatment of alopecia. Here we report the development of "squarticles," nanoparticles formed from sebum-derived lipids such as squalene and fatty esters, for use in achieving targeted drug delivery to the follicles. Two different nanosystems, nanostructured lipid carriers (NLC) and nanoemulsions (NE), were prepared. The physicochemical properties of squarticles, including size, zeta potential, drug encapsulation efficiency, and drug release, were examined. Squarticles were compared to a free control solution with respect to skin absorption, follicular accumulation, and dermal papilla cell targeting. The particle size of the NLC type was 177 nm; that of the NE type was 194 nm. Approximately 80% of DPCP and 60% of minoxidil were entrapped into squarticles. An improved drug deposition in the skin was observed in the in vitro absorption test. Compared to the free control, the squarticles reduced minoxidil penetration through the skin. This may indicate a minimized absorption into systemic circulation. Follicular uptake by squarticles was 2-and 7-fold higher for DPCP and minoxidil respectively compared to the free control. Fluorescence and confocal images of the skin confirmed a great accumulation of squarticles in the follicles and the deeper skin strata. Vascular endothelial growth factor expression in dermal papilla cells was significantly upregulated after the loading of minoxidil into the squarticles. In vitro papilla cell viability and in vivo skin irritancy tests in nude mice suggested a good tolerability of squarticles to skin. Squarticles provide a promising nanocarrier for topical delivery of DPCP and minoxidil.

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“…Obviously, MTO transdermal delivery depends on the form of the dosage. The key excipient GMO intercalated with the extracellular lipid matrix of the skin and disrupted the highly compacted structures (Kwon & Kim, 2010;Luo et al, 2011). These comprehensive actions resulted in the MTO cubic phase exhibiting great transdermal efficiency.…”

Section: In Vitro Permeation Of the Mto Cubic Phasesmentioning

confidence: 99%

Melanoma therapy with transdermal mitoxantrone cubic phases

Du²,

Zhu

et al. 2015

Drug Delivery

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Objective: An effective transdermal formulation for the convenient melanoma therapy was found and evaluated. Materials and methods: A mitoxantrone (MTO) cubic phase was prepared with glyceryl monooleate, ethanol and water. The permeation, cytotoxicity, in vivo anti-melanoma effect of the MTO cubic phases were evaluated. The anti-cancer mechanism of the MTO cubic phases was explored according to the immunohistochemistry and flow cytometry.Results and discussion: The isotropic structure of MTO cubic phases was identified. The transdermal permeability of MTO was greatly improved by the cubic phase compared to that of the MTO solution. The MTO cubic phases showed the high cytotoxicity in B 16 melanoma cells evidenced by a modified electrical cell-substrate impedance sensing system. High antimelanoma effect of the MTO cubic phases was confirmed according to the tumor volume changes and tumor weight. The tumor inhibitory rate of the MTO cubic phases was 68.44%. The calreticulin expression of B 16 cells was improved by the MTO cubic phases, and the improved cell uptake of MTO was confirmed by the flow cytometry. Conclusion:The MTO cubic phase is a promising topical delivery system for melanoma therapy with the advantages of non-invasion and no severe side effects.

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In vitro skin permeation of monoolein nanoparticles containing hydroxypropyl β-cyclodextrin/minoxidil complex

Cited by 40 publications

References 23 publications

Transdermal delivery of paeonol using cubic gel and microemulsion gel

Transdermal delivery of paeonol using cubic gel and microemulsion gel

Squarticles as a Lipid Nanocarrier for Delivering Diphencyprone and Minoxidil to Hair Follicles and Human Dermal Papilla Cells

Melanoma therapy with transdermal mitoxantrone cubic phases

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