Liposomes increase skin penetration of entrapped and non-entrapped hydrophilic substances into human skin: a skin penetration and confocal laser scanning microscopy study

Verma, Daya D.; Verma, Sushma; Blume, G.; Fahr, Alfred

doi:10.1016/s0939-6411(03)00021-3

Cited by 240 publications

(135 citation statements)

References 22 publications

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“…6 However, it has become evident that it is difficult for conventional liposomes (CLs) to penetrate deep into the skin, with a large fraction retained in upper layers of stratum corneum 832 lin et al and accumulated in skin appendages. 7 It has been reported that deformable liposomes, consisting of phospholipids and so-called edge activators, could be driven deep into the skin by a hydration gradient when applied nonocclusively. 8 The edge activators used for the preparation of deformable liposomes are generally single-chain surfactants with a high radius of curvature, which destabilizes and increases deformability of the lipid bilayers of the vesicles.…”

Section: Introductionmentioning

confidence: 99%

Increased skin permeation efficiency of imperatorin via charged ultradeformable lipid vesicles for transdermal delivery

Lin¹,

Xie²,

Huang³

et al. 2018

IJN

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Aim The aim of this work was to develop a novel vesicular carrier, ultradeformable liposomes (UDLs), to expand the applications of the Chinese herbal medicine, imperatorin (IMP), and increase its transdermal delivery. Methods In this study, we prepared IMP-loaded UDLs using the thin-film hydration method and evaluated their encapsulation efficiency, vesicle deformability, skin permeation, and the amounts accumulated in different depths of the skin in vitro. The influence of different charged surfactants on the properties of the UDLs was also investigated. Results The results showed that the UDLs containing cationic surfactants had high entrapment efficiency (60.32%±2.82%), an acceptable particle size (82.4±0.65 nm), high elasticity, and prolonged drug release. The penetration rate of IMP in cationic-UDLs was 3.45-fold greater than that of IMP suspension, which was the highest value among the vesicular carriers. UDLs modified with cationic surfactant also showed higher fluorescence intensity in deeper regions of the epidermis. Conclusion The results of our study suggest that cationic surfactant-modified UDLs could increase the transdermal flux, prolong the release of the drug, and serve as an effective dermal delivery system for IMP.

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Section: Introductionmentioning

confidence: 99%

Increased skin permeation efficiency of imperatorin via charged ultradeformable lipid vesicles for transdermal delivery

Lin¹,

Xie²,

Huang³

et al. 2018

IJN

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“…For example, liposomes are a versatile drug nanocarrier, have been widely used in systemic therapy, and have shown potential for delivering drugs into multiple layers of the skin. 5,6 The mechanism of enhanced skin delivery includes but is not limited to: the cell membrane-like structure of the liposome having good biocompatibility; the small size of liposomes; formation of drug reservoirs in the skin; and specific liposome-skin interactions. 6,7 Cevc et al have introduced a further step to create flexible liposomes and transfersomes containing lecithin and cholesterol.…”

Section: Introductionmentioning

confidence: 99%

“…5,6 The mechanism of enhanced skin delivery includes but is not limited to: the cell membrane-like structure of the liposome having good biocompatibility; the small size of liposomes; formation of drug reservoirs in the skin; and specific liposome-skin interactions. 6,7 Cevc et al have introduced a further step to create flexible liposomes and transfersomes containing lecithin and cholesterol. 8,9 Surface-active agents can be inserted into the lipid bilayers of flexible liposomes and create a "softened" bilayer membrane, thus making liposomes more flexible and permeable than ordinary liposomes.…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy

Li¹,

Zhang²,

Huang³

et al. 2013

IJN

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Abstract:The purpose of this study was to investigate flexible nanoliposomes for mediating topical delivery of daptomycin, and to document permeation rates and bacteriostatic activity towards skin infections. Response surface methodology was used to optimize the daptomycinloaded flexible nanoliposomes (DAP-FL), and the amount of drug loaded into the particles was evaluated as the investigation index. The optimal lipid ratio was lecithin to sodium cholate 17:1 (w/w) and the lipid to drug ratio was 14:1 (w/w). The hydration temperature was set at 37°C and the duration of treatment with ultrasound was 20 minutes. The DAP-FL obtained had a small mean particle size (55.4 nm) with a narrow size distribution (polydispersity index 0.15). The mean entrapment efficiency was 87.85% ± 2.15% and the mean percent drug loading was 5.61% ± 0.14%. Using skin mounted between the donor and receptor compartments of a modified Franz diffusion cell, the percentage and quantity of cumulative daptomycin permeation from DAP-FL within 12 hours were measured at 96.28% ± 0.70% and (132.23 ± 17.73) μg/cm 2 *5 = 661.15 ± 88.65 μg/cm 2 , directly, showing rapid and efficient antibacterial activity against Staphylococcus aureus. Following local administration of DAP-FL, daptomycin was detected in multilayer tissues within the skin and underlying structures in the dorsal skin of the mouse. Effective therapeutic concentrations were maintained for several hours, and significantly inhibited bacterial growth and injury-induced biofilms. These results demonstrate that the DAP-FL can enhance the ability of daptomycin to permeate the skin efficiently, where it has a powerful antibacterial action and activity against biofilms. This novel formulation of daptomycin has potential as a new approach in the clinical application of daptomycin.

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“…Based on previous studies, 29,30 it is possible to consider the size of present rhEGF loaded-SLNs formulation is suitable to deliver rhEGF into rat skin layer. In particular, the system showed uniform particle size distribution and good physical colloidal stability as nanoparticle.…”

Section: Discussionmentioning

confidence: 99%

Recombinant Human Epidermal Growth Factor (rhEGF)-loaded Solid Lipid Nanoparticles: Fabrication and Their Skin Accumulation Properties for Topical rhEGF Delivery

Hwang¹,

Han²,

Jeon³

et al. 2014

Bulletin of the Korean Chemical Society

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For the present study, rhEGF was encapsulated into solid lipid nanoparticles (SLNs). The SLNs were prepared by the W 1 /O/W 2 double emulsification method combined with the high pressure homogenization method and the physical properties such as particle size, zeta-potential and encapsulation efficiency were measured. The overall particle morphology of SLNs was investigated using a transmission electron microscopy (TEM). The percutaneous skin permeation and accumulation property of rhEGF was evaluated using Franz diffusion cell system along with confocal laser scanning microscopy (CLSM). The mean particle size of rhEGF-loaded SLNs was 104.00 ± 3.99 nm and the zeta-potential value was in the range of −36.99 ± 0.54 mV, providing a good colloidal stability. The TEM image revealed a spherical shape of SLNs about 100 nm and the encapsulation efficiency was 18.47 ± 0.22%. The skin accumulation of rhEGF was enhanced by SLNs. CLSM image analysis provided that the rhEGF rat skin accumulation is facilitated by an entry of SLNs through the pores of skin.

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Liposomes increase skin penetration of entrapped and non-entrapped hydrophilic substances into human skin: a skin penetration and confocal laser scanning microscopy study

Cited by 240 publications

References 22 publications

Increased skin permeation efficiency of imperatorin via charged ultradeformable lipid vesicles for transdermal delivery

Increased skin permeation efficiency of imperatorin via charged ultradeformable lipid vesicles for transdermal delivery

Preparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy

Recombinant Human Epidermal Growth Factor (rhEGF)-loaded Solid Lipid Nanoparticles: Fabrication and Their Skin Accumulation Properties for Topical rhEGF Delivery

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