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Compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement.

Shen S, Liu SZ, Zhang YS, Du MB, Liang AH, Song LH, Ye ZG - Int J Nanomedicine (2015)

Bottom Line: With the help of ethosomal technology, the accumulated permeation quantity of artesunate significantly increased at 8 hours after administration, which was 1.57 times as much as that of conventional cataplasm.The microstructure, ultrastructure, and birefringent structure in skin were observed.Data obtained in this study showed that the application of ethosomal technology to antimalarial cataplasm could improve the transdermal delivery of drug, enhance the efficacy, and facilitate practical application in clinic.

View Article: PubMed Central - PubMed

Affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, People's Republic of China.

ABSTRACT
Malaria is still a serious public health problem in some parts of the world. The problems of recurrence and drug resistance are increasingly more serious. Thus, it is necessary to develop a novel antimalarial agent. The objectives of this study were to construct a novel compound antimalarial transdermal nanosystem-ethosomal cataplasm, to investigate its characteristics and efficiency, and to systematically explore the penetration-enhancing mechanisms of ethosomal cataplasm. Artesunate-loaded ethosomes and febrifugine-loaded ethosomes were prepared, and their characteristics were evaluated. Drug-loaded ethosomes were incorporated in the matrix of cataplasm to form the compound antimalarial ethosomal cataplasm. With the help of ethosomal technology, the accumulated permeation quantity of artesunate significantly increased at 8 hours after administration, which was 1.57 times as much as that of conventional cataplasm. Soon after administration, the ethosomal cataplasm could make a large quantity of antimalarial drug quickly penetrate through skin, then the remaining drug in the ethosomal cataplasm could be steadily released. These characteristics of ethosomal cataplasm are favorable for antimalarial drugs to kill Plasmodium spp. quickly and prevent the resurgence of Plasmodium spp. As expected, the ethosomal cataplasm showed good antimalarial efficiency in this experiment. The negative conversion rates were 100% and the recurrence rates were 0% at all dosages. The mechanism of penetration enhancement of the ethosomal cataplasm was systematically explored using an optics microscope, polarization microscope, and transmission electron microscopy. The microstructure, ultrastructure, and birefringent structure in skin were observed. Data obtained in this study showed that the application of ethosomal technology to antimalarial cataplasm could improve the transdermal delivery of drug, enhance the efficacy, and facilitate practical application in clinic.

No MeSH data available.


Related in: MedlinePlus

Scanning electron microscope cross-section microphotographs of skins.Notes: (A) Untreated skin; (B) skin treated with ethosomal cataplasm; (C) skin treated with conventional cataplasm. The magnifications of (A–C) are all 200×.
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f15-ijn-10-4239: Scanning electron microscope cross-section microphotographs of skins.Notes: (A) Untreated skin; (B) skin treated with ethosomal cataplasm; (C) skin treated with conventional cataplasm. The magnifications of (A–C) are all 200×.

Mentions: The polarized light microscope could directly display the birefringent structure in unstained skin samples (Figure 14), such as collagenous fiber structure, and the changes in skin structure could be observed more clearly. After treatment with ethosomal cataplasm, the birefringent structure in the deep skin layer (corium layer) became even more disordered (Figure 14B). Furthermore, the orientation (independent polarization) pseudocolor microphotograph (Figure 14D–F) could provide more information about the structure of deep skin. Various colors represent different polarization orientations in Figure 14. The more disordered the birefringent structure was, the more varied the polarization orientation would be. So the complexity of the color system in the orientation microphotograph reflected the degree of disorder in the skin structure. In the study, the color system in skin treated with ethosomal cataplasm was the most complex (Figure 14E), especially in the deep skin layer. From the novel research perspective, this result indicated that etho-somes in cataplasm could penetrate deeply into the skin and change the fine-structure of skin. Scanning electron microscope cross-section microphotographs show that the ultrastructure of skin treated with ethosomal cataplasm became loose (Figure 15B).


Compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement.

Shen S, Liu SZ, Zhang YS, Du MB, Liang AH, Song LH, Ye ZG - Int J Nanomedicine (2015)

Scanning electron microscope cross-section microphotographs of skins.Notes: (A) Untreated skin; (B) skin treated with ethosomal cataplasm; (C) skin treated with conventional cataplasm. The magnifications of (A–C) are all 200×.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4494185&req=5

f15-ijn-10-4239: Scanning electron microscope cross-section microphotographs of skins.Notes: (A) Untreated skin; (B) skin treated with ethosomal cataplasm; (C) skin treated with conventional cataplasm. The magnifications of (A–C) are all 200×.
Mentions: The polarized light microscope could directly display the birefringent structure in unstained skin samples (Figure 14), such as collagenous fiber structure, and the changes in skin structure could be observed more clearly. After treatment with ethosomal cataplasm, the birefringent structure in the deep skin layer (corium layer) became even more disordered (Figure 14B). Furthermore, the orientation (independent polarization) pseudocolor microphotograph (Figure 14D–F) could provide more information about the structure of deep skin. Various colors represent different polarization orientations in Figure 14. The more disordered the birefringent structure was, the more varied the polarization orientation would be. So the complexity of the color system in the orientation microphotograph reflected the degree of disorder in the skin structure. In the study, the color system in skin treated with ethosomal cataplasm was the most complex (Figure 14E), especially in the deep skin layer. From the novel research perspective, this result indicated that etho-somes in cataplasm could penetrate deeply into the skin and change the fine-structure of skin. Scanning electron microscope cross-section microphotographs show that the ultrastructure of skin treated with ethosomal cataplasm became loose (Figure 15B).

Bottom Line: With the help of ethosomal technology, the accumulated permeation quantity of artesunate significantly increased at 8 hours after administration, which was 1.57 times as much as that of conventional cataplasm.The microstructure, ultrastructure, and birefringent structure in skin were observed.Data obtained in this study showed that the application of ethosomal technology to antimalarial cataplasm could improve the transdermal delivery of drug, enhance the efficacy, and facilitate practical application in clinic.

View Article: PubMed Central - PubMed

Affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, People's Republic of China.

ABSTRACT
Malaria is still a serious public health problem in some parts of the world. The problems of recurrence and drug resistance are increasingly more serious. Thus, it is necessary to develop a novel antimalarial agent. The objectives of this study were to construct a novel compound antimalarial transdermal nanosystem-ethosomal cataplasm, to investigate its characteristics and efficiency, and to systematically explore the penetration-enhancing mechanisms of ethosomal cataplasm. Artesunate-loaded ethosomes and febrifugine-loaded ethosomes were prepared, and their characteristics were evaluated. Drug-loaded ethosomes were incorporated in the matrix of cataplasm to form the compound antimalarial ethosomal cataplasm. With the help of ethosomal technology, the accumulated permeation quantity of artesunate significantly increased at 8 hours after administration, which was 1.57 times as much as that of conventional cataplasm. Soon after administration, the ethosomal cataplasm could make a large quantity of antimalarial drug quickly penetrate through skin, then the remaining drug in the ethosomal cataplasm could be steadily released. These characteristics of ethosomal cataplasm are favorable for antimalarial drugs to kill Plasmodium spp. quickly and prevent the resurgence of Plasmodium spp. As expected, the ethosomal cataplasm showed good antimalarial efficiency in this experiment. The negative conversion rates were 100% and the recurrence rates were 0% at all dosages. The mechanism of penetration enhancement of the ethosomal cataplasm was systematically explored using an optics microscope, polarization microscope, and transmission electron microscopy. The microstructure, ultrastructure, and birefringent structure in skin were observed. Data obtained in this study showed that the application of ethosomal technology to antimalarial cataplasm could improve the transdermal delivery of drug, enhance the efficacy, and facilitate practical application in clinic.

No MeSH data available.


Related in: MedlinePlus