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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

Influence of ethosomes on the release of (A) artesunate and (B) febrifugine from cataplasm (n=6).
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f10-ijn-10-4239: Influence of ethosomes on the release of (A) artesunate and (B) febrifugine from cataplasm (n=6).

Mentions: The drug release behaviors of ethosomal cataplasm and conventional cataplasm are shown in Table 7 and Figure 10. The release of artesunate and febrifugine from the investigated formulations followed the Higuchi equation.34 Compared with conventional cataplasm, ethosomal cataplasm showed a higher release rate. The drug release rates of ethosomal cataplasm were 0.2277 mg/cm2/h1/2 (artesunate) and 1.6563 μg/cm2/h1/2 (febrifugine). The drug release rates of conventional cataplasm were 0.2136 mg/cm2/h1/2 (artesunate) and 0.8846 μg/cm2/h1/2 (febrifugine) (Table 7; Figure 10). With the help of ethosomes, the accumulative release quantity of artesunate at 8 hours after administration was 1.14 times as much as that of conventional cataplasm (P<0.05), and the accumulated release quantity of febrifugine at 8 hours after administration of ethosomal cataplasm was 1.86 times as much as that of conventional cataplasm (P<0.05). Ethosomal technology could accelerate drug release from cataplasm.


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)

Influence of ethosomes on the release of (A) artesunate and (B) febrifugine from cataplasm (n=6).
© Copyright Policy
Related In: Results  -  Collection

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

f10-ijn-10-4239: Influence of ethosomes on the release of (A) artesunate and (B) febrifugine from cataplasm (n=6).
Mentions: The drug release behaviors of ethosomal cataplasm and conventional cataplasm are shown in Table 7 and Figure 10. The release of artesunate and febrifugine from the investigated formulations followed the Higuchi equation.34 Compared with conventional cataplasm, ethosomal cataplasm showed a higher release rate. The drug release rates of ethosomal cataplasm were 0.2277 mg/cm2/h1/2 (artesunate) and 1.6563 μg/cm2/h1/2 (febrifugine). The drug release rates of conventional cataplasm were 0.2136 mg/cm2/h1/2 (artesunate) and 0.8846 μg/cm2/h1/2 (febrifugine) (Table 7; Figure 10). With the help of ethosomes, the accumulative release quantity of artesunate at 8 hours after administration was 1.14 times as much as that of conventional cataplasm (P<0.05), and the accumulated release quantity of febrifugine at 8 hours after administration of ethosomal cataplasm was 1.86 times as much as that of conventional cataplasm (P<0.05). Ethosomal technology could accelerate drug release from cataplasm.

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