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Development of triptolide-nanoemulsion gels for percutaneous administration: physicochemical, transport, pharmacokinetic and pharmacodynamic characteristics.
J Nanobiotechnology. 2017 Dec 04; 15(1):88.JN

Abstract

BACKGROUND

This work aimed to provide useful information on the use of nanoemulsions for the percutaneous administration of triptolide. Lipid nanosystems have great potential for transdermal drug delivery. Nanoemulsions and nanoemulsion gels were prepared to enhance percutaneous permeation. Microstructure and in vitro/in vivo percutaneous delivery characteristics of triptolide (TPL)-nanoemulsions and TPL-nanoemulsion gels were compared. The integrity of the nanoemulsions and nanoemulsion gels during transdermal delivery and its effects on the surface of skin were also investigated. The penetration mechanisms of nanoemulsions and nanoemulsion gels were investigated by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The transport characteristics of fluorescence-labelled nanoemulsions were probed using laser scanning confocal microscopy. A chronic dermatitis/eczema model in mice ears and the pharmacodynamic of the TPL-nanoemulsion gels were also investigated.

RESULTS

Compared to TPL gels, significantly greater cumulative amounts of TPL-nanoemulsion gels and TPL-nanoemulsions penetrated rat skin in vitro. The in vivo microdialysis showed the concentration-time curve AUC0-t for TPL-NPs is bigger than the TPL-gels. At the same time, TPL-NPs had a larger effect on the surface of skin. By hydrating keratin and changing the structure of both the stratum corneum lipids and keratin, nanoemulsions and nanoemulsion gels influence skin to promote percutaneous drug penetration. Both hairfollicles and the stratum corneum are also important in this transdermal drug delivery system. Moderate and high dosages of the TPL-nanoemulsion gels can significantly improve the symptoms of dermatitis/eczema inflammation and edema erythematic in mice ears and can reduce the expression of IFN-γ and IL-4. Moreover, the TPL-nanoemulsion gels cause less gastrointestinal damage than that of the Tripterygium wilfordii oral tablet does.

CONCLUSIONS

Nanoemulsions could be suitable for transdermal stably releasing drugs and maintaining the effective drug concentration. The TPL-nanoemulsion gels provided higher percutaneous amounts than other carriers did. These findings suggest that nanoemulsion gels could be promising percutaneous carriers for TPL. The TPL-nanoemulsion gels have a significant treatment effect on dermatitis/eczema in the mice model and is expected to provide a new, low-toxicity and long-term preparation for the clinical treatment of dermatitis/eczema in transdermal drug delivery systems.

Authors+Show Affiliations

Department of Pharmacy, Changhai Hospital, Second Military Medical University, Shanghai, 200433, China.Department of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan, 250355, China.Department of Pharmacy, Changhai Hospital, Second Military Medical University, Shanghai, 200433, China.Department of Pharmacy, Changhai Hospital, Second Military Medical University, Shanghai, 200433, China.Department of Pharmacy, Changhai Hospital, Second Military Medical University, Shanghai, 200433, China. liujiyong999@126.com.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29202753

Citation

Yang, Meng, et al. "Development of Triptolide-nanoemulsion Gels for Percutaneous Administration: Physicochemical, Transport, Pharmacokinetic and Pharmacodynamic Characteristics." Journal of Nanobiotechnology, vol. 15, no. 1, 2017, p. 88.
Yang M, Gu Y, Yang D, et al. Development of triptolide-nanoemulsion gels for percutaneous administration: physicochemical, transport, pharmacokinetic and pharmacodynamic characteristics. J Nanobiotechnology. 2017;15(1):88.
Yang, M., Gu, Y., Yang, D., Tang, X., & Liu, J. (2017). Development of triptolide-nanoemulsion gels for percutaneous administration: physicochemical, transport, pharmacokinetic and pharmacodynamic characteristics. Journal of Nanobiotechnology, 15(1), 88. https://doi.org/10.1186/s12951-017-0323-0
Yang M, et al. Development of Triptolide-nanoemulsion Gels for Percutaneous Administration: Physicochemical, Transport, Pharmacokinetic and Pharmacodynamic Characteristics. J Nanobiotechnology. 2017 Dec 4;15(1):88. PubMed PMID: 29202753.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of triptolide-nanoemulsion gels for percutaneous administration: physicochemical, transport, pharmacokinetic and pharmacodynamic characteristics. AU - Yang,Meng, AU - Gu,Yongwei, AU - Yang,Dishun, AU - Tang,Xiaomeng, AU - Liu,Jiyong, Y1 - 2017/12/04/ PY - 2017/07/16/received PY - 2017/11/25/accepted PY - 2017/12/6/entrez PY - 2017/12/6/pubmed PY - 2018/7/20/medline KW - Chronic dermatitis/eczema model KW - Nanoemulsion gels KW - Nanoemulsions KW - Skin-vessel synchronous microdialysis KW - Transdermal drug delivery system KW - Triptolide SP - 88 EP - 88 JF - Journal of nanobiotechnology JO - J Nanobiotechnology VL - 15 IS - 1 N2 - BACKGROUND: This work aimed to provide useful information on the use of nanoemulsions for the percutaneous administration of triptolide. Lipid nanosystems have great potential for transdermal drug delivery. Nanoemulsions and nanoemulsion gels were prepared to enhance percutaneous permeation. Microstructure and in vitro/in vivo percutaneous delivery characteristics of triptolide (TPL)-nanoemulsions and TPL-nanoemulsion gels were compared. The integrity of the nanoemulsions and nanoemulsion gels during transdermal delivery and its effects on the surface of skin were also investigated. The penetration mechanisms of nanoemulsions and nanoemulsion gels were investigated by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The transport characteristics of fluorescence-labelled nanoemulsions were probed using laser scanning confocal microscopy. A chronic dermatitis/eczema model in mice ears and the pharmacodynamic of the TPL-nanoemulsion gels were also investigated. RESULTS: Compared to TPL gels, significantly greater cumulative amounts of TPL-nanoemulsion gels and TPL-nanoemulsions penetrated rat skin in vitro. The in vivo microdialysis showed the concentration-time curve AUC0-t for TPL-NPs is bigger than the TPL-gels. At the same time, TPL-NPs had a larger effect on the surface of skin. By hydrating keratin and changing the structure of both the stratum corneum lipids and keratin, nanoemulsions and nanoemulsion gels influence skin to promote percutaneous drug penetration. Both hairfollicles and the stratum corneum are also important in this transdermal drug delivery system. Moderate and high dosages of the TPL-nanoemulsion gels can significantly improve the symptoms of dermatitis/eczema inflammation and edema erythematic in mice ears and can reduce the expression of IFN-γ and IL-4. Moreover, the TPL-nanoemulsion gels cause less gastrointestinal damage than that of the Tripterygium wilfordii oral tablet does. CONCLUSIONS: Nanoemulsions could be suitable for transdermal stably releasing drugs and maintaining the effective drug concentration. The TPL-nanoemulsion gels provided higher percutaneous amounts than other carriers did. These findings suggest that nanoemulsion gels could be promising percutaneous carriers for TPL. The TPL-nanoemulsion gels have a significant treatment effect on dermatitis/eczema in the mice model and is expected to provide a new, low-toxicity and long-term preparation for the clinical treatment of dermatitis/eczema in transdermal drug delivery systems. SN - 1477-3155 UR - https://www.unboundmedicine.com/medline/citation/29202753/Development_of_triptolide_nanoemulsion_gels_for_percutaneous_administration:_physicochemical_transport_pharmacokinetic_and_pharmacodynamic_characteristics_ L2 - https://jnanobiotechnology.biomedcentral.com/articles/10.1186/s12951-017-0323-0 DB - PRIME DP - Unbound Medicine ER -