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Ethosomal Gel for Improving Transdermal Delivery of Thymosin β-4.
Int J Nanomedicine. 2019; 14:9275-9284.IJ

Abstract

Purpose

Thymosin β-4(Tβ-4) is a macromolecular protein drug with potential for drug development in wound repair but is limited by the shortcomings of macromolecular protein, such as large volumes, poor membrane permeability, and unstable physicochemical characteristics. Ethosomes could enhance cell membrane fluidity and reduce epidermal membrane density to make macromolecular drugs through the stratum corneum into the deeper layers of the skin easily. Herein, we developed and characterized a novel transdermal delivery vehicle to load macromolecular protein peptides and use Tβ-4 as a model drug wrapped into ethosomes.

Methods

We used the orthogonal method to optimize the formulation of the ethosome preparation prepared by the ethonal infusion method. Ethosomal gels were characterized by using different analytical methods. Transdermal release rate in vitro have been demonstrated in Franz diffusion cells and the efficacy of drug-loaded nanocarriers in vivo was investigated in a mouse model.

Results

Optimized Tβ-4 ethosomal gels have good physicochemical properties. The drug amounts of the cumulative release in the ethosomal gel within 5 hours were 1.67 times that of the T-β4 gel in vitro release study, and the wound healing time of ethosomal gel group was only half of the T-β4 gel group in vivo pharmacokinetic study. Compared with the free drug group, the ethosome preparation not only promotes the percutaneous absorption process of the macromolecular protein drugs but also shortened wound recovery time.

Conclusion

Hence, we provide a possible good design for ethosomal gel system that can load macromolecular protein peptide drugs to achieve transdermal drug administration, promoting the percutaneous absorption of the drug and improving the effect.

Authors+Show Affiliations

School of Pharmaceutical Science, Shandong University, Jinan 250012,People's Republic of China.School of Mechanical & Automotive Engineering, Qilu University of Technology (Shandong Academy of Sciences), Jinan 250353, People's Republic of China.School of Pharmaceutical Science, Shandong University, Jinan 250012,People's Republic of China.The Second Hospital of Shandong University, Jinan 250033, People's Republic of China.The Second Hospital of Shandong University, Jinan 250033, People's Republic of China.School of Pharmaceutical Science, Shandong University, Jinan 250012,People's Republic of China.School of Pharmaceutical Science, Shandong University, Jinan 250012,People's Republic of China.School of Pharmaceutical Science, Shandong University, Jinan 250012,People's Republic of China.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

31819429

Citation

Fu, Xianglei, et al. "Ethosomal Gel for Improving Transdermal Delivery of Thymosin Β-4." International Journal of Nanomedicine, vol. 14, 2019, pp. 9275-9284.
Fu X, Shi Y, Wang H, et al. Ethosomal Gel for Improving Transdermal Delivery of Thymosin β-4. Int J Nanomedicine. 2019;14:9275-9284.
Fu, X., Shi, Y., Wang, H., Zhao, X., Sun, Q., Huang, Y., Qi, T., & Lin, G. (2019). Ethosomal Gel for Improving Transdermal Delivery of Thymosin β-4. International Journal of Nanomedicine, 14, 9275-9284. https://doi.org/10.2147/IJN.S228863
Fu X, et al. Ethosomal Gel for Improving Transdermal Delivery of Thymosin Β-4. Int J Nanomedicine. 2019;14:9275-9284. PubMed PMID: 31819429.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Ethosomal Gel for Improving Transdermal Delivery of Thymosin β-4. AU - Fu,Xianglei, AU - Shi,Yanbin, AU - Wang,Hui, AU - Zhao,Xiaogang, AU - Sun,Qifeng, AU - Huang,Yi, AU - Qi,Tongtong, AU - Lin,Guimei, Y1 - 2019/11/27/ PY - 2019/08/27/received PY - 2019/11/16/accepted PY - 2019/12/11/entrez PY - 2019/12/11/pubmed PY - 2019/12/11/medline KW - ethosomes KW - macromolecular protein drugs KW - skin wound healing KW - transdermal drug delivery system SP - 9275 EP - 9284 JF - International journal of nanomedicine JO - Int J Nanomedicine VL - 14 N2 - Purpose: Thymosin β-4(Tβ-4) is a macromolecular protein drug with potential for drug development in wound repair but is limited by the shortcomings of macromolecular protein, such as large volumes, poor membrane permeability, and unstable physicochemical characteristics. Ethosomes could enhance cell membrane fluidity and reduce epidermal membrane density to make macromolecular drugs through the stratum corneum into the deeper layers of the skin easily. Herein, we developed and characterized a novel transdermal delivery vehicle to load macromolecular protein peptides and use Tβ-4 as a model drug wrapped into ethosomes. Methods: We used the orthogonal method to optimize the formulation of the ethosome preparation prepared by the ethonal infusion method. Ethosomal gels were characterized by using different analytical methods. Transdermal release rate in vitro have been demonstrated in Franz diffusion cells and the efficacy of drug-loaded nanocarriers in vivo was investigated in a mouse model. Results: Optimized Tβ-4 ethosomal gels have good physicochemical properties. The drug amounts of the cumulative release in the ethosomal gel within 5 hours were 1.67 times that of the T-β4 gel in vitro release study, and the wound healing time of ethosomal gel group was only half of the T-β4 gel group in vivo pharmacokinetic study. Compared with the free drug group, the ethosome preparation not only promotes the percutaneous absorption process of the macromolecular protein drugs but also shortened wound recovery time. Conclusion: Hence, we provide a possible good design for ethosomal gel system that can load macromolecular protein peptide drugs to achieve transdermal drug administration, promoting the percutaneous absorption of the drug and improving the effect. SN - 1178-2013 UR - https://www.unboundmedicine.com/medline/citation/31819429/Ethosomal_Gel_for_Improving_Transdermal_Delivery_of_Thymosin_β-4 L2 - https://dx.doi.org/10.2147/IJN.S228863 DB - PRIME DP - Unbound Medicine ER -