Enhancement of Avermectin Water-solubility by Addition of Poloxamer 188 and Deep Eutectic Solvent into PEG 6000 Solid Dispersion System
1, 2, 3, 3, 2, 2
- 1College of Materials Science and Engineering, Zhejiang University of Technology, Hangzhou, Zhejiang Province, CHINA.
- 2College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou, Zhejiang Province, CHINA.
- 3Shaoxing Testing Institute of Quality and Technical Supervision, Shaoxing, Zhejiang Province, CHINA.
CORRESPONDENCE
Prof. Zhi-Min Jin
College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou-310014, CHINA.
Received: 18-12-2021; Accepted: 24-06-2022.
Volume 57, Issue 3 · pp. 736-741 · 2023 · DOI: 10.5530/ijper.57.3.89
ABSTRACT
Background: It has been reported previously that AV water-solubility was enhanced great by solid dispersion in PEG6k carrier.Materials and Methods: In this study, AV water-solubility was improved primarily by addition of PLX188 into PEG6k carrier, and further by addition of a deep eutectic solvent of CBU (choline chloride, betaine and urea) in the combinatory carrier of PEG6k and PLX188.Results: The result showed that the water-solubility of AV-PEG6k-PLX188 solid dispersion was 10.8 times of AV-PEG6k solid dispersion, and the cumulative dissolution rate (within 60 min) of AV-PEG6k-PLX188 solid dispersion was 3.3 times of AV-PEG6k solid dispersions. With the further addition of CBU in the AV-PEG6k-PLX188 system, the water-solubility of AV-PEG6k-PLX188-CBU solid dispersion was increased by 3.4 times, and the cumulative dissolution rate (within 60 min) was increased by 1.6 times. The X-ray powder diffraction measurement indicated that AV existed in the AV-PEG6k-PLX188-CBU solid dispersion as a non-crystalline state. Further, the in vitro toxicity against 3rd instar Asiatic migratory locust was measured, which showed that the LC50 of the AV-PEG6k-PLX188-CBU solid dispersion (0.88 mg/L) was a third of that of AV emulsifiable concentrate (2.64 mg/L), suggesting a higher bioavailability.Conclusion: The finding of this work showed that AV-PEG6k-PLX188-CBU solid dispersion was more effective than AV emulsifiable concentrate, in suppressing or killing locusts.
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He, X., Chen, M., Pu, Y., Huang, X., Han, H., & Jin, Z. (2023). Enhancement of Avermectin Water-solubility by Addition of Poloxamer 188 and Deep Eutectic Solvent into PEG 6000 Solid Dispersion System. Indian Journal of Pharmaceutical Education and Research, 57(3), 736-741. https://doi.org/10.5530/ijper.57.3.89
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