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Indian Journal of Pharmaceutical Education and ResearchNOW IN
Article

Enhancement of Avermectin Water-solubility by Addition of Poloxamer 188 and Deep Eutectic Solvent into PEG 6000 Solid Dispersion System

Xue-Hua He1, Meng Chen2, Yang Pu3, Xing-Zhou Huang3, He Han2, Zhi-Min Jin2★★ Corresponding author

  1. 1College of Materials Science and Engineering, Zhejiang University of Technology, Hangzhou, Zhejiang Province, CHINA.
  2. 2College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou, Zhejiang Province, CHINA.
  3. 3Shaoxing Testing Institute of Quality and Technical Supervision, Shaoxing, Zhejiang Province, CHINA.

CORRESPONDENCE

Zhi-Min Jin

College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou-310014, CHINA.

apharm@sina.com

Received: 18-12-2021; Revised: 28-03-2022; Accepted: 24-06-2022.

Volume 57, Issue 3 · pp. 736–741 · PUBLISHED 2023 · DOI: 10.5530/ijper.57.3.89

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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