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Albendazole solid dispersions prepared using PEG6000 and Poloxamer188: formulation, characterization and in vivo evaluation.
Pharm Dev Technol. 2020 Jul 03 [Online ahead of print]PD

Abstract

This study aimed to optimize the preparation process of albendazole (ABZ) solid dispersion (SD) and enhance its dissolution rate and oral bioavailability in dogs. The ABZ-SD formulations were prepared by a fusion method with ABZ and polyethylene glycol 6000 (PEG 6000), poloxamer 188 (P 188) polymers at various weight ratios or the combination of PEG 6000&P 188. The characterizations of the optimal formulations were performed by scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), in vitro dissolution test and molecular docking. The in vivo pharmacokinetic study was conducted in beagle dogs. As a result, ABZ solid dispersion based on PEG 6000&P 188 (1:2) was successfully prepared. The ABZ-SD formulation could significantly improve the apparent solubility and dissolution rate of ABZ compared with commercial tablets. Furthermore, the water solubility of ABZ-SD was improved mainly based on hydrogen bond association. Besides, at an oral dosage of 15 mg/kg ABZ, the SDs had higher Cmax values and areas under the curve (AUCs) compared to those of commercial ABZ tablets. Preparation of ABZ-loaded SDs by PEG 6000&P 188 is a promising strategy to improve the oral bioavailability of ABZ.

Authors+Show Affiliations

College of Veterinary Medicine, Northeast Agricultural University, Harbin, China. Heilongjiang Key Laboratory for Animal Disease Control and Pharmaceutical Development, Harbin, China.College of Veterinary Medicine, Northeast Agricultural University, Harbin, China. Heilongjiang Key Laboratory for Animal Disease Control and Pharmaceutical Development, Harbin, China.College of Veterinary Medicine, Northeast Agricultural University, Harbin, China. Heilongjiang Key Laboratory for Animal Disease Control and Pharmaceutical Development, Harbin, China.College of Veterinary Medicine, Northeast Agricultural University, Harbin, China. Heilongjiang Key Laboratory for Animal Disease Control and Pharmaceutical Development, Harbin, China.College of Veterinary Medicine, Northeast Agricultural University, Harbin, China. Heilongjiang Key Laboratory for Animal Disease Control and Pharmaceutical Development, Harbin, China.College of Veterinary Medicine, Northeast Agricultural University, Harbin, China. Heilongjiang Key Laboratory for Animal Disease Control and Pharmaceutical Development, Harbin, China.College of Veterinary Medicine, Northeast Agricultural University, Harbin, China. Heilongjiang Key Laboratory for Animal Disease Control and Pharmaceutical Development, Harbin, China.College of Veterinary Medicine, Northeast Agricultural University, Harbin, China. Heilongjiang Key Laboratory for Animal Disease Control and Pharmaceutical Development, Harbin, China.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32546042

Citation

Dong, Chun-Liu, et al. "Albendazole Solid Dispersions Prepared Using PEG6000 and Poloxamer188: Formulation, Characterization and in Vivo Evaluation." Pharmaceutical Development and Technology, 2020, pp. 1-10.
Dong CL, Zheng SD, Liu YY, et al. Albendazole solid dispersions prepared using PEG6000 and Poloxamer188: formulation, characterization and in vivo evaluation. Pharm Dev Technol. 2020.
Dong, C. L., Zheng, S. D., Liu, Y. Y., Cui, W. Q., Hao, M. Q., God'spower, B. O., Chen, X. Y., & Li, Y. H. (2020). Albendazole solid dispersions prepared using PEG6000 and Poloxamer188: formulation, characterization and in vivo evaluation. Pharmaceutical Development and Technology, 1-10. https://doi.org/10.1080/10837450.2020.1783553
Dong CL, et al. Albendazole Solid Dispersions Prepared Using PEG6000 and Poloxamer188: Formulation, Characterization and in Vivo Evaluation. Pharm Dev Technol. 2020 Jul 3;1-10. PubMed PMID: 32546042.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Albendazole solid dispersions prepared using PEG6000 and Poloxamer188: formulation, characterization and in vivo evaluation. AU - Dong,Chun-Liu, AU - Zheng,Si-Di, AU - Liu,Yan-Yan, AU - Cui,Wen-Qiang, AU - Hao,Mei-Qi, AU - God'spower,Bello-Onaghise, AU - Chen,Xue-Ying, AU - Li,Yan-Hua, Y1 - 2020/07/03/ PY - 2020/6/18/pubmed PY - 2020/6/18/medline PY - 2020/6/18/entrez KW - Albendazole KW - dissolution KW - molecular docking KW - oral bioavailability KW - solid dispersion SP - 1 EP - 10 JF - Pharmaceutical development and technology JO - Pharm Dev Technol N2 - This study aimed to optimize the preparation process of albendazole (ABZ) solid dispersion (SD) and enhance its dissolution rate and oral bioavailability in dogs. The ABZ-SD formulations were prepared by a fusion method with ABZ and polyethylene glycol 6000 (PEG 6000), poloxamer 188 (P 188) polymers at various weight ratios or the combination of PEG 6000&P 188. The characterizations of the optimal formulations were performed by scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), in vitro dissolution test and molecular docking. The in vivo pharmacokinetic study was conducted in beagle dogs. As a result, ABZ solid dispersion based on PEG 6000&P 188 (1:2) was successfully prepared. The ABZ-SD formulation could significantly improve the apparent solubility and dissolution rate of ABZ compared with commercial tablets. Furthermore, the water solubility of ABZ-SD was improved mainly based on hydrogen bond association. Besides, at an oral dosage of 15 mg/kg ABZ, the SDs had higher Cmax values and areas under the curve (AUCs) compared to those of commercial ABZ tablets. Preparation of ABZ-loaded SDs by PEG 6000&P 188 is a promising strategy to improve the oral bioavailability of ABZ. SN - 1097-9867 UR - https://www.unboundmedicine.com/medline/citation/32546042/Albendazole_solid_dispersions_prepared_using_PEG6000_and_Poloxamer188:_formulation,_characterization_and_in vivo_evaluation L2 - http://www.tandfonline.com/doi/full/10.1080/10837450.2020.1783553 DB - PRIME DP - Unbound Medicine ER -
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