Phospholipid Complexation for Bioavailability Improvement of Albendazole: Preparation, Characterization and In Vivo Evaluation

Liyao Liu; Jinju Nie; Letao Li

doi:10.1208/s12249-022-02497-1

Phospholipid Complexation for Bioavailability Improvement of Albendazole: Preparation, Characterization and In Vivo Evaluation

Liyao Liu, Jinju Nie^*, Letao Li

^*Corresponding author for this work

Pharmacy

Research output: Contribution to journal › Article › Academic › peer-review

7 Citations (Scopus)

Abstract

The current study aimed to improve the poor solubility of albendazole (ABZ) by means of phospholipid complexation, hence to improve its oral bioavailability. The solvent-evaporation method for ABZ-phospholipid complex (ABZ-PC) preparation was established for the first time. And a systematic optimization of preparation conditions of ABZ-PC was performed. Physicochemical studies of ABZ-PC were performed with FTIR, DSC, and XRD measurements to confirm the formation of the ABZ-PC and reveal the interaction mechanism between ABZ and phospholipid molecules. Solubility determination and morphological characterization were applied to verify the solubility improvement of prepared ABZ-PC. Moreover, the pharmacokinetic performance of ABZ-PC was further evaluated in vivo compared with raw materials of ABZ. Under optimal preparation conditions, the AE of ABZ-PC could be approximately 100%. Physicochemical studies indicated that the P = O group in the phospholipid molecule would interact with the N-H group in the ABZ molecule through hydrogen bonds and ABZ was dispersed in an amorphous state after being prepared into ABZ-PC. The aqueous solubility of ABZ-PC in deionized water (pH7.0) improved by 30-folds than free ABZ, and the AUC(0-t) of ABZ-PC was significantly increased by 2.32 times in comparison with raw materials of ABZ through oral administration. The current study developed an effective method for the phospholipid complexation of ABZ. With significantly improved solubility in an aqueous environment, the prepared ABZ-PC exhibited improved oral bioavailability and pharmacokinetic characteristics indicating it could be potentially applied in the oral drug delivery of ABZ.

Original language	English
Article number	36
Journal	AAPS PharmSciTech
Volume	24
Issue number	1
DOIs	https://doi.org/10.1208/s12249-022-02497-1
Publication status	Published - 12 Jan 2023

Bibliographical note

Funding Information:
This work was supported by the project of Scientific Research Program of Tianjin Municipal Education Commission (Grant No. 2017KJ181).

Publisher Copyright:
© 2023, The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.

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10.1208/s12249-022-02497-1

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title = "Phospholipid Complexation for Bioavailability Improvement of Albendazole: Preparation, Characterization and In Vivo Evaluation",

abstract = "The current study aimed to improve the poor solubility of albendazole (ABZ) by means of phospholipid complexation, hence to improve its oral bioavailability. The solvent-evaporation method for ABZ-phospholipid complex (ABZ-PC) preparation was established for the first time. And a systematic optimization of preparation conditions of ABZ-PC was performed. Physicochemical studies of ABZ-PC were performed with FTIR, DSC, and XRD measurements to confirm the formation of the ABZ-PC and reveal the interaction mechanism between ABZ and phospholipid molecules. Solubility determination and morphological characterization were applied to verify the solubility improvement of prepared ABZ-PC. Moreover, the pharmacokinetic performance of ABZ-PC was further evaluated in vivo compared with raw materials of ABZ. Under optimal preparation conditions, the AE of ABZ-PC could be approximately 100\%. Physicochemical studies indicated that the P = O group in the phospholipid molecule would interact with the N-H group in the ABZ molecule through hydrogen bonds and ABZ was dispersed in an amorphous state after being prepared into ABZ-PC. The aqueous solubility of ABZ-PC in deionized water (pH7.0) improved by 30-folds than free ABZ, and the AUC(0-t) of ABZ-PC was significantly increased by 2.32 times in comparison with raw materials of ABZ through oral administration. The current study developed an effective method for the phospholipid complexation of ABZ. With significantly improved solubility in an aqueous environment, the prepared ABZ-PC exhibited improved oral bioavailability and pharmacokinetic characteristics indicating it could be potentially applied in the oral drug delivery of ABZ.",

author = "Liyao Liu and Jinju Nie and Letao Li",

note = "Funding Information: This work was supported by the project of Scientific Research Program of Tianjin Municipal Education Commission (Grant No. 2017KJ181). Publisher Copyright: {\textcopyright} 2023, The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.",

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T2 - Preparation, Characterization and In Vivo Evaluation

AU - Liu, Liyao

AU - Nie, Jinju

AU - Li, Letao

N1 - Funding Information: This work was supported by the project of Scientific Research Program of Tianjin Municipal Education Commission (Grant No. 2017KJ181). Publisher Copyright: © 2023, The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.

PY - 2023/1/12

Y1 - 2023/1/12

N2 - The current study aimed to improve the poor solubility of albendazole (ABZ) by means of phospholipid complexation, hence to improve its oral bioavailability. The solvent-evaporation method for ABZ-phospholipid complex (ABZ-PC) preparation was established for the first time. And a systematic optimization of preparation conditions of ABZ-PC was performed. Physicochemical studies of ABZ-PC were performed with FTIR, DSC, and XRD measurements to confirm the formation of the ABZ-PC and reveal the interaction mechanism between ABZ and phospholipid molecules. Solubility determination and morphological characterization were applied to verify the solubility improvement of prepared ABZ-PC. Moreover, the pharmacokinetic performance of ABZ-PC was further evaluated in vivo compared with raw materials of ABZ. Under optimal preparation conditions, the AE of ABZ-PC could be approximately 100%. Physicochemical studies indicated that the P = O group in the phospholipid molecule would interact with the N-H group in the ABZ molecule through hydrogen bonds and ABZ was dispersed in an amorphous state after being prepared into ABZ-PC. The aqueous solubility of ABZ-PC in deionized water (pH7.0) improved by 30-folds than free ABZ, and the AUC(0-t) of ABZ-PC was significantly increased by 2.32 times in comparison with raw materials of ABZ through oral administration. The current study developed an effective method for the phospholipid complexation of ABZ. With significantly improved solubility in an aqueous environment, the prepared ABZ-PC exhibited improved oral bioavailability and pharmacokinetic characteristics indicating it could be potentially applied in the oral drug delivery of ABZ.

AB - The current study aimed to improve the poor solubility of albendazole (ABZ) by means of phospholipid complexation, hence to improve its oral bioavailability. The solvent-evaporation method for ABZ-phospholipid complex (ABZ-PC) preparation was established for the first time. And a systematic optimization of preparation conditions of ABZ-PC was performed. Physicochemical studies of ABZ-PC were performed with FTIR, DSC, and XRD measurements to confirm the formation of the ABZ-PC and reveal the interaction mechanism between ABZ and phospholipid molecules. Solubility determination and morphological characterization were applied to verify the solubility improvement of prepared ABZ-PC. Moreover, the pharmacokinetic performance of ABZ-PC was further evaluated in vivo compared with raw materials of ABZ. Under optimal preparation conditions, the AE of ABZ-PC could be approximately 100%. Physicochemical studies indicated that the P = O group in the phospholipid molecule would interact with the N-H group in the ABZ molecule through hydrogen bonds and ABZ was dispersed in an amorphous state after being prepared into ABZ-PC. The aqueous solubility of ABZ-PC in deionized water (pH7.0) improved by 30-folds than free ABZ, and the AUC(0-t) of ABZ-PC was significantly increased by 2.32 times in comparison with raw materials of ABZ through oral administration. The current study developed an effective method for the phospholipid complexation of ABZ. With significantly improved solubility in an aqueous environment, the prepared ABZ-PC exhibited improved oral bioavailability and pharmacokinetic characteristics indicating it could be potentially applied in the oral drug delivery of ABZ.

UR - https://www.scopus.com/pages/publications/85146195231

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DO - 10.1208/s12249-022-02497-1

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SN - 1530-9932

VL - 24

JO - AAPS PharmSciTech

JF - AAPS PharmSciTech

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M1 - 36

ER -

Phospholipid Complexation for Bioavailability Improvement of Albendazole: Preparation, Characterization and In Vivo Evaluation

Abstract

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