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ORIGINAL RESEARCH article

Front. Vet. Sci.
Sec. Veterinary Pharmacology and Toxicology
Volume 11 - 2024 | doi: 10.3389/fvets.2024.1522856

Combining Solubilization and Controlled Release Strategies to Prepare pH-Sensitive Solid Dispersion Loaded with Albendazole: In Vitro and In Vivo Studies

Provisionally accepted
Dehai Su Dehai Su Bai Mingyang Bai Mingyang Chaoqun Wei Chaoqun Wei Xiangyang Long Xiangyang Long 雪真 刘 雪真 刘 Xiangguang Shen Xiangguang Shen Huanzhong Ding Huanzhong Ding *
  • Guangdong Provincial Key Laboratory of Veterinary Drugs Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, China

The final, formatted version of the article will be published soon.

    Albendazole (ABZ), classified as a class II basic drug under the Biopharmaceutics Classification System (BCS), is widely recognized for its therapeutic efficacy in treating and preventing trichuriasis. However, despite its clinical relevance, ABZ's oral administration presents challenges due to its poor solubility and pH sensitivity, which diminish its therapeutic effectiveness. Additionally, high dosing regimens of ABZ pose risks of developmental toxicity in animal models.This study developed a pH-sensitive solid dispersion of albendazole (ABZ-pHs-SD) using Glyceryl Monostearate (GM) in conjunction with Hypromellose Acetate Succinate (HPMC-AS).Characterization via Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), and Fourier Transform Infrared Spectroscopy (FT-IR) confirmed the high dispersion of ABZ in a crystalline state within the carrier. Furthermore, we compared the in vitro dissolution profile, pharmacokinetics, and intestinal drug concentration of ABZ-pHs-SD with commercially available formulations. Our findings demonstrated that ABZ-pHs-SD exhibited an excellent dissolution profile, significantly increasing the solubility of ABZ in water by 3.15 times. The formulation effectively prevented drug release in acidic environments while maintaining a slow release in weakly alkaline conditions.Additionally, compared to commercial formulations, ABZ-pHs-SD showed significantly lower Cmax (4.70 ± 1.16 vs. 6.83 ± 0.66 µg/mL) and higher Tmax (5.5 ± 0.93 vs. 3.75 ± 0.71 h) in vivo, achieving elevated drug concentration levels in the cecal and colonic environments (p < 0.01) without significantly decreasing bioavailability. Overall, our research findings indicate that ABZ-pHs-SD serves as a promising drug delivery strategy for the poorly soluble and pH-sensitive ABZ. Particularly, the simple preparation of solid dispersion demonstrates strong industrial feasibility.

    Keywords: Albendazole, Controlled Release, HPMC-AS, pharmacokinetics, Solid dispersion

    Received: 05 Nov 2024; Accepted: 11 Dec 2024.

    Copyright: © 2024 Su, Mingyang, Wei, Long, 刘, Shen and Ding. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

    * Correspondence: Huanzhong Ding, Guangdong Provincial Key Laboratory of Veterinary Drugs Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, China

    Disclaimer: All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.