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Nanosized-Loratadine Embedded Orodispersible Films for Enhanced Bioavailability: Scalable Preparations and Characterizations

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Abstract

The patient-centric strategy urges the pharmaceutical companies to develop orodispersible films (ODF) as a new approach for pediatrics. However, the most common ODF-fabricated method, solvent casting, is facing the safety challenges of safety during manufacturing. To obtain favorable formulations with the ease of use and rapid dissolution, nanotechnology has been accounted for the development process. In this work, we investigated the wet-milling technique in preparing nanocarriers for loratadine—a hydrophobic anti-histamine drug. The results showed that the wet-milling technique could produce nanocarriers at the size of 400 nm. The reduction of particle size induced the increase of solubility and the dissolution rate of loratadine. Moreover, the pre-formulation of nanosized materials could adapt to the preparation of orodispersible films that disintegrated (less than 60s) and dissolved quickly. The DSC results showed that after the milling process, the crystallinity of loratadine was unchanged; however, the reduction in size induced an enhancement of drug bioavailability. After orally administrated to rats, the drug was quickly reached to the blood circulation, just after 30 min. Cmax increased from 44.97 ng/mL for the raw drug to 101.02 ng/mL for the nanocrystal leading to an enhancement of the AUC0-24h by 5.69-fold when the nanocrystal ODF was administrated. The ease of formulation and the improvement of drug solubility as well as bioavailability potentiated orodispersible films as a promising drug delivery for loratadine.

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Funding

This research is funded by PHENIKAA University under grant number 2-01.2020.01

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Authors and Affiliations

  1. University of Medicine and Pharmacy, Vietnam National University, Hanoi, Y1 Building, 144 Xuan Thuy, Cau Giay, Hanoi, Vietnam

    Khanh Van Nguyen & Huyen Thi Nguyen

  2. Institute of Physics, Vietnam Academy of Science and Technology (VAST), Hanoi, 100000, Viet Nam

    Lien Ha Thi Nghiem

  3. Department of Pathophysiology, Vietnam Military Medical University, 160 Phung Hung, Phuc La, Ha Dong, Hanoi, 100000, Vietnam

    Mao Van Can

  4. Faculty of Pharmacy, PHENIKAA University, Yen Nghia, Ha Dong, Hanoi, 12116, Vietnam

    Tuan Hiep Tran

Authors
  1. Khanh Van Nguyen
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  2. Huyen Thi Nguyen
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  3. Lien Ha Thi Nghiem
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  4. Mao Van Can
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  5. Tuan Hiep Tran
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Contributions

Khanh Van Nguyen: design of the work; acquisition, analysis, and interpretation of data for the work

Huyen Thi Nguyen: acquisition, analysis, and interpretation of data for the work

Lien Thi Ha Nghiem: acquisition, analysis, and interpretation of data for the work

Mao Van Can: acquisition, analysis, and interpretation of data for the work

Tuan Hiep Tran: design of the work; analysis, interpretation of data for the work; drafting the work

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Correspondence to Tuan Hiep Tran.

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Van Nguyen, K., Nguyen, H.T., Nghiem, L.H.T. et al. Nanosized-Loratadine Embedded Orodispersible Films for Enhanced Bioavailability: Scalable Preparations and Characterizations. AAPS PharmSciTech 23, 78 (2022). https://doi.org/10.1208/s12249-022-02230-y

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  • DOI: https://doi.org/10.1208/s12249-022-02230-y

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