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Orodispersible film incorporating nanoparticulate loratadine for an enhanced oral bioavailability

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Abstract

Purpose

Loratadine (LOR), a commonly prescribed antihistamine, has low water solubility but high permeability. In this study, an orodispersible film incorporating the nanoparticulate loratadine was prepared to enhance the oral bioavailability of a poorly water-soluble drug.

Methods

Nanoparticulate loratadine was formulated using the antisolvent precipitation method and optimized by a single-factor design based on the particle size and polydispersity index. The optimal formulation was spray-dried and characterized by powder X-ray diffraction and differential scanning calorimetry. Nanoparticulate loratadine was loaded into an orodispersible film using a solvent casting method.

Results

In the dissolution tests, the nanoparticulate loratadine-loaded orodispersible film exhibited a 6.5-fold higher dissolution rate than the pure loratadine-loaded film and a similar dissolution rate compared to the commercialized orodispersible tablet, Loratadine SPM. In pharmacokinetic studies conducted on rats, the maximum concentration (Cmax) and area under the curve of the plasma concentration–time profile from 0 to 24 h (AUC0-24 h) of the nanoparticulate loratadine-loaded orodispersible film significantly increased 1.8-fold and 5.8-fold, respectively. The elimination half-life (t1//2) increased 5.1-fold compared to the loratadine-loaded counterpart.

Conclusion

These results suggest the potential of orodispersible films to improve the oral bioavailability of poorly water-soluble drugs and promote compliance in pediatric and geriatric patients.

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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, Thu Kim Dang & Linh Thi Dieu Vu

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

    Nhan Thi Ha & Tuan Hiep Tran

  3. Quang Binh Pharmaceutical Joint-Stock Company, Dong Hoi, Quangbinh, 510000, Vietnam

    Hieu Duy Truong

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  1. Khanh Van Nguyen
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  2. Thu Kim Dang
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Correspondence to Tuan Hiep Tran.

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All authors (Khanh Van Nguyen, Thu Kim Dang, Linh Thi Dieu Vu, Nhan Thi Ha, Hieu Duy Truong, and Tuan Hiep Tran) declare that they have no conflict of interest.

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Animal studies were performed after receiving approval from the Animal Ethics Experimentation Committee of Vietnam Military Medical University No. LORA.01 (Hanoi, Vietnam).

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Van Nguyen, K., Dang, T.K., Vu, L.T.D. et al. Orodispersible film incorporating nanoparticulate loratadine for an enhanced oral bioavailability. J. Pharm. Investig. 53, 417–426 (2023). https://doi.org/10.1007/s40005-023-00613-2

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