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<p>Morphine is an effective and widely used drug in the relief of acute and chronic pain, but its half-life and low bioavailability pose limitations and prevent achieving an appropriate level of morphine in plasma. Therefore, for greater effectiveness and better pain control, it needs to be taken several times a day. Our aim in this study was to overcome these limitations by loading morphine–nanoparticles (morphine–NPs) into polymeric adhesive mucus films and synthesizing an effective buccal drug delivery system. To make these polymer nanoparticles (NPs), first chitosan solution of 1% was added to the surfactant solution containing Polysorbate 80 and benzalkonium chloride, and then morphine was slowly added drop by drop to the solution. To strengthen the polymer bonds, an amount of 0.125 mg of tripolyphosphate (TPP) was added, and then, the resulting NPs were encapsulated by Eudragit FS 30D polymer. Finally, NPs were loaded on the polymer film obtained from combining three polymers: hydroxypropyl methylcellulose (HPMC), carbopol, and ethyl cellulose (EC). After evaluating the NPs by electron microscopy, it was found that the dimensions of the NPs are between 25 and 30 nm. The drug loading percentage in the NPs was 57%, and no cytotoxicity effect on the fibroblast cells was observed. Polymer films illustrated suitable release profiles that were dependent on the amount of EC and followed the Higuchi model. These findings revealed that our formulation can release morphine continuously for up to 6 h, and therefore, its oral administration in future studies could be a promising approach for drugs that have a short half-life and undergo first-pass metabolism.</p>

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Development of Morphine-Loaded Polymer Nanoparticle Oral Films and Their In Vitro Impact on Fibroblast Cells

  • 期刊论文

  • 发表日期：

    2025年7月14日

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  • Mohammad Javad Hoseinifar,
  • Faranak Aghaz,
  • Iman Godazi Langroudi,
  • Fereshteh Bagheri,
  • Reza Tahvilian

摘要

Morphine is an effective and widely used drug in the relief of acute and chronic pain, but its half-life and low bioavailability pose limitations and prevent achieving an appropriate level of morphine in plasma. Therefore, for greater effectiveness and better pain control, it needs to be taken several times a day. Our aim in this study was to overcome these limitations by loading morphine–nanoparticles (morphine–NPs) into polymeric adhesive mucus films and synthesizing an effective buccal drug delivery system. To make these polymer nanoparticles (NPs), first chitosan solution of 1% was added to the surfactant solution containing Polysorbate 80 and benzalkonium chloride, and then morphine was slowly added drop by drop to the solution. To strengthen the polymer bonds, an amount of 0.125 mg of tripolyphosphate (TPP) was added, and then, the resulting NPs were encapsulated by Eudragit FS 30D polymer. Finally, NPs were loaded on the polymer film obtained from combining three polymers: hydroxypropyl methylcellulose (HPMC), carbopol, and ethyl cellulose (EC). After evaluating the NPs by electron microscopy, it was found that the dimensions of the NPs are between 25 and 30 nm. The drug loading percentage in the NPs was 57%, and no cytotoxicity effect on the fibroblast cells was observed. Polymer films illustrated suitable release profiles that were dependent on the amount of EC and followed the Higuchi model. These findings revealed that our formulation can release morphine continuously for up to 6 h, and therefore, its oral administration in future studies could be a promising approach for drugs that have a short half-life and undergo first-pass metabolism.