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<p>A promising strategy to overcome the problems in treatment with pharmaceutical active ingredients involves the development of suitable drug carrier systems using nanoparticles (NPs). Tetrahydrocurcumin (THC) is an active metabolite of curcumin, which comes under BCS Class II due to its less solubility. A novel, integrated system known as lipid-polymer hybrid nanoparticles (LPH-NPs) has been introduced in an effort to mitigate limitations associated with unpredictable physicochemical properties. The particle size, polydispersive index (PDI), zeta potential, encapsulation efficiency, and morphology were characterized for the prepared formulation. In vitro drug release, release kinetics, and stability of the prepared LPH-NPs were evaluated. The particle size of all the prepared 27 LPH-NPs formulations (F) was found to be in the range of 98.06 to 158&#xa0;nm. The formulation F14 has shown the maximum encapsulation efficiency (80.3%) with less particle size (129.8&#xa0;nm) and PDI (0.085). Also, the zeta potential was found to be −36.4, and it confirms the stability of the formulation. The transmission electron microscope (TEM) and atomic force microscope (AFM) morphological images of formulation F14 showed spherical, smooth-surfaced, and uniformly sized particles. The formulations F13, F14, F15, F16, F17, and F18 showed maximum drug release of 93.1, 95.1, 91.6, 86.2, 89.7, and 87.3%, respectively, when compared to pure drug THC. The drug release from the formulation and kinetic results was clearly indicative of sustained release of THC. The obtained drug release results indicate that the solubility of THC is improved with LPH-NPs. Hence, the developed formulation would enable the increased oral bioavailability of THC.</p>

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Lipid-Polymer Hybrid Nanoparticles for Solubility Enhancement of Tetrahydrocurcumin in a Novel Discriminative Dissolution Medium

  • 期刊论文

  • 发表日期：

    2025年9月15日

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  • Habibur Rahman,
  • Lakshman Prathap,
  • Hariprasad Ranganathan,
  • Telny Thomas,
  • Dinesh Babu,
  • Sivaselvakumar Muthusamy,
  • Arjunan Karuppaiah

摘要

A promising strategy to overcome the problems in treatment with pharmaceutical active ingredients involves the development of suitable drug carrier systems using nanoparticles (NPs). Tetrahydrocurcumin (THC) is an active metabolite of curcumin, which comes under BCS Class II due to its less solubility. A novel, integrated system known as lipid-polymer hybrid nanoparticles (LPH-NPs) has been introduced in an effort to mitigate limitations associated with unpredictable physicochemical properties. The particle size, polydispersive index (PDI), zeta potential, encapsulation efficiency, and morphology were characterized for the prepared formulation. In vitro drug release, release kinetics, and stability of the prepared LPH-NPs were evaluated. The particle size of all the prepared 27 LPH-NPs formulations (F) was found to be in the range of 98.06 to 158 nm. The formulation F14 has shown the maximum encapsulation efficiency (80.3%) with less particle size (129.8 nm) and PDI (0.085). Also, the zeta potential was found to be −36.4, and it confirms the stability of the formulation. The transmission electron microscope (TEM) and atomic force microscope (AFM) morphological images of formulation F14 showed spherical, smooth-surfaced, and uniformly sized particles. The formulations F13, F14, F15, F16, F17, and F18 showed maximum drug release of 93.1, 95.1, 91.6, 86.2, 89.7, and 87.3%, respectively, when compared to pure drug THC. The drug release from the formulation and kinetic results was clearly indicative of sustained release of THC. The obtained drug release results indicate that the solubility of THC is improved with LPH-NPs. Hence, the developed formulation would enable the increased oral bioavailability of THC.