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<p>Nanomaterials are an efficient approach for augmenting bioavailability by following uptake mechanisms involving the lymphatic efflux system via chylomicron routes. This study used this enhancement approach for two drugs using Nanostructured Lipid Carriers (NLCs) for comorbid hypertension (HTN) and diabetes mellitus (DM). Box-Behnken design-based optimization with the Design-Expert software was utilized by varying the weight ratios of sitagliptin (SITA), lisinopril (LIS), surfactant, and solid/liquid lipid proportion employing hot melt homogenization method. The size along with the size distribution of the developed NLCs was assessed using the dynamic light scattering (DLS) method while the morphological analysis of the particle surface was performed using scanning electron microscopy (SEM). Solid-state characterization was evaluated using Fourier transform infrared spectroscopy (FT-IR) and x-ray diffraction (XRD). Moreover, the dialysis bag diffusion method was employed to determine the release behavior of the optimized formulation at pH 1.2, 6.8, and 7.4 compared to the pure drug solutions of LIS and SITA. The optimized NLCs co-loaded with SITA and LIS (NSL-20) demonstrated particle size of 162&#xa0;nm, zeta value of − 25.4&#xa0;mV, and polydispersity value of 0.274, with an entrapment efficiency (EE) of 97% and 46% for SITA and LIS, respectively. The release profile depicted the prolonged release pattern for both drugs after 24&#xa0;h in comparison to a pure drug solution. The bioavailability of both drugs was enhanced, which was evident from the in vivo pharmacokinetic study. Overall, the study provides valuable insights into the use of NSL for the efficient delivery of low-permeability BCS class III drugs.</p>

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Dual-Action Nanocarriers for the Management of Diabetes and Hypertension: A Sitagliptin-Lisinopril Co-delivery Approach

  • 期刊论文

  • 发表日期：

    2025年3月15日

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  • Ahmad Abdur Rahman,
  • Abeer Tariq,
  • Muhammad Tayyab,
  • Muhammad Usman,
  • Muhammad Akhtar,
  • Adnan Nadir,
  • Ahmad Khan

摘要

Nanomaterials are an efficient approach for augmenting bioavailability by following uptake mechanisms involving the lymphatic efflux system via chylomicron routes. This study used this enhancement approach for two drugs using Nanostructured Lipid Carriers (NLCs) for comorbid hypertension (HTN) and diabetes mellitus (DM). Box-Behnken design-based optimization with the Design-Expert software was utilized by varying the weight ratios of sitagliptin (SITA), lisinopril (LIS), surfactant, and solid/liquid lipid proportion employing hot melt homogenization method. The size along with the size distribution of the developed NLCs was assessed using the dynamic light scattering (DLS) method while the morphological analysis of the particle surface was performed using scanning electron microscopy (SEM). Solid-state characterization was evaluated using Fourier transform infrared spectroscopy (FT-IR) and x-ray diffraction (XRD). Moreover, the dialysis bag diffusion method was employed to determine the release behavior of the optimized formulation at pH 1.2, 6.8, and 7.4 compared to the pure drug solutions of LIS and SITA. The optimized NLCs co-loaded with SITA and LIS (NSL-20) demonstrated particle size of 162 nm, zeta value of − 25.4 mV, and polydispersity value of 0.274, with an entrapment efficiency (EE) of 97% and 46% for SITA and LIS, respectively. The release profile depicted the prolonged release pattern for both drugs after 24 h in comparison to a pure drug solution. The bioavailability of both drugs was enhanced, which was evident from the in vivo pharmacokinetic study. Overall, the study provides valuable insights into the use of NSL for the efficient delivery of low-permeability BCS class III drugs.