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<p>This study focuses on the development, characterization, and evaluation of a mucoadhesive, thermosensitive in situ nasal gel formulation of artemether for enhanced intranasal delivery. The aim is to improve drug solubility, stability, and bioavailability for effective antimalarial treatment. Artemether was encapsulated in mesoporous silica particles and incorporated into a nasal gel formulation. The optimized batch (F1) contained 100% w/v Phytantriol and 20% w/v Poloxamer 407. Various analyses, including FTIR, DSC, XRD, and solubility studies, were conducted. The formulation’s gelling properties, mucoadhesive strength, viscosity, pH, and stability were evaluated. Ex vivo permeation and in vitro antimalarial activity were assessed. The optimized formulation F1 demonstrated a gelling temperature of 29.67 ± 0.32&#xa0;°C, a mucoadhesive strength of 6572 ± 11.32 dyne/cm<sup>2</sup>, and a viscosity of 2665.3 ± 13.65 cps. Stability studies showed consistent performance over 6&#xa0;months at 40 ± 2&#xa0;°C and 75 ± 5% RH. The ex vivo permeation study revealed significant drug permeation, with 95.78% at 10&#xa0;h. In vitro antimalarial activity showed 60.41% suppression at 40&#xa0;mg/mL, increasing to 94.11% at 120&#xa0;mg/mL. The IC<sub>50</sub> and IC90 values for the in situ nasal gel were 11.00 ± 0.67&#xa0;mg/mL and 107.07 ± 2.42&#xa0;mg/mL, respectively. The ARM-MSPs loaded in situ nasal gel (F1) is a promising formulation for intranasal delivery of artemether, providing enhanced solubility, stability, and effective antimalarial activity, potentially improving patient compliance and therapeutic outcomes.</p> Graphical Abstract <p></p>

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Mucoadhesive, Thermosensitive Mesoporous Silica Loaded In Situ Nasal Gel for Intranasal Delivery of Artemether: Formulation, Optimization, and In Vitro Antimalarial Activity

  • 期刊论文

  • 发表日期：

    2025年7月7日

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  • Mahesh Hari Kolhe,
  • Mansi Bhagwan Chitnis,
  • Payal Sopan Gawali,
  • Manjusha Pandharinath Mhaske,
  • Pratibha Sudhakar Bhalerao,
  • Rohit Jaysing Bhor

摘要

This study focuses on the development, characterization, and evaluation of a mucoadhesive, thermosensitive in situ nasal gel formulation of artemether for enhanced intranasal delivery. The aim is to improve drug solubility, stability, and bioavailability for effective antimalarial treatment. Artemether was encapsulated in mesoporous silica particles and incorporated into a nasal gel formulation. The optimized batch (F1) contained 100% w/v Phytantriol and 20% w/v Poloxamer 407. Various analyses, including FTIR, DSC, XRD, and solubility studies, were conducted. The formulation’s gelling properties, mucoadhesive strength, viscosity, pH, and stability were evaluated. Ex vivo permeation and in vitro antimalarial activity were assessed. The optimized formulation F1 demonstrated a gelling temperature of 29.67 ± 0.32 °C, a mucoadhesive strength of 6572 ± 11.32 dyne/cm2, and a viscosity of 2665.3 ± 13.65 cps. Stability studies showed consistent performance over 6 months at 40 ± 2 °C and 75 ± 5% RH. The ex vivo permeation study revealed significant drug permeation, with 95.78% at 10 h. In vitro antimalarial activity showed 60.41% suppression at 40 mg/mL, increasing to 94.11% at 120 mg/mL. The IC50 and IC90 values for the in situ nasal gel were 11.00 ± 0.67 mg/mL and 107.07 ± 2.42 mg/mL, respectively. The ARM-MSPs loaded in situ nasal gel (F1) is a promising formulation for intranasal delivery of artemether, providing enhanced solubility, stability, and effective antimalarial activity, potentially improving patient compliance and therapeutic outcomes.

Graphical Abstract