Scholarlink

<p>Methylphenidate (MPH) undergoes extensive first-pass metabolism, primarily via de-esterification leading to inter-individual variability in systemic bioavailability, which can range from 11 to 53%. The short half-life of around 2–3&#xa0;h necessitates multiple daily dosing or the use of extended-release formulations. To increase absolute oral bioavailability, of Methylphenidate (MPH), the current study aims to develop MPH loaded lipid–polymer hybrid nanoparticles (LPHNP). The single-step nano-precipitation self-assembly process was used to develop the formulation, followed by high-speed homogenization and ultra sonication. The formulation of LPHNPs was optimized utilizing the Box-Behnken Design approach. The optimized formulation (LPHNP) was freeze-dried by using cryoprotectant (mannitol). The optimized LPHNP formulation showed high entrapment efficiency with desirable particle size (PS) 214 ± 7.8&#xa0;nm, zeta potential (ZP) −30.87 ± 3.62&#xa0;mV, and poly dispersity index 0.21 ± 0.028 (PDI). The pharmacokinetic study of the optimized lyophilized LPHNP in albino rat revealed the improvement in oral bioavailability nearly two times in comparison to that of aqueous suspension of MPH. The lyophilized LPHNP has the capability to encapsulate MPH into the hybrid nanoparticles with improved stability and oral bioavailability.</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Methylphenidate HCl Lyophilized Lipid–Polymer Hybrid Nanoparticles: Formulation and Characterization

  • 期刊论文

  • 发表日期：

    2025年7月13日

查看全文
  • Sashank Sekhar Hota,
  • Goutam Kumar Jena,
  • Jammula Sruti,
  • Ch. Niranjan Patra

摘要

Methylphenidate (MPH) undergoes extensive first-pass metabolism, primarily via de-esterification leading to inter-individual variability in systemic bioavailability, which can range from 11 to 53%. The short half-life of around 2–3 h necessitates multiple daily dosing or the use of extended-release formulations. To increase absolute oral bioavailability, of Methylphenidate (MPH), the current study aims to develop MPH loaded lipid–polymer hybrid nanoparticles (LPHNP). The single-step nano-precipitation self-assembly process was used to develop the formulation, followed by high-speed homogenization and ultra sonication. The formulation of LPHNPs was optimized utilizing the Box-Behnken Design approach. The optimized formulation (LPHNP) was freeze-dried by using cryoprotectant (mannitol). The optimized LPHNP formulation showed high entrapment efficiency with desirable particle size (PS) 214 ± 7.8 nm, zeta potential (ZP) −30.87 ± 3.62 mV, and poly dispersity index 0.21 ± 0.028 (PDI). The pharmacokinetic study of the optimized lyophilized LPHNP in albino rat revealed the improvement in oral bioavailability nearly two times in comparison to that of aqueous suspension of MPH. The lyophilized LPHNP has the capability to encapsulate MPH into the hybrid nanoparticles with improved stability and oral bioavailability.