<p>Compatibility studies between the plant-derived bioactive compound Quercetin (QUE) and selected lipids were conducted to assess their suitability for developing QUE loaded solid lipid nanoparticles (QSLNs). Quantification of QUE was performed by a developed and validated Reverse Phase High Performance Liquid Chromatography (RP-HPLC) technique. Based on lipid screening and drug-excipient compatibility (DEC) studies, Stearic Acid (SA), Soy Lecithin (Soy Lec), and Glyceryl Monostearate (GMS) were selected as optimal lipids. QSLNs were formulated using the microemulsion cooling technique and characterized by spectral and thermal analysis, photostability, particle size, zeta potential, and % entrapment efficiency. The selected optimal formulations (SF2 and SF5) were subjected to physical stability studies according to ICH Q1A (R2) guidelines under 5 ± 3° C and room temperature, 25 ± 2&#xa0;°C/60 ± 5% RH for a period of 3&#xa0;months. RP-HPLC confirmed the purity of QUE with a peak at 6.3&#xa0;min. Lipid screening showed SA as the most suitable lipid, with the highest solubility (18.33&#xa0;mg/g) and partition coefficient (0.703). DEC, spectral and thermal analysis confirmed stable incorporation of QUE with protection against UV degradation. The particle size of QSLNs ranged from 198.32 to 331.6&#xa0;nm, with S-F5 exhibiting the smallest size (198.32 ± 4.89&#xa0;nm) and low polydispersity index (0.23 ± 0.02), indicating the uniformity. The developed QSLNs exhibited stable formulations with efficient drug encapsulation and UV protection, demonstrating promising potential to enhance QUE bioavailability and stability.</p> Graphical Abstract <p></p>

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Compatibility Study of Phyto Bioactive Compound with Lipid Excipients for the Development of Solid Lipid Nanoparticles

  • Pavithra Kothapalli,
  • Manimaran Vasanthan

摘要

Compatibility studies between the plant-derived bioactive compound Quercetin (QUE) and selected lipids were conducted to assess their suitability for developing QUE loaded solid lipid nanoparticles (QSLNs). Quantification of QUE was performed by a developed and validated Reverse Phase High Performance Liquid Chromatography (RP-HPLC) technique. Based on lipid screening and drug-excipient compatibility (DEC) studies, Stearic Acid (SA), Soy Lecithin (Soy Lec), and Glyceryl Monostearate (GMS) were selected as optimal lipids. QSLNs were formulated using the microemulsion cooling technique and characterized by spectral and thermal analysis, photostability, particle size, zeta potential, and % entrapment efficiency. The selected optimal formulations (SF2 and SF5) were subjected to physical stability studies according to ICH Q1A (R2) guidelines under 5 ± 3° C and room temperature, 25 ± 2 °C/60 ± 5% RH for a period of 3 months. RP-HPLC confirmed the purity of QUE with a peak at 6.3 min. Lipid screening showed SA as the most suitable lipid, with the highest solubility (18.33 mg/g) and partition coefficient (0.703). DEC, spectral and thermal analysis confirmed stable incorporation of QUE with protection against UV degradation. The particle size of QSLNs ranged from 198.32 to 331.6 nm, with S-F5 exhibiting the smallest size (198.32 ± 4.89 nm) and low polydispersity index (0.23 ± 0.02), indicating the uniformity. The developed QSLNs exhibited stable formulations with efficient drug encapsulation and UV protection, demonstrating promising potential to enhance QUE bioavailability and stability.

Graphical Abstract