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. 2023 Sep 29;13(41):28590-28601.
doi: 10.1039/d3ra04844f. eCollection 2023 Sep 26.

Molecular insights into the aggregation and solubilizing behavior of biocompatible amphiphiles Gelucire® 48/16 and Tetronics® 1304 in aqueous media

Deep Bhalani  1 , Hiral Kakkad  1 , Jignasa Modh  1 , Debes Ray  2   3 , Vinod K Aswal  2 , Sadafara A Pillai  1
Affiliations

Molecular insights into the aggregation and solubilizing behavior of biocompatible amphiphiles Gelucire® 48/16 and Tetronics® 1304 in aqueous media

Deep Bhalani et al. RSC Adv. .

Abstract

A comparative analysis of the micellar and solubilizing properties of two polyethylene glycol (PEG)-based amphiphilic biocompatible excipients: Gelucire® 48/16 (Ge 48/16) and Tetronics® 1304 (T1304), in the presence and absence of salt, was conducted. As there is a dearth of research in this area, the study aims to shed light on the behavior of these two nonionic surfactants and their potential as nanocarriers for solubilizing pharmaceuticals. Various techniques such as cloud point (CP), dynamic light scattering (DLS), small-angle neutron scattering (SANS), Fourier transform infrared spectroscopy (FT-IR), UV spectrophotometry, and high-performance liquid chromatography (HPLC) were employed. The solubility of quercetin (QCT), a flavonoid with anti-inflammatory, antioxidant, and anti-cancer properties, was evaluated and the interaction between QCT and the micellar system was examined. The analysis revealed the occurrence of strong interactions between QCT and surfactant molecules, resulting in enhanced solubility. It was observed that the micellar size and solubilizing ability were significantly improved in the presence of salt, while the CP decreased. Ge 48/16 exhibited superior performance, with a remarkable increase in the solubility of QCT in the presence of salt, suggesting its potential as an effective nanocarrier for a range of pharmaceutics, and yielding better therapeutic outcomes.

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Conflict of interest statement

There are no conflicts to declare.

Figures

Fig. 1
Fig. 1. Chemical structure of Gelucire® 48/16 and T1304.
Fig. 2
Fig. 2. Pictorial representation of clouding phenomenon observed in 1% w/v aqueous solution of (a) Ge 48/16 and (b) T1304 as a function of salt concentration.
Fig. 3
Fig. 3. (a) Apparent hydrodynamic diameter of 1% w/v aqueous solution of (a) Ge 48/16 and (b) T1304.
Fig. 4
Fig. 4. SANS curves for 1% w/v solutions of (a) Ge 48/16 and (b) T1304 in the presence and absence of salt at 30 °C.
Fig. 5
Fig. 5. UV-vis absorbance spectra of QCT in 1% w/v aqueous solutions of (a) Ge 48/16 and (b) T1304.
Fig. 6
Fig. 6. FT-IR spectral profile illustrating the favourable interaction of QCT with Ge 48/16.
Fig. 7
Fig. 7. Drug loading amount/solubility (mg mL−1) of QCT in 1% w/v aqueous solutions of Ge 48/16 and T1304 as a function of salt concentration.
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