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<p>The oral bioavailability is challenged by the intrinsic low solubility of some drugs, such as nimodipine (NMD). Lipid-based formulations (LBFs), comprising drug and lipid carriers, can generate supersaturation, thus increasing lipophilic drugs' solubility and dissolution rate. As a result, they can provide superior outcomes for the patient with a lower dose. The choice of excipients is essential to stabilize and prolong supersaturation in the gastrointestinal tract. In this study, different compounds, such as fatty acids (FAs) and surfactants were pre-selected to verify if they can inhibit precipitation during the supersaturated state of LBFs containing NMD. Excipient selection, miscibility and compatibility studies were performed through theoretical and practical methods. Theoretical solubility parameter calculations demonstrated that all pre-selected excipients exhibited minimal miscibility potential with NMD. From a practical perspective, the interactions between these excipients and NMD were evaluated using DSC and revealed the non-ionic surfactant derived from fatty acids, Gelucire® 48/16 (GLC), as the most promising excipients for the development of LBFs. LBFs prepared with different proportions of drug, GLC and an adsorbent exhibited lower crystallinity and higher thermal stability compared to the isolated drug. Through dissolution studies under supersaturation conditions, one of the LBF formulations, in particular, showed an area under the curve approximately 66% larger than NMD, in biorelevant medium. Overall, the LBFs obtained with the lipophilic carrier GLC appear as a promising and innovative system with the aim of improving the biopharmaceutical properties of NMD.</p>

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Evaluating component preformulation strategies for supersaturating lipid-based systems: a combined theoretical and experimental study with nimodipine

  • 期刊论文

  • 发表日期：

    2026年3月6日

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  • Tatyane Martins Marcos,
  • Giovana Carolina Bazzo,
  • Maria Terezinha França,
  • Hellen Karine Stulzer

摘要

The oral bioavailability is challenged by the intrinsic low solubility of some drugs, such as nimodipine (NMD). Lipid-based formulations (LBFs), comprising drug and lipid carriers, can generate supersaturation, thus increasing lipophilic drugs' solubility and dissolution rate. As a result, they can provide superior outcomes for the patient with a lower dose. The choice of excipients is essential to stabilize and prolong supersaturation in the gastrointestinal tract. In this study, different compounds, such as fatty acids (FAs) and surfactants were pre-selected to verify if they can inhibit precipitation during the supersaturated state of LBFs containing NMD. Excipient selection, miscibility and compatibility studies were performed through theoretical and practical methods. Theoretical solubility parameter calculations demonstrated that all pre-selected excipients exhibited minimal miscibility potential with NMD. From a practical perspective, the interactions between these excipients and NMD were evaluated using DSC and revealed the non-ionic surfactant derived from fatty acids, Gelucire® 48/16 (GLC), as the most promising excipients for the development of LBFs. LBFs prepared with different proportions of drug, GLC and an adsorbent exhibited lower crystallinity and higher thermal stability compared to the isolated drug. Through dissolution studies under supersaturation conditions, one of the LBF formulations, in particular, showed an area under the curve approximately 66% larger than NMD, in biorelevant medium. Overall, the LBFs obtained with the lipophilic carrier GLC appear as a promising and innovative system with the aim of improving the biopharmaceutical properties of NMD.