DEVELOPMENT AND CHARACTERIZATION OF VERSATILE NANOSTRUCTURED LIPID CARRIERS FOR BUTAMBEN ADMINISTRATION.

Vol 2, 2024 - 315647
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Abstract

Butamben is an anesthetic drug (Class II) with a log P of 2.87. Considered a 'brick dust' drug (poorly soluble in water and lipids), which makes the development of nanostructured lipid carriers (NLC) a challenge since it is not soluble in the NLC lipid core, previous studies were carried out to develop a NLC core consisting of lipophilic solid lipid liquid, medium polarity lipid and a hydrophilic solvent aiming at increasing the solubility of butamben in the system. The lipid core proportions were determined by analyzing the miscibility of the excipients by Raman mapping and chemometric data processing. Two surfactants (Crodasol™ HS HP and Synperonic™ PE/F68) were evaluated, and due to its chemical structure, Synperonic™ PE/F68 was shown to be superior. Therefore, this study aimed at characterizing the optimized NLC and evaluating its stability in aqueous media. The NLCs were prepared using the emulsification-ultrasonication technique with Crodamol CP™, SR™ Lauryl Lactate, SR™ DMI, and Synperonic™ PE/F68, and optimized by factorial design, where particle size (nm), polydispersity index (PDI), and zeta potential (mV) were evaluated as Critical Quality Attributes (CQAs). The NLCs selected after optimization were then characterized by measurements of size, PDI and zeta potential, NTA, encapsulation efficiency, transmission electron microscopy (TEM), differential scanning calorimetry (DSC), infrared spectroscopy (ATR-FTIR) and X-ray diffraction (PXRD). The optimized NLCs successfully incorporated butamben, resulting in particles with an appropriate size (below 166 nm) and polydispersity (0.16), and exhibited high encapsulation efficiency (98%). The addition of Super Refined™ DMI to the lipid core favored desired NLC features, including particle size, PDI, and zeta potential, showing that it remained in the lipid core after dilution, in addition to being crucial for the solubilization of BTB in the NLC core. Based on the DSC results, it is evident that NLC presented a decrease in fusion enthalpy, reducing lipid crystallinity, thus minimizing drug expulsion during the storage period. This same decrease in lipid crystallinity was found in the PXRD results. In this way, it was possible to obtain formulations with the desired characteristics for the administration of butamben and possible other ‘brick dust’ type drugs.

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Institutions
  • 1 State University of Campinas
  • 2 State University of Campinas (UNICAMP)
  • 3 Croda Brazil
Track
  • 3. Drug design and delivery
Keywords
Nanostructured Lipid Carriers (NLCs)
Butamben
Optimization