| Full text | |
| Author(s): |
Mitsutake, Hery
;
da Silva, Gustavo H. Rodrigues
;
de Paula, Eneida
;
Breitkreitz, Marcia C.
Total Authors: 4
|
| Document type: | Journal article |
| Source: | Journal of Pharmaceutical and Biomedical Analysis; v. 235, p. 9-pg., 2023-10-25. |
| Abstract | |
Butamben is a topical local anesthetic which formulation in lipid-based drug delivery systems (DDS) is challenging due to its affinity for hydrophilic excipients. This means that a medium polarity excipient is preferred for the development of a stable nanostructured lipid carrier (NLC) formulation. In turn, in NLC, the type and number of excipients will determine the active pharmaceutical ingredient (API) solubility and the maximum drug upload. To solve this dilemma and get the best formulation, a throughout screening study to evaluate API solubilization in different excipients was carried out. Subsequently, excipients with different solubilization capacities were selected for microscopic evaluation by Raman mapping, and in turn analysis of the distributional homogeneity index (DHI) and standard deviation of the histograms allowed solving the posed question. Design of experiments (DoE) was employed to understand better the interactions between the excipients; linear and higher-order models were obtained with R2 above of 0.8824. Even though DHI is a good parameter to be used as response, an API concentration higher than 30% (w/w) provided a homogeneous surface in case of good miscibility and, in this case, this parameter needs to be employed with an inspection and/or evaluation of other parameters. A curve of concentration vs. mean scores of images proved to be an alternative to identify the saturation/limit of linear range. (AU) | |
| FAPESP's process: | 18/22975-7 - Evaluation of the miscibility and structural modifications of lipids for the development of nanostructured lipid carriers and hydrogels for anesthetic using Raman imaging associated with chemometric methods |
| Grantee: | Hery Mitsutake |
| Support Opportunities: | Scholarships in Brazil - Post-Doctoral |