| dc.description.abstract | This study investigated the drug loading (DL) and encapsulation efficiency (EE) of antimalarial drugs with varying hydrophobicity in glycerol monooleate-based cubosomes stabilized with dα-tocopherol polyethylene glycol 1000 succinate (TPGS). The antimalarial drugs studied were proguanil, DSM265, and lumefantrine, with log P values of 2.21, 5.95, and 9.15, respectively. The objective was to assess how their hydrophobicity influences their encapsulation within cubosomes and to optimize the formulation for improved drug delivery. The study revealed that the drug’s hydrophobicity significantly affects DL and EE Lumefantrine, the most lipophilic drug, exhibited the highest DL at 5.3% and EE at 46%. DSM265 had a DL of 0.31% and EE of 1.7%. Proguanil, the least lipophilic drug, showed the lowest DL at 0.13% and EE at 0.59%. Furthermore, increasing the amount of TPGS enhanced the DL of lumefantrine and DSM265. This enhancement can be attributed to the improved stabilization of the drug-loaded cubosomes and the prevention of precipitation. Measurements of particle size and polydispersity index indicated that drug encapsulation did not significantly alter the size of the cubosomes, except for lumefantrine, which caused a slight increase in particle size. Zeta potential measurements showed that the presence of drugs did not alter the electric double layers, except for proguanil, which resulted in a more negative zeta potential. The study concluded that a drug's lipophilicity, as indicated by its log P value, is a critical factor in facilitating drug encapsulation in cubosomes and should be one of the key physicochemical properties to consider when optimizing DL. However, other physicochemical properties should also be considered, such as solubility, which is crucial in optimizing cubosomal drug formulations. This study enhances our understanding of cubosome-based drug delivery systems and highlights the potential of using such systems for the effective delivery of antimalarial drugs. | |
