Main Article Content
Formulation and characterization of lomustine-loaded solusomes nanovesicles
Abstract
Purpose: To design and characterize Lomustine (LOM) nanoparticles encapsulated by solusomes to enhance the physicochemical properties.
Methods: Thin-film hydration technique was employed to prepare LOM-loaded solusomes. Sixteen formulations were produced and evaluated for entrapment efficiency, particle size, polydispersity index, and <i>in vitro</i> drug release. Then, the optimum formula was chosen for further evaluation using differential scanning calorimetry (DSC), transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FTIR) and using a sheep nasal membrane to perform <i>ex vivo</i> drug permeation studies.
Results: Solusomes-loaded LOM F4 (lomustine 10 mg, cholesterol 10 mg, phosphatidylcholine 98 % 50 mg and Soluplus® 25 mg) was selected as an ideal formula since it has the optimum characteristics: high entrapment efficiency 99.76 ± 1.64 %, a small particle size 90.4 ± 9.98 nm, and a stable zeta potential - 32.16 mV. Additionally, it demonstrated significantly (p < 0.05) faster <i>in vitro</i> drug release 93 % after 120 minutes and a higher <i>ex vivo</i> permeation coefficient compared to the LOM suspension. Finally, encapsulating LOM in a more soluble and amorphous state facilitates rapid absorption for brain tumour treatment.
Conclusion: The LOM-solusomes could be considered a new approach to enhance the solubility and permeability of the drug and deliver optimum therapeutic benefit.



