Characterizing the Drug-Release Enhancement Effect of Surfactants on Megestrol-Acetate-Loaded Granules

Abstract

In this study, the effect of Cremophor® RH 40 (CR 40) classic micelles and Soluplus® (SP) polymeric micelles were investigated on a novel granule-type drug-delivery system containing megestrolacetate (MGA). Using a risk assessment-based approach on the formulation via melt technology resulted in the formation of these granules, presented as the dosage, with proper particle size and flow characteristics. Due to the application of a eutectic carrier base composition, gentle process conditions were reached, retaining the crystalline structure of the carrier system and allowing for the proper distribution of MGA in the granules. The increased water solubility (0.111 mg/mL to 2.154 mg/mL), and the decreased nano particle size (102.27 nm) with uniform distribution (polydispersity index of 0.259) and colloid stability (zeta potential of −12.99 mV) resulted in SP polymeric micelles prevailing over CR 40 micelles in this gastric dissolution study, performed in biorelevant fasted and fed state drug-release media. Mathematical characterization and kinetic model fitting supported the fast drug-release mechanism of polymeric micelles over micelles. The value-added polymeric micelle-containing formulation developed can be successfully administered perorally and the enhanced drug release offers the possibility of greater drug absorption in the gastrointestinal tract.

Development of Computational In Silico Model for Nano Lipid Carrier Formulation of Curcumin

“…It could be attributed to the fact that curcumin, which is contained deep within the lipidic core and must travel along a longer diffusion path to reach the surface than a medication encapsulated near the surface, is hydrophobic [ 64 ]. The increased drug release from the F1 formulation compared to the other formulations (F2, F4, F12, and F19) could be attributed to the much smaller particle size, which increases the surface area and, as a result, the drug release rate [ 65 , 66 ].…”

Quality by Design based development and investigation of nasal polymeric micelles loaded with meloxicam

“…Polymeric micelles are made up by the so-called amphiphilic graft co-polymers, which just like classic micellar systems prepared by surfactants, tend to self-associate above the critical micellar concentration (CMC) and temperature, allowing a highly efficient drug encapsulation . Generally, they can be described as non-toxic agents and they do not harm the cell membranes, less likely than in case of classic surfactant-like molecules (Zakharova et al, 2019;Katona et al, 2022). Their main advantage might lie in the fact that they can transport poorly water soluble active pharmaceutical ingredients (APIs) with low permeation tendency across biological barriers difficult to get through, such as the BBB (Sun et al, 2020).…”