Effect of Lipophilicity of Dispersed Drugs on the Physicochemical and Technological Properties of Solid Lipid Nanoparticles

Abstract

A series of aliphatic esters of the NSAID naproxen (NAP) were synthesised and encapsulated in solid lipid nanoparticles (SLN) to evaluate the influence of lipophilicity on drug loading and release, as well as physicochemical properties and stability of SLN. The lipophilicity of esters mainly showed to influence their affinity for the solid lipid matrix, modifying the drug release profile compared to the parent drug, whereas drug encapsulation efficiency and the technological properties and stability of SLN were not affected. After storage at room temperature the in vitro release profiles of esters changed with respect to freshly prepared systems, depending on the lipophilicity of the dispersed derivative. In particular, the SLN containing the medium-chain hexyl and octyl esters showed a 70-80% increase of drug release after storage; SLN loaded with NAP or the lower ethyl and butyl esters did not show significant changes in the drug release rate. Such findings reveal that the affinity of NAP esters for the lipid network of the nanoparticles is strongly dependent on their lipophilicity and an excessive increase of the latter negatively influences the allocation and retention on these compounds in the nanoparticles.

Optimization of carvedilol solid lipid nanoparticles: An approach to control the release and enhance the oral bioavailability on rabbits

“…The percent of CVD entrapped in the prepared SLNs was determined by an ultracentrifugation method as described before [ 27 , 28 ]. Briefly, the sample was centrifuged, filtered and the amount of free and entrapped CVD was dissolved in methanol and analyzed at 248 nm using the HPLC method [ 29 ].…”

In‐Vitro Permeability of Neutral Polystyrene Particles via Buccal Mucosa

“…The PdI indicates the distribution of particles sizes. Values <0.2 are interpreted as indication for homogenous samples,45 while values up to 0.5 indicate reliable and reproducible results. The zeta potential was measured by laser doppler velocimetry (scattering angle of 17°) coupled with photon correlation spectroscopy (Zetasizer Nano ZS, Malvern Instruments, Malvern, UK) and calculated out of the electrophoretic mobility by applying the henry equation.…”

Preparation and Microbiological Evaluation of Amphiphilic Kanamycin-Lipoamino Acid Ion-Pairs

“…As a side aim of this study, it is however conceivable that the increased lipophilic character of KAN-LAA ion-pairs would positively affect drug encapsulation and retention in lipid-based carrier systems, such as liposomes and lipid nanoparticles. Several reports in the literature support the idea of optimizing the absorption or fate of compounds by combining a prodrug strategy and lipid nanocarriers [ 38 , 39 , 40 , 41 ]. This technological potentiality is going to be exploited in a separate study.…”