Compritol^®-based solid lipid nanoparticles of desvenlafaxine prepared by ultrasonication-assisted hot-melt encapsulation to modify its release

Abstract

Aims: Desvenlafaxine (DES) in conventional dosage forms shows initial burst release after oral administration, leading to exaggeration of its side effects. These side effects can be overcome by a sustained-release dosage form using the chemically inert, low-melting-point lipid Compritol^® 888 ATO, as it reduces initial burst release. Materials & methods: The potential of DES-loaded solid lipid nanoparticles (DES-SLNs) synthesized by ultrasonication-assisted hot-melt encapsulation to modify the release of DES was investigated. Results: The entrapment efficiency of DES-SLNs was 65.90% with the in vitro release profile showing a sustained-release behavior achieving 81% cumulative release within 16 h without initial burst release. Conclusion: DES-SLNs are a potential carrier for sustained release of water-soluble antidepressant drugs such as DES.

Summary points

• Desvenlafaxine (DES) is a hydrophilic drug showing initial burst release from conventional dosage forms. It is rapidly absorbed after its oral administration, which intensifies its side effects.

• Its burst release was overcome by incorporating it into Compritol-based solid lipid nanoparticles (SLNs).

• DES-SLNs prepared by the hot-melt encapsulation technique had a particle size of 156 nm with an encapsulation efficiency of 69.50% and appeared spherical with a smooth surface when observed under a scanning electron microscope.

• The DES-SLNs had a polydispersity index value of 0.139, indicative of homogenous dispersion.

• x-ray diffraction analysis revealed the conversion of DES from crystalline form to amorphous form, exhibiting molecular dispersion of the DES in the Compritol matrix.

• An in vitro release study of DES presented a sustained release of drug from lipid matrix with no initial burst release that is observed in commercially available tablets of DES.

Keywords: :

• antidepressant
• desvenlafaxine
• hydrophilic
• solid lipid nanoparticles
• sustained-release
• ultrasonication-assisted hot-melt encapsulation

Financial disclosure

The authors did not receive any funding for this study. The authors have no financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending or royalties.

Competing interests disclosure

The authors have no competing interests or relevant affiliations with any organization or entity with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending or royalties.

Writing disclosure

No writing assistance was utilized in the production of this manuscript.