Next Article in Journal
Sugar and Polymer Excipients Enhance Uptake and Splice-Switching Activity of Peptide-Dendrimer/Lipid/Oligonucleotide Formulations
Next Article in Special Issue
MRI/Photoluminescence Dual-Modal Imaging Magnetic PLGA Nanocapsules for Theranostics
Previous Article in Journal
Monitoring the Clinical Response to an Innovative Transdermal Delivery System for Ibuprofen
Previous Article in Special Issue
Monitoring the Fate of Orally Administered PLGA Nanoformulation for Local Delivery of Therapeutic Drugs
Open AccessArticle

Risperidone-Loaded PLGA–Lipid Particles with Improved Release Kinetics: Manufacturing and Detailed Characterization by Electron Microscopy and Nano-CT

1
Institute of Pharmacy, Faculty of Biosciences, Martin Luther University Halle-Wittenberg, 06120 Halle (Saale), Germany
2
Department of Biological and Macromolecular Materials, Fraunhofer Institute for Microstructure of Materials and Systems IMWS, 06120 Halle (Saale), Germany
3
Institute of Physics, Martin Luther University Halle-Wittenberg, 06120 Halle (Saale), Germany
4
Department of Psychiatry, Psychotherapy and Psychosomatics, Martin Luther University Halle-Wittenberg, 06120 Halle (Saale), Germany
5
MilliporeSigma a Business of Merck KGaA, 64293 Darmstadt, Germany
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(12), 665; https://doi.org/10.3390/pharmaceutics11120665
Received: 31 October 2019 / Revised: 24 November 2019 / Accepted: 2 December 2019 / Published: 9 December 2019
(This article belongs to the Special Issue PLGA Based Drug Carrier and Pharmaceutical Applications)
For parenteral controlled drug release, the desired zero order release profile with no lag time is often difficult to achieve. To overcome the undesired lag time of the current commercial risperidone controlled release formulation, we developed PLGA–lipid microcapsules (MCs) and PLGA–lipid microgels (MGs). The lipid phase was composed of middle chain triglycerides (MCT) or isopropylmyristate (IPM). Hydroxystearic acid was used as an oleogelator. The three-dimensional inner structure of Risperidone-loaded MCs and MGs was assessed by using the invasive method of electron microscopy with focused ion beam cutting (FIB-SEM) and the noninvasive method of high-resolution nanoscale X-ray computed tomography (nano-CT). FIB-SEM and nano-CT measurements revealed the presence of highly dispersed spherical structures around two micrometres in size. Drug release kinetics did strongly depend on the used lipid phase and the presence or absence of hydroxystearic acid. We achieved a nearly zero order release without a lag time over 60 days with the MC-MCT formulation. In conclusion, the developed lipid-PLGA microparticles are attractive alternatives to pure PLGA-based particles. The advantages include improved release profiles, which can be easily tuned by the lipid composition. View Full-Text
Keywords: controlled release; PLGA; risperidone; microparticles; microcapsules; oleogels; electron microscopy; three-dimensional X-ray imaging; nano-CT; biodegradable polymers; hydroxy-stearic acid controlled release; PLGA; risperidone; microparticles; microcapsules; oleogels; electron microscopy; three-dimensional X-ray imaging; nano-CT; biodegradable polymers; hydroxy-stearic acid
Show Figures

Graphical abstract

MDPI and ACS Style

Janich, C.; Friedmann, A.; Martins de Souza e Silva, J.; Santos de Oliveira, C.; Souza, L.E.; Rujescu, D.; Hildebrandt, C.; Beck-Broichsitter, M.; Schmelzer, C.E.H.; Mäder, K. Risperidone-Loaded PLGA–Lipid Particles with Improved Release Kinetics: Manufacturing and Detailed Characterization by Electron Microscopy and Nano-CT. Pharmaceutics 2019, 11, 665.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop