Title:Solid lipid Particles as Drug Carriers – Effects of Particle Preparation Methods and Lipid Excipients on Particle Characteristics
VOLUME: 6 ISSUE: 2
Author(s):Cintia Kieffer Gamboa*, Ranoda Samir, Chengyu Wu and Huiling Mu
Affiliation:Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen
Keywords:Excipients, lipidified protein, oral drug delivery, particulate delivery systems, peptide/protein drugs, solid lipid
microparticles, solid lipid nanoparticles.
Abstract:Background: Oral delivery of biopharmaceuticals is limited by the absorption barriers in
the Gastrointestinal Tract (GIT) such as low permeability across the biological membranes and the enzymatic
degradation by proteases. In this study, lipid-based drug delivery systems were proposed to
overcome these obstacles.
Objective: The aim of this study was to evaluate the effect of particle preparation methods and excipients
on the characteristics of Solid Lipid Microparticles (SLM) and Solid Lipid Nanoparticles (SLN).
Method: Different triglycerides (TG) were used as the major excipients for the SLM and SLN. Insulin
was used as the model protein; insulin-phospholipid (PL) was prepared to increase drug lipophilicity
and compatibility with lipid excipients. Four methods were used for preparing lipid particles, i.e. a Hot
Melting Dispersion (HMD) technique, a Solvent Evaporation (SE) method, a modified Solvent Evaporation
(mSE) method and a Spray Drying technique. The lipid particles were evaluated in terms of
size, size distribution, surface morphology and drug Entrapment Efficiency (EE).
Results: The results suggested that SE method was the most suitable method for preparing insulin-PL
loaded Solid Lipid Particles (SLP). No differences were observed when the SLP with a Long Chain
Triglyceride (LCT) either a Medium Chain Triglyceride (MCT) in term of size. 70-90% of the lipidified
insulin was incorporated in the lipid particles.
Conclusion: The preparation methods affected the size and morphology of SLP significantly, and the
selection of lipid excipient should be done based on specific application requirements. Furthermore,
the use of the lipidified protein was an efficient way to encapsulate protein in lipid carriers.
