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Glyceryl Trilaurate/Trilaurin

Trilaurin is a triglyceride obtained by formal acylation of the three hydroxy groups of glycerol by lauric (dodecanoic) acid. It is a triglyceride and a dodecanoate ester.

Skeletal formula of trilaurin.Fig.1 Skeletal formula of trilaurin.

Trilaurin in Solid Lipid Particles for Oral Delivery of Peptide and Protein Drugs

Solid lipid particles are promising carriers for the oral delivery of peptide and protein drugs. Reports have shown that such carriers protect the macromolecules from degradation in the gastrointestinal tract (GIT) and possibly enhance the membrane permeation of the macromolecules. Trilaurin (TG12), trimyristin (TG14), tripalmitin (TG16), and tristearin (TG18) were used as lipid excipients to produce solid lipid microparticles. The release of desmopressin from all lipid particles was accelerated by adding TG12 to the lipolysis medium as drug-free microparticles or incorporated in TG16 particles. In addition, TG12 particles, along with other lipid microparticles, can protect desmopressin from degradation in the lipolysis medium.

SEM-micrographs of solid lipid microparticles at 1500× magnification unless otherwise specified. (a) TG14 microparticles, (b) TG16 microparticles (750× magnification), (c) TG18 microparticles, (d) TG12:TG16 (20:80) microparticles, (e) TG12:TG16 (50:50) microparticles (2000× magnification), (f) TG12:TG16 (80:20) microparticles. Size bars: 10 μm.Fig.2 SEM-micrographs of solid lipid microparticles at 1500× magnification unless otherwise specified. (a) TG14 microparticles, (b) TG16 microparticles (750× magnification), (c) TG18 microparticles, (d) TG12:TG16 (20:80) microparticles, (e) TG12:TG16 (50:50) microparticles (2000× magnification), (f) TG12:TG16 (80:20) microparticles. Size bars: 10 μm. (Christophersen, 2014)

Nanostructured Lipid Carriers with Trilaurin and Oleic Acid as Lipid Core Mediate Carbamazepine Brain Delivery

Carbamazepine (CBZ) is an antiepileptic and anxiolytic drug widely used to treat seizures, trigeminal neuralgia, and bipolar disorders. CBZ-NLCs were prepared by using a binary mixture of trilaurin and oleic acid as a lipid core stabilized with Poloxamer 188, Tween 80, and Span 80. The direct measurement of CBZ in brain tissues (brain kinetics) along with in vivo anticonvulsant and anxiolytic activities would truly reflect the therapeutic potential of CBZ-loaded nanostructured lipid carriers (CBZ-NLCs) in brain delivery. The optimized CBZ-NLCs enabled high drug incorporation (85%) with a 7.9-folds increase in CBZ aqueous solubility. CBZ-NLCs significantly improved brain deposition of CBZ coupled with enhanced in vivo anticonvulsant and anxiolytic activities compared with CBZ dispersion. Consequently, NLCs-mediated brain drug delivery suggests a promising strategy that will open a new perspective for the treatment of neurological diseases.

Particle size distribution curve (A) and TEM image (B) of CBZ-NLCs.Fig.3 Particle size distribution curve (A) and TEM image (B) of CBZ-NLCs. (Khan, 2020)

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References

  1. Christophersen, P.C.; et al. Solid lipid particles for oral delivery of peptide and protein drugs II-the digestion of trilaurin protects desmopressin from proteolytic degradation. Pharm Res. 2014 Sep; 31(9): 2420-8.
  2. Khan, N.; et al. Nanostructured lipid carriers-mediated brain delivery of carbamazepine for improved in vivo anticonvulsant and anxiolytic activity. Int J Pharm. 2020 Mar 15; 577: 119033.
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