Track topics on Twitter Track topics that are important to you
Studies have shown that the N-terminus and lysine side residue of peptides are prone to acylation in poly(D,L-lactide-co-glycolide) (PLGA) microspheres. Peptides such as leuprorelin lack a free N-terminus or lysine and only contain serine, arginine, and tyrosine as nucleophilic residues. The purpose of this study was to detect potential acylation impurities and determine their corresponding acylation sites in commercial leuprorelin-loaded PLGA microspheres. Commercial samples from three vendors were selected as targets for our study. The high-performance liquid chromatography (HPLC) conditions of the European Pharmacopoeia were used to separate and collect impurities. HPLC-tandem mass spectrometry (HPLC-MS/MS) was applied to confirm both the structure and acylation sites of the impurities. Our study demonstrated that impurities originating from both degradation of microspheres and synthesis of leuprorelin were well separated and identified using these HPLC conditions. HPLC-MS/MS analysis of acylated leuprorelin showed that diglycoyl, lactoyl-glycoyl, dilactoyl, and monolactoyl groups were conjugated to serine in leuprorelin-loaded PLGA microspheres. This is the first report showing serine to be the acylation site in peptide-loaded PLGA microspheres. Separation and identification of acylated leuprorelin derivatives will assist in minimising acylation and guiding the development of quality control for commercial leuprorelin-loaded PLGA microspheres.
This article was published in the following journal.
Name: International journal of pharmaceutics
The aim of this study was to investigate the influence of end group of poly(lactic-co-glycolic acid) (PLGA) on the drug loading and release behavior of electrospray-generated PLGA microspheres. To thi...
We developed a facile fabrication method for preparing poly(ethylene glycol)(PEG)-coated poly (lactic-co-glycolic acid) (PLGA) microspheres with homogeneous size distribution via a combination of mPEG...
Bevacizumab, a vascular endothelial growth factor (VEGF)-targeting drug, is widely used as an off-label therapeutic for age-related macular degeneration (AMD). To reduce the monthly administration fre...
Ketoprofen, a non-steroid anti-inflammatory drug, is widely used for relieving the pain and swelling caused by rheumatoid arthritis. However, ketoprofen can't suppress disease progression effectively....
BACKGROUND The aim of this study was to design and test a novel composite scaffold with antibacterial efficacy for treating bone infections using a three-dimensional (3D) printed poly(ε-caprolactone)...
the purpose of this study "Leuprorelin associated with radiotherapy versus leuprorelin alone in T3 - T4 or pT3 (on biopsy) N0, M0 prostate cancer" is to assess the possible benefits of the...
The purpose of this study is to evaluate the efficacy of TAK-385 40 mg admistered orally once daily for 12 weeks, compared with leuprorelin injection (once/4 weeks, 1.88 mg or 3.75 mg SC/t...
The aim of this clinical study is to asses the effect of ultrasonic periodontal debridement associated to locally delivered doxycycline (20%) by PLGA microspheres on chronic generalized pe...
The purpose of this study is to demonstrate comparability between Contour SE™ Microspheres and Embosphere® Microspheres for achieving post UFE fibroid devascularization in women with s...
The study aims to investigate the radiological and histomorphometric results of the use of PLGA-coated biphasic calcium phosphate granules in sinus floor elevation, to analyze the underlyi...
A cell-separation technique where magnetizable microspheres or beads are first coated with monoclonal antibody, allowed to search and bind to target cells, and are then selectively removed when passed through a magnetic field. Among other applications, the technique is commonly used to remove tumor cells from the marrow (BONE MARROW PURGING) of patients who are to undergo autologous bone marrow transplantation.
Techniques for separation and identification of ionized molecules based on their drift through a gas phase after being accelerated by an electric field. Their mobilities will be effected by their shape, size, and charge.
Works consisting of book owner's identification labels. They are usually intended for attaching inside a book or similar object. (From Thesaurus for Graphic Materials II: Genre and Physical Characteristic Terms, 1995)
The separation of individuals or groups resulting in the lack of or minimizing of social contact and/or communication. This separation may be accomplished by physical separation, by social barriers and by psychological mechanisms. In the latter, there may be interaction but no real communication.
The separation of particles from a suspension by passage through a filter with very fine pores. In ultrafiltration the separation is accomplished by convective transport; in DIALYSIS separation relies instead upon differential diffusion. Ultrafiltration occurs naturally and is a laboratory procedure. Artificial ultrafiltration of the blood is referred to as HEMOFILTRATION or HEMODIAFILTRATION (if combined with HEMODIALYSIS).
Multiple Sclerosis MS
Multiple sclerosis (MS) is the most common disabling neurological condition affecting 100,000 young adults in the UK. The condition results from autoimmune damage to myelin, causing interference in nerve signaling. Symptoms experienced depend on the pa...