Separation and identification of acylated leuprorelin inside PLGA microspheres.

07:00 EST 4th February 2019 | BioPortfolio

Summary of "Separation and identification of acylated leuprorelin inside PLGA microspheres."

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.


Journal Details

This article was published in the following journal.

Name: International journal of pharmaceutics
ISSN: 1873-3476


DeepDyve research library

PubMed Articles [7180 Associated PubMed Articles listed on BioPortfolio]

Encapsulation and release of Doxycycline from electrospray-generated PLGA microspheres: effect of polymer end groups.

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...

Facile fabrication of PEG-coated PLGA microspheres via SPG membrane emulsification for the treatment of scleroderma by ECM degrading enzymes.

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...

Highly bioactive, bevacizumab-loaded, sustained-release PLGA/PCADK microspheres for intravitreal therapy in ocular diseases.

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 and MicroRNA-124 Co-loaded poly (lactic-co-glycolic acid) Microspheres Inhibit Progression of Adjuvant-induced Arthritis in Rats.

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....

Antimicrobial Activity of 3D-Printed Poly(ε-Caprolactone) (PCL) Composite Scaffolds Presenting Vancomycin-Loaded Polylactic Acid-Glycolic Acid (PLGA) Microspheres.

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)...

Clinical Trials [1865 Associated Clinical Trials listed on BioPortfolio]

Leuprorelin Associated With Radiotherapy Versus Leuprorelin Alone in T3 - T4 or pT3 (on Biopsy) N0, M0 Prostate Cancer

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...

A Phase 3 Study to Evaluate the Efficacy and Safety of TAK-385 40 mg Compared With Leuprorelin in the Treatment of Uterine Fibroids

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...

Locally Delivered Doxycycline Adjunct to Nonsurgical Periodontal Therapy.

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...

A Prospective Study Comparing Contour SE™ Microspheres to Embosphere® Microspheres for Treating Symptomatic Uterine Fibroids With Uterine Fibroid Embolization (UFE)

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...

PLGA-coated Biphasic Calcium Phosphate in Sinus Lift

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...

Medical and Biotech [MESH] Definitions

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).

Quick Search


DeepDyve research library

Relevant Topic

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...

Searches Linking to this Article