Long-acting release microspheres containing novel GLP-1 analog as an antidiabetic system.

08:00 EDT 15th May 2018 | BioPortfolio

Summary of "Long-acting release microspheres containing novel GLP-1 analog as an antidiabetic system."

Glucagon-like peptide 1 (GLP-1) has recently received significant attention as an efficacious way to treat diabetes mellitus. However, the short half-life of the peptide limits its clinical application in diabetes. In our previous study, a novel GLP-1 analog (PGLP-1) with a longer half-life was synthesized and evaluated. Herein, we prepared the PGLP-1-loaded poly(D,L-lactide-co- glycolide) microspheres to achieve long-term effects on blood glucose control. The incorporation of zinc ion into the formulation can effectively decrease the initial burst release, and a uniform drug distribution was obtained, in contrast to native PGLP-1 encapsulated microspheres. We demonstrated that the solubility of the drug encapsulated in microspheres played an important role in the release behavior and drug distribution inside the microspheres. Zn-PGLP-1 microspheres had a prominent acute glucose reduction effect in healthy mice during two weeks after the initial injection. A hypoglycemic effect was observed in the streptozotocin (STZ) induced diabetic mice through a 6-week treatment of Zn-PGLP-1-loaded microspheres. Meanwhile, the administration of Zn-PGLP-1 microspheres led to the β-cell protection and stimulation of insulin secretion. The novel GLP-1 analog-loaded sustained microspheres may greatly improve patient compliance with an excellent safety feature.


Journal Details

This article was published in the following journal.

Name: Molecular pharmaceutics
ISSN: 1543-8392


DeepDyve research library

PubMed Articles [12331 Associated PubMed Articles listed on BioPortfolio]

Preparation of new risperidone depot microspheres based on novel biocompatible poly(alkylene adipate) polyesters as long acting injectable formulations.

Risperidone (RIS) loaded microspheres based on poly(alkylene adipate)s derived from dicarboxylic acids and different aliphatic diols were prepared by the o/w emulsion and solvent evaporation method. S...

Morphology and internal structure control over PLA microspheres by compounding PLLA and PDLA and effects on drug release behavior.

The applications of Polylactide (PLA) microspheres in biomedical areas are greatly determined by the size, morphology and internal structure. Taking advantage of the formation of stereocomplex (SC) cr...

Costs associated with long-acting insulin analogues in patients with diabetes.

The objective of this literature review was to evaluate the costs associated with the use of long-acting insulin analogues (LAIAs) compared with non-LAIA agents, including human insulin, oral antidiab...

PLGA microsphere/PVA hydrogel coatings suppress the foreign body reaction for 6 months.

The application of dexamethasone releasing poly (lactic-co-glycolic acid) (PLGA) microspheres embedded in a poly vinyl alcohol (PVA) hydrogel coatings have been successfully used in the suppression of...

Paclitaxel and etoposide-loaded Poly (lactic-co-glycolic acid) microspheres fabricated by coaxial electrospraying for dual drug delivery.

In this study, we fabricated paclitaxel (PTX) and etoposide (ETP) loaded Poly (lactic-co-glycolic acid) (PLGA) microspheres with core-shell structures and particle sizes ranging from 1 to 4 µm by coa...

Clinical Trials [5060 Associated Clinical Trials listed on BioPortfolio]

Effects of Exenatide Long-Acting Release on Glucose Control and Safety in Subjects With Type 2 Diabetes Mellitus(DURATION - 1)

The purpose of this study is to examine the effects of exenatide long-acting release (LAR) on glucose control and safety in subjects with type 2 diabetes mellitus managed with diet modific...

Evaluation of Efficacy and Safety of Long-acting Risperidone Microspheres in Patients With Schizophrenia or Other Psychotic Disorders When Switching From Typical Antipsychotic (Oral/Depot) or Atypical Oral Other Than Risperidone

The purpose of this study is to evaluate the efficacy, tolerability and safety of patients on long-acting Risperidone microshpheres injection. The major advantage of long-acting injection ...

Study Examining Exenatide Long-Acting Release in Subjects With Type 2 Diabetes

Exenatide LAR is a long-acting release formulation of exenatide, which is a twice-daily dosage form currently under investigation as a potential treatment for people with type 2 diabetes m...

A Study to Evaluate Symptomatic Remission in Schizophrenia With Long Acting Risperidone Microspheres

The purpose of this study is to evaluate symptomatic remission rate in patients with schizophrenia using long acting risperidone microspheres

A Study to Evaluate Treatment Adherence in Schizophrenia With Long Acting Risperidone Microspheres (e-STAR)

This study is a non-interventional web based registry designed to assess demographic, treatment and outcomes data in patients receiving treatment with long-acting injectable risperidone. O...

Medical and Biotech [MESH] Definitions

Small uniformly-sized spherical particles, of micrometer dimensions, frequently labeled with radioisotopes or various reagents acting as tags or markers.

A potent, long-acting synthetic SOMATOSTATIN octapeptide analog that inhibits secretion of GROWTH HORMONE and is used to treat hormone-secreting tumors; DIABETES MELLITUS; HYPOTENSION, ORTHOSTATIC; HYPERINSULINISM; hypergastrinemia; and small bowel fistula.

One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.

An insulin preparation that is designed to provide immediate and long term glycemic control in a single dosage. Biphasic insulin typically contains a mixture of REGULAR INSULIN or SHORT-ACTING INSULIN combined with a LONG-ACTING INSULIN.

A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE that regulates the synthesis and release of pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE.

Quick Search


DeepDyve research library

Relevant Topics

Diabetes is a lifelong condition that causes a person's blood sugar level to become too high. The two main types of diabetes are: type 1 diabetes type 2 diabetes In the UK, diabetes affects approximately 2.9 million people. There are a...

Nephrology - kidney function
Nephrology is a specialty of medicine and pediatrics that concerns itself with the study of normal kidney function, kidney problems, the treatment of kidney problems and renal replacement therapy (dialysis and kidney transplantation). Systemic conditions...

Drug Discovery
Clinical Approvals Clinical Trials Drug Approvals Drug Delivery Drug Discovery Generics Drugs Prescription Drugs In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which drugs are dis...

Searches Linking to this Article