Advertisement

Topics

In vivo evaluation of solid lipid microparticles and hybrid polymer-lipid microparticles for sustained delivery of leuprolide.

08:00 EDT 9th July 2019 | BioPortfolio

Summary of "In vivo evaluation of solid lipid microparticles and hybrid polymer-lipid microparticles for sustained delivery of leuprolide."

This study aims to investigate the potential of solid lipid microparticles (MP) and hybrid polymer-lipid MPs for sustained delivery of a peptide drug, leuprolide. A peptide-phospholipid complex was prepared to increase the compatibility of the peptide with triglyceride (TG) and poly (lactide-co-glycolide) (PLGA). Peptide loaded solid lipid MPs, PLGA MPs, and hybrid MPs were prepared using a spray drying method and characterized in terms of particle size, morphology and encapsulation efficiency. The pharmacokinetics and pharmacodynamics of leuprolide after subcutaneous injection of spray-dried MPs were evaluated in rats. Spray-dried MPs were spherical ranging in size from 4 μm to 10 μm, which are suitable for injection. After subcutaneous administration of reconstituted MPs, leuprolide could be detected in plasma samples of rats for one to two months, depending on the formulation and dose. Sustained release of leuprolide from PLGA MPs and glyceryl tristearate (TG18) MPs was observed over one month, with a chemical castration effect of 25 and 30 days, respectively. The bioavailability of leuprolide from PLGA-TG18 hybrid MPs was approximately four times higher than that from TG18 MP and PLGA MP alone using the same dose of leuprolide (6 mg/kg). Chemical castration in rats was observed over 30 and 60 days after injection of the PLGA-TG18 hybrid MP with a dose of 3 mg/kg and 6 mg/kg leuprolide, respectively. Additionally, a much lower C was observed for the hybrid MP group. In conclusion, spray-dried PLGA-triglyceride hybrid MPs can be used as better carriers than other MPs for subcutaneous delivery of peptide drugs due to the synergetic effect of lipids and PLGA for sustained drug release from the spray-dried MP.

Affiliation

Journal Details

This article was published in the following journal.

Name: European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
ISSN: 1873-3441
Pages:

Links

DeepDyve research library

PubMed Articles [18720 Associated PubMed Articles listed on BioPortfolio]

Microfluidic preparation of polymer-lipid Janus microparticles with staged drug release property.

This work demonstrated a microfluidic preparation process for novel Janus microparticles with individual drug release properties in each compartment. A flow-focusing microfluidic chip was designed to ...

Solid lipid nanoparticles for ocular delivery of isoniazid: evaluation, proof of concept and in vivo safety & kinetics.

Evaluation of solid lipid nanoparticles (SLNs) for ocular delivery of isoniazid (INH).

Hybrid membranes of lipids and diblock copolymers: From homogeneity to rafts to phase separation.

Hybrid lipid-polymer vesicles can integrate benefits of liposomes and polymersomes. In this work, the phase behavior of hybrid membranes containing lipids and diblock copolymers is explored by dissipa...

A new melatonin oral delivery platform based on orodispersible films containing solid lipid microparticles.

An innovative delivery system for melatonin, based on the incorporation of solid lipid microparticles in orodispersible films (ODFs) made of maltodextrin, was designed and developed. Lipid micropartic...

Polymer-lipid hybrid nanoparticles: a novel drug delivery system for enhancing the activity of Psoralen against breast cancer.

A polymer-lipid hybrid nanocarrier was developed to encapsulate psoralen (PSO) to improve its water solubility and bioavailability. The effects of PSO-loaded polymer-lipid hybrid nanoparticles (PSO-PL...

Clinical Trials [7082 Associated Clinical Trials listed on BioPortfolio]

Digestion of Biopolymer Based Lipid Emulsions

In this randomized, double blind, unbalanced three way crossover trial, four lipid emulsions will be assessed on three study days. The lipid emulsions (LEs) have been engineered so that th...

Nanosomal Docetaxel Lipid Suspension in Treating Patients With Advanced Solid Tumors

This randomized phase I trial studies the side effects and best dose of nanosomal docetaxel lipid suspension in treating patients with advanced solid tumors. Drugs used in chemotherapy, su...

Genetic Origin of Lipid Disorders

Several lipid disorders are without known genetic origin. The scope of this project is to sequence genes superior involved in lipid and carbohydrate metabolism in patients with severe lipi...

The Clinical Evaluation of Efficacy of Lipid-Lowing Tea on Hyperlipidemia Patients’ Lipid Profiles

The purpose of this study is to determine whether the Lipid-lowing Tea is effective and safe in the treatment of Hyperlipidemia Patients

Quantitative MR Methods for Lipid Emulsions

Quantitative MR methods will be validated for the non-invasive imaging of GI processing of lipid emulsions in 18 (12+6) healthy subjects. Validation is performed by a randomized single bli...

Medical and Biotech [MESH] Definitions

Conditions characterized by abnormal lipid deposition due to disturbance in lipid metabolism, such as hereditary diseases involving lysosomal enzymes required for lipid breakdown. They are classified either by the enzyme defect or by the type of lipid involved.

Peroxides produced in the presence of a free radical by the oxidation of unsaturated fatty acids in the cell in the presence of molecular oxygen. The formation of lipid peroxides results in the destruction of the original lipid leading to the loss of integrity of the membranes. They therefore cause a variety of toxic effects in vivo and their formation is considered a pathological process in biological systems. Their formation can be inhibited by antioxidants, such as vitamin E, structural separation or low oxygen tension.

Protein components on the surface of LIPOPROTEINS. They form a layer surrounding the hydrophobic lipid core. There are several classes of apolipoproteins with each playing a different role in lipid transport and LIPID METABOLISM. These proteins are synthesized mainly in the LIVER and the INTESTINES.

A family of vertebrate and insect lipid droplet associated proteins. They consist of a conserved N-terminal PAT domain (an alpha-helical region of about 110 amino acids), an 11-mer repeat region, and lipid-binding hydrophobic regions or 4-helix bundles near their C-termini. Perilipins transiently or constitutively localize to LIPID DROPLETS in ADIPOCYTES and FOAM CELLS, especially in regions adjacent to the PLASMA MEMBRANE and ENDOPLASMIC RECTICULUM. They are critical for lipid droplet synthesis and homeostasis as well as the regulation of lipid metabolism. Genetic variations in perilipins are associated with ATHEROSCLEROSIS; OBESITY; and DIABETES MELLITUS.

Proteins that are covalently-linked to lipid molecules or hydrophobic molecules such as those that contain prenyl groups. The lipid moieties aid in the association of the proteins with CELL MEMBRANES.

Advertisement
Quick Search
Advertisement
Advertisement

 


DeepDyve research library

Relevant Topics

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...

Blood
Blood is a specialized bodily fluid that delivers necessary substances to the body's cells (in animals) – such as nutrients and oxygen – and transports waste products away from those same cells.  In vertebrates, it is composed of blo...


Searches Linking to this Article