Development and in vivo evaluation of a new oral nanoparticulate dosage form for leuprolide based on polyacrylic acid.
Summary of "Development and in vivo evaluation of a new oral nanoparticulate dosage form for leuprolide based on polyacrylic acid."
It was the aim of this study to develop a nanoparticulate oral drug delivery system for leuprolide based on polyacrylic acid (PAA). In order to achieve formation of nanoparticles in a mild, aqueous environment, two different techniques were combined, namely hydrophobic ion pairing between leuprolide and sodium dodecyl sulphate in a first step, followed by encapsulation into nanoparticles gained by interpolymer complexation between polyacrylic acid and Pluronic F68. The obtained nanoparticles were characterized regarding particle size distribution, drug encapsulation efficiency and in vitro release profile. Additionally, the pharmacokinetic profiles of leuprolide after oral administration of PAA-nanoparticulate and PAA-control tablets to male Sprague-Dawley rats were assessed and compared. It could be shown, that hydrophobic ion pairing increased encapsulation efficacy of leuprolide and leads to a slowed drug release of nanoparticulate suspensions. Relative oral bioavailability of leuprolide could be increased by nanoparticulate tablets up to 4.2-fold. Results verify that the suggested approach is a promising strategy for the design of oral delivery systems for oral administration of peptide drugs.
Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 52c, Josef Möller Haus, 6020 Innsbruck, Austria.
This article was published in the following journal.
Name: Drug delivery
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/21557716
- DOI: http://dx.doi.org/10.3109/10717544.2011.577108
The objective of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) for the model peptide drug leuprorelin to prove a protective effect against luminal enzymatic metabolis...
Plasmodium falciparum is responsible of the most severe form of malaria, and new targets and novel chemotherapeutic scaffolds are needed to fight emerging multidrug-resistant strains of this parasite....
Drugs with good solubility exhibit good oral absorption, and subsequently good bioavailability. Thus, most exigent phase of drug development practice particularly for oral dosage forms is the enhancem...
Abstract A major constraint in oral controlled release drug delivery is that not all the drug candidates are absorbed uniformly throughout the gastrointestinal tract (GIT). Drugs having "absorption wi...
The present study introduces a miniaturized high-throughput platform to understand the influence of excipients on the performance of oral solid dosage forms during early drug development. Wet massing...
OBJECTIVES: I. Evaluate the beneficial effects of leuprolide depot, oral contraceptive therapy, and leuprolide/oral contraceptive therapy in the management of patients with ovarian...
The purpose of this research study is to determine the effects of abiraterone acetate plus leuprolide acetate and prednisone versus leuprolide acetate alone on hormone levels in the blood...
Paracetamol is the centrally acting analgesic most commonly used in the world, indicated for the symptomatic treatment of fever and pain in mild to moderate. It comes in different formulat...
The purpose of this study is to determine if new formulations (11.25 and 30 mg) of leuprolide are effective in treating children with Central Precocious Puberty.
RATIONALE: The body's response to one injection of leuprolide may provide more information than the standard test for gonadotropin deficiency in determining whether the cause of gonadotrop...
Medical and Biotech [MESH] Definitions
Drugs intended for human or veterinary use, presented in their finished dosage form. Included here are materials used in the preparation and/or formulation of the finished dosage form.
The number of copies of a given gene present in the cell of an organism. An increase in gene dosage (by GENE DUPLICATION for example) can result in higher levels of gene product formation. GENE DOSAGE COMPENSATION mechanisms result in adjustments to the level GENE EXPRESSION when there are changes or differences in gene dosage.
Genetic mechanisms that allow GENES to be expressed at a similar level irrespective of their GENE DOSAGE. This term is usually used in discussing genes that lie on the SEX CHROMOSOMES. Because the sex chromosomes are only partially homologous, there is a different copy number, i.e., dosage, of these genes in males vs. females. In DROSOPHILA, dosage compensation is accomplished by hypertranscription of genes located on the X CHROMOSOME. In mammals, dosage compensation of X chromosome genes is accomplished by random X CHROMOSOME INACTIVATION of one of the two X chromosomes in the female.
The stages of development of the psychological aspects of sexuality from birth to adulthood; i.e., oral, anal, genital, and latent periods.
Any process by which toxicity, metabolism, absorption, elimination, preferred route of administration, safe dosage range, etc., for a drug or group of drugs is determined through clinical assessment in humans or veterinary animals.