Show/Hide Menu
Hide/Show Apps
Logout
Türkçe
Türkçe
Search
Search
Login
Login
OpenMETU
OpenMETU
About
About
Open Science Policy
Open Science Policy
Open Access Guideline
Open Access Guideline
Postgraduate Thesis Guideline
Postgraduate Thesis Guideline
Communities & Collections
Communities & Collections
Help
Help
Frequently Asked Questions
Frequently Asked Questions
Guides
Guides
Thesis submission
Thesis submission
MS without thesis term project submission
MS without thesis term project submission
Publication submission with DOI
Publication submission with DOI
Publication submission
Publication submission
Supporting Information
Supporting Information
General Information
General Information
Copyright, Embargo and License
Copyright, Embargo and License
Contact us
Contact us
Raloxifene delivery systems for osteoporosis treatment
Download
index.pdf
Date
2014
Author
Kavas, Ayşegül
Metadata
Show full item record
Item Usage Stats
311
views
144
downloads
Cite This
One of the osteoporosis drugs, Raloxifene (Ral) is systemically administrated in high dose at frequent intervals, causing high risk of side effects which influence all the body. As a solution to such issues, delivery systems providing controlled and sustained drug release at therapeutic level from a carrier have been studied recently. The aim of this study was to develop Ral- or Ral-poly(ethylene glycol) (PEG)-loaded poly(ε-caprolactone) (PCL) or PCL:poly(D,L-lactide-co-glycolide) (PLGA) microspheres and to evalute their potential usage. Mean diameters of the microspheres were around 1.5 μm. Ral-loaded PCL microspheres had maximum Ral encapsulation efficiency (%) because of high hydrophobic natures of Ral and PCL. Total amount of Ral released from Ral-PEG-loaded PCL:PLGA microspheres was significantly higher than from other microsphere groups. This finding can be ascribed to enhanced wettability of Ral and conversion of crystalline nature of Ral to amorphous form provided by Ral-PEG conjugation, resulting in increased water-solubility of Ral. Enhanced wettability of Ral increases degradation rates of PCL and PLGA by allowing more water penetration into the polymer matrix. Related with this outcome, Ral release from Ral-PEG-loaded PCL:PLGA microspheres resulted with significantly higher mineralization of female adipose-derived mesenchymal stem cells than other groups. In vitro cytotoxicity studies performed using adipose-derived stem cells demonstrated that all microspheres were non-toxic. It was demonstrated that Ral-PEG-loaded PCL:PLGA microsphere formulation provided increased Ral release rate and therefore enhanced mineralization of the stem cells compared to the other formulations in this study. This formulation holds promise for osteoporosis therapy as an effective controlled drug delivery system. For forthcoming studies, PEG conjugation to Ral presents the possibility of adjusting rate of Ral release from microspheres readily by changing PEG ratio in the conjugate.
Subject Keywords
Raloxifene.
,
Osteoporosis.
,
Osteoporosis drugs.
URI
http://etd.lib.metu.edu.tr/upload/12618416/index.pdf
https://hdl.handle.net/11511/24323
Collections
Graduate School of Natural and Applied Sciences, Thesis
Suggestions
OpenMETU
Core
Structural effects of simvastatin on liver rate tissue: Fourier transform infrared and Raman microspectroscopic studies
Garip, Sebnem; Bayari, Sevgi Haman; Severcan, Mete; Abbas, Sherif; Lednev, Igor K.; Severcan, Feride (2016-02-01)
Simvastatin is one of the most frequently prescribed statins because of its efficacy in the treatment of hypercholesterolemia, reducing cardiovascular risk and related mortality. Determination of its side effects on different tissues is mandatory to improve safe use of this drug. In the present study, the effects of simvastatin on molecular composition and structure of healthy rat livers were investigated by Fourier transform infrared and Raman imaging. Simvastatin-treated groups received 50 mg/kg/day simva...
Determination of hypothalamic neuropeptide levels involved in appetite regulation in atypical antipsychotic drug, risperidone treatment
Kurşungöz, Canan; Yanık, Tülin; Department of Biology (2012)
Although the use of atypical antipsychotic drugs is successful in the treatment of schizophrenia, they cause complications in the long term use that is mainly weight gain. In this study, circulating levels of hypothalamic neuropeptides/hormones, which are related to appetite regulation; neuropeptide Y (NPY), alpha melanocyte stimulating hormone (α-MSH), cocaine and amphethamine regulated transcript (CART) and plus leptin in male schizophrenic patients who were treated with an atypical antipsychotic drug, ri...
Metformin – Cisplatin Combination Treatment Alters mRNA Expression of Hexokinase II Gene in LNCaP and PC3 Prostate Cancer Cell Lines
Durukan, Özlem; Evin, Emre; Arslan, Şevki; Adalı, Orhan (null; 2017-07-08)
Metformin is an antidiabetic drug with anticancer properties. Cisplatin is known as one of the most potent chemotherapeutics for treatment of various types of cancer. In order to overcome cisplatin resistance and toxicity, the drug can be combined with other chemotherapeutics that sensitize tumour cells to cisplatin. The ability of metformin to potentiate cisplatin-mediated killing of cancer cells in vitro, makes it a plausible candidate for combination with cisplatin-based therapy. The aim of this study is...
Prenatal ethanol intoxication and maternal intubation stress alter cell survival and apoptosis in the postnatal development of rat hippocampus
ELİBOL, BİRSEN; BEKER, MERVE; Sahbaz, Cigdern Dilek; Kilic, Ulkan; Jakubowska-Dogru, Ewa (Exeley, Inc., 2019-01-01)
It is well known that the fetal ethanol exposure and prenatal stress may have adverse effects on brain development. Interestingly, some morphological and functional recovery from their teratogenic effects that take place during brain maturation. However, mechanisms that underlie this recovery are not fully elucidated. The aim of this study was to examine whether the postnatal attenuation of fetal alcohol - and maternal stress-induced morphological and functional deficits correlates with compensatory changes...
Functional Application Of İmmununoliposomes Encapsulating Celecoxib On Colon Cancer Cell Lines.
Banerjee, Sreeparna(2010-12-31)
Long term regular use of nonsteroidal anti-inflammatory drugs (NSAIDs) has been correlated with reduced risk of variety of cancers. Celecoxib is a new generation NSAID that can selectively inhibit activity of cyclooxygenase-2 (COX-2) Celecoxib serves as a chemopreventive agent in colorectal cancer. Therefore there is growing interest in developing drug delivery systems for celecoxib, Targeting will be carried out by conjugation of a chimeric monoclonal antibody (Cetuximab) against the Epidermal Growth Fac...
Citation Formats
IEEE
ACM
APA
CHICAGO
MLA
BibTeX
A. Kavas, “Raloxifene delivery systems for osteoporosis treatment,” Ph.D. - Doctoral Program, Middle East Technical University, 2014.
