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Superparamagnetic reconstituted high-density lipoprotein nanocarriers for magnetically guided drug delivery.

Recent Research Articles from UNTHSC - Tue, 03/07/2017 - 07:36
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Superparamagnetic reconstituted high-density lipoprotein nanocarriers for magnetically guided drug delivery.

Int J Nanomedicine. 2017;12:1453-1464

Authors: Sabnis S, Sabnis NA, Raut S, Lacko AG

Abstract
Current cancer chemotherapy is frequently associated with short- and long-term side effects, affecting the quality of life of cancer survivors. Because malignant cells are known to overexpress specific surface antigens, including receptors, targeted drug delivery is often utilized to reduce or overcome side effects. The current study involves a novel targeting approach using specifically designed nanoparticles, including encapsulation of the anti-cancer drug valrubicin into superparamagnetic iron oxide nanoparticle (SPION) containing reconstituted high-density lipoprotein (rHDL) nanoparticles. Specifically, rHDL-SPION-valrubicin hybrid nanoparticles were assembled and characterized with respect to their physical and chemical properties, drug entrapment efficiency and receptor-mediated release of the drug valrubicin from the nanoparticles to prostate cancer (PC-3) cells. Prussian blue staining was used to assess nanoparticle movement in a magnetic field. Measurements of cytotoxicity toward PC-3 cells showed that rHDL-SPION-valrubicin nanoparticles were up to 4.6 and 31 times more effective at the respective valrubicin concentrations of 42.4 µg/mL and 85 µg/mL than the drug valrubicin alone. These studies showed, for the first time, that lipoprotein drug delivery enhanced via magnetic targeting could be an effective chemotherapeutic strategy for prostate cancer.

PMID: 28260891 [PubMed - in process]

Glucocorticoid therapy and ocular hypertension.

Recent Research Articles from UNTHSC - Tue, 03/07/2017 - 07:36
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Glucocorticoid therapy and ocular hypertension.

Eur J Pharmacol. 2016 Sep 15;787:57-71

Authors: Dibas A, Yorio T

Abstract
The projected number of people who will develop age-related macular degeneration in estimated at 2020 is 196 million and is expected to reach 288 million in 2040. Also, the number of people with Diabetic retinopathy will grow from 126.6 million in 2010 to 191.0 million by 2030. In addition, it is estimated that there are 2.3 million people suffering from uveitis worldwide. Because of the anti-inflammatory properties of glucocorticoids (GCs), they are often used topically and/or intravitreally to treat ocular inflammation conditions or edema associated with macular degeneration and diabetic retinopathy. Unfortunately, ocular GC therapy can lead to severe side effects. Serious and sometimes irreversible eye damage can occur as a result of the development of GC-induced ocular hypertension causing secondary open-angle glaucoma. According to the world health organization, glaucoma is the second leading cause of blindness in the world and it is estimated that 80 million will suffer from glaucoma by 2020. In the current review, mechanisms of GC-induced damage in ocular tissue, GC-resistance, and enhancing GC therapy will be discussed.

PMID: 27388141 [PubMed - indexed for MEDLINE]

4-Chlorophenylguanidine is an ASIC3 agonist and positive allosteric modulator.

Recent Research Articles from UNTHSC - Mon, 03/06/2017 - 07:35

4-Chlorophenylguanidine is an ASIC3 agonist and positive allosteric modulator.

J Pharmacol Sci. 2017 Feb 17;:

Authors: Agharkar AS, Gonzales EB

Abstract
Acid-sensing ion channels (ASICs) are proton-sensitive sodium channels that open in response to lowered extracellular pH and are expressed in the central and peripheral nervous systems. The ASIC3 subtype is found primarily in the periphery where the channel mediates pain signals caused by ischemia and inflammation. Here, we provide identify 4-chlorophenylguanidine (4-CPG) as an ASIC3 positive allosteric modulator and newest member of the growing group of guanidine modulators of ASICs. Furthermore, the 4-CPG reversed the effects of ASIC3 desensitization. The molecule 4-CPG offers a novel chemical backbone for the design of new ASIC3 ligands to study ASIC3 in vivo.

PMID: 28259560 [PubMed - as supplied by publisher]

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