Abstract:
:Intravitreal sustained delivery of corticosteroids such as dexamethasone is an effective means of treating a number of ocular diseases, including diabetic retinopathy, uveitis, and age-related or diabetic macular edema. There are currently marketed devices for this purpose, yet only one, Ozurdex, is degradable. In vitro release of dexamethasone from the Ozurdex device is limited to approximately 30 days, however. It was the objective of this study to examine the potential for prolonged and sustained release of a corticosteroid in vitro from a degradable polymer prepared from terminally acrylated star co- and ter-prepolymers composed of d,l-lactide, ε-caprolactone, and trimethylene carbonate co-photo-cross-linked with poly(ethylene glycol) diacrylate. Through manipulation of the network polymer glass transition temperature and degradation rate, a sustained release of triamcinolone was achieved, with an estimated release duration greater than twice that of the Ozurdex system. Moreover, a period of nearly constant release was obtained using a network prepared from 5000 Da star-poly(trimethylene carbonate-co-d,l-lactide) triacrylate (3:1 trimethylene carbonate:d,l-lactide) co-cross-linked with 700 Da poly(ethylene glycol diacrylate). These formulations show promise as implantable, intravitreal corticosteroid delivery devices.
journal_name
Mol Pharmjournal_title
Molecular pharmaceuticsauthors
Amsden BG,Marecak Ddoi
10.1021/acs.molpharmaceut.6b00358subject
Has Abstractpub_date
2016-09-06 00:00:00pages
3004-12issue
9eissn
1543-8384issn
1543-8392journal_volume
13pub_type
杂志文章abstract::The effect of tertiary butyl alcohol (TBA) as a cosolvent on the phase behavior of mannitol in frozen and freeze-dried systems was characterized using differential scanning calorimetry (DSC) and X-ray diffractometry (XRD; laboratory and synchrotron sources). Solutions of mannitol (2 and 5% w/w) in TBA-water systems of...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.0c00492
更新日期:2020-08-03 00:00:00
abstract::The particle shape of the drug delivery systems had a strong impact on their in vitro and in vivo performance, but there was limited availability of techniques to produce the specific shaped drug carriers. In this article, the novel methotrexate (MTX) decorated MPEG-PLA nanobacillus (MPEG-PLA-MTX NB) was prepared by t...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp500464b
更新日期:2015-04-06 00:00:00
abstract::Though metastasis is considered an inefficient process, over 90% of cancer related deaths are attributed to the formation of secondary tumors. Thus, eliminating circulating cancer cells could lead to improved patient survival. This study was aimed at exploiting the interactions of cancer cells with selectins under flo...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp300073j
更新日期:2012-08-06 00:00:00
abstract::Cancer is a leading cause of death within developed nations, and part of this morbidity is due to difficulties associated with its treatment. Currently, anticancer therapy relies heavily upon the administration of small molecule cytotoxic drugs that attack both cancerous and noncancerous cells due to limited selectivi...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章,评审
doi:10.1021/mp2005966
更新日期:2012-03-05 00:00:00
abstract::Saquinavir mesylate (SQV) is the first-in-class and prototypical HIV protease inhibitor (PI) used in the treatment of HIV infection. SQV undergoes extensive hepatic metabolism and intestinal and bile secretion, and has poor and variable oral bioavailability. In previous studies, our group and others have described the...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp0340136
更新日期:2004-01-12 00:00:00
abstract::The reaction of singlet oxygen with water to form hydrogen peroxide was catalyzed by antibodies and has been termed as the antibody catalyzed water oxidation pathway (ACWOP) (Nieva and Wentworth, Trends Biochem. Sci. 2004, 29, 274-278; Nieva et al. Immunol. Lett. 2006, 103, 33-38). While conserved and buried tryptopha...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp300418r
更新日期:2013-01-07 00:00:00
abstract::A combination of microbubbles (MBs) and ultrasound (US) is an emerging method for noninvasive and targeted enhancement of anti-cancer drug uptake. This method showed an increase local drug extravasation in tumor tissue while reducing the systemic adverse effects in various tumor models. The present study aims to evalu...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.9b00416
更新日期:2019-09-03 00:00:00
abstract::Fluid bed coating has been shown to be a suitable manufacturing technique to formulate poorly soluble drugs in glass solutions. Layering inert carriers with a drug-polymer mixture enables these beads to be immediately filled into capsules, thus avoiding additional, potentially destabilizing, downstream processing. In ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.6b01023
更新日期:2017-04-03 00:00:00
abstract::Here, we report the antiproliferative/cytotoxic properties of 8-hydroxyquinoline (8-HQ) derivatives on HeLa cells in the presence of transition metal ions (Cu(2+), Fe(3+), Co(2+), Ni(2+)). Two series of ligands were tested, the arylvinylquinolinic L1-L8 and the arylethylenequinolinic L9-L16, which can all interact wit...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp400592n
更新日期:2014-04-07 00:00:00
abstract::Adsorption of antibody therapeutics to air-liquid interfaces can enhance aggregation, particularly when the solution does not contain protective surfactant or when the surfactant is diluted as occurs during preparation of intravenous infusion bags. The ability to predict an antibody's propensity for interfacially medi...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.5b00089
更新日期:2015-09-08 00:00:00
abstract::The controversy surrounding the use of diphtheria toxin (DT) as a therapeutic agent against tumor cells arises mainly from its unexpected harmfulness to healthy tissues. We encoded the cytotoxic fragment A of DT (DTA) as an objective gene in the Light-On gene-expression system to construct plasmids pGAVPO (pG) and pU5...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.9b01038
更新日期:2020-01-06 00:00:00
abstract::Lipid-based nanoparticles are considered as promising candidates for delivering siRNA into the cytoplasm of targeted cells. However, in vivo efficiency of these nanoparticles is critically dependent on formulation strategies of lipid-siRNA complexes. Adsorption of serum proteins to lipid-siRNA complexes and its charge...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp500677x
更新日期:2015-02-02 00:00:00
abstract::We evaluated the chemical and enzymatic stabilities of prodrugs containing methoxy, ethoxy and propylene glycol linkers in order to find a suitable linker for prodrugs of carboxylic acids with amino acids. l-Valine and l-phenylalanine prodrugs of model compounds (benzoic acid and phenyl acetic acid) containing methoxy...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900084v
更新日期:2009-09-01 00:00:00
abstract::BCS classification is a vital tool in the development of both generic and innovative drug products. The purpose of this work was to provisionally classify the world's top selling oral drugs according to the BCS, using in silico methods. Three different in silico methods were examined: the well-established group contri...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp400485k
更新日期:2013-11-04 00:00:00
abstract::Subcutaneous allergen-specific immunotherapy (SCIT) qualifies as a promising approach for the permanent cure of IgE-mediated airway allergies, which can often manifest into allergic rhinitis and other allergic respiratory diseases. SCIT entails repeated administration of a high allergen dose into the subcutaneous (sc)...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.0c00447
更新日期:2020-08-03 00:00:00
abstract::Progesterone receptor (PR) is a significant biomarker in diseases such as endometriosis and breast, ovarian, and uterine cancers that is associated with disease prognosis and therapeutic efficacy. While receptor status is currently determined by immunohistochemistry assays, the development of noninvasive PR imaging ag...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp200219e
更新日期:2011-08-01 00:00:00
abstract::Novel multivalent copper(II)-conjugated phosphorus dendrimers and their corresponding mononuclear copper(II) complexes were synthesized, characterized, and screened for antiproliferative activity against human cancer cell lines. Selected copper ligands were grafted on the surface of phosphorus dendrimers of generation...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp4000184
更新日期:2013-04-01 00:00:00
abstract::Constitutively activated signal transducer and activator of transcription-3 (STAT3) in tumor and dendritic cells (DCs) plays a critical role in tumor-induced immunosuppression. This is considered a major challenge in effective immunotherapy of cancer. Herein we describe the development of a polymeric nanocarrier for t...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900145g
更新日期:2010-04-05 00:00:00
abstract::In this study, a facile strategy for efficient codelivery of gene and drug was developed. Using a coprecipitation method, doxorubicin hydrochloride (DOX), an antitumor drug, and p53 expression plasmid were encapsulated in alginate/CaCO(3)/DNA/DOX nanoparticles with high encapsulation efficiency. The in vitro cell inhi...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp3002123
更新日期:2012-10-01 00:00:00
abstract::Cancer research regarding near-infrared (NIR) agents for chemothermal therapy (CTT) has shown that agents with specific functions are able to inhibit tumor growth. The aim of current study was to optimize CTT efficacy for treatment of colorectal cancer (CRC) by exploring strategies which can localize high temperature ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.7b00315
更新日期:2017-08-07 00:00:00
abstract::This study aims to investigate the crystallization behavior and molecular dynamics of amorphous griseofulvin (GSF) in the presence of low-concentration poly(ethylene oxide) (PEO). We observe that the addition of 3% w/w PEO remarkably increases the crystal growth rate of GSF by two orders of magnitude in both the super...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.7b00097
更新日期:2017-07-03 00:00:00
abstract::The primary cause of mortality for glioblastoma (GBM) is local tumor recurrence following standard-of-care therapies, including surgical resection. With most tumors recurring near the site of surgical resection, local delivery of chemotherapy at the time of surgery is a promising strategy. Herein drug-loaded polymer s...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.7b01114
更新日期:2018-03-05 00:00:00
abstract::Mucus layer, a selective diffusion barrier, has an important effect on the fate of drug delivery systems in the gastrointestinal tract. To study the fate of microemulsions in the mucus layer, four microemulsion formulations with different particle sizes and lipid compositions were prepared. The microemulsion-mucin int...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp500475y
更新日期:2015-03-02 00:00:00
abstract::The use of adult stem cells for therapeutic purposes has met with great success in recent years. Among several types of adult stem cells, mesenchymal stem cells (MSCs) derived from bone marrow (BM) and other sources have gained popularity for basic research and clinical applications because of their therapeutic potent...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章,评审
doi:10.1021/mp200135e
更新日期:2011-10-03 00:00:00
abstract::Topical delivery of small interfering RNA (siRNA) can be an attractive method for the treatment of skin diseases and improving the quality of life of patients. However, it is difficult for siRNA to pass through the two major barriers of the skin: the stratum corneum (SC) and tight junctions. We have previously reporte...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.0c00997
更新日期:2021-01-04 00:00:00
abstract::Solid lipid nanoparticles (SLNs) are one of the most promising nanocarriers to increase the oral absorption of drugs with poor solubility and low permeability. However, the absorption mechanism of SLNs remains incomplete and thus requires further careful consideration. In this study, positively charged chitosan (CS) m...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.6b00226
更新日期:2016-08-01 00:00:00
abstract::Polymeric systems have been extensively studied as polyelectrolyte complexes to enhance the cellular delivery and transfection efficiency of genetic materials, such as plasmid DNA (pDNA). Here, self-assembled nanoparticles were formulated by complexation of hyaluronic acid (HA)-conjugated poly(ethylene glycol) (HA-PEG...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.8b00904
更新日期:2019-01-07 00:00:00
abstract::The purpose of this study was to determine the effect of PEGylation on the interaction of poly(amidoamine) (PAMAM) dendrimer nanocarriers (DNCs) with in vitro and in vivo models of the pulmonary epithelium. Generation-3 PAMAM dendrimers with varying surface densities of PEG 1000 Da were synthesized and characterized. ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp500662z
更新日期:2015-03-02 00:00:00
abstract::Oral chemotherapy with SN38 is restricted by its poor solubility in gastrointestinal (GI) fluids and low permeability. Here we report the oral delivery of SN38 by a combined lipophilic prodrug and lipid-based formulation strategy. A lead lipophilic prodrug of SN38, SN38-undecanoate (SN38-unde20), was incorporated into...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.6b00591
更新日期:2016-10-03 00:00:00
abstract::2-Methoxyestradiol (2MeO-E2) is an endogenous metabolite of estrogen which was initially considered to be inactive. During the last few decades it has been shown that 2MeO-E2 is a promising anticancer drug. In vitro experiments have demonstrated that it has several anticancer activities, and potential to alleviate hyp...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章,评审
doi:10.1021/mp100190f
更新日期:2010-12-06 00:00:00