Polyamide/Poly(Amino Acid) Polymers for Drug Delivery.

Polymers have always played a critical role in the development of novel drug delivery systems by providing the sustained, controlled and targeted release of both hydrophobic and hydrophilic drugs. Among the different polymers, polyamides or poly(amino acid)s exhibit distinct features such as good biocompatibility, slow degradability and flexible physicochemical modification. The degradation rates of poly(amino acid)s are influenced by the hydrophilicity of the amino acids that make up the polymer.

NAG-PEGylated multilamellar liposomes for BBB-GLUT transporter targeting.

The primary objective of the research study is to investigate Glucose (GLUT) transporter targeting of the drug (Citalopram-Hbr) for increased permeability across the Blood-Brain Barrier (BBB). The current study reports the development, physicochemical characterization, cytotoxicity analysis and in-vitro BBB permeability assessment of the Citalopram-Hbr liposomal formulations. Rat Primary Brain Microvascular Endothelial Cells (RPBECs) were used for cytotoxicity analysis and drug permeability testing.

Ocular Drug Delivery Barriers-Role of Nanocarriers in the Treatment of Anterior Segment Ocular Diseases.

Ocular drug delivery is challenging due to the presence of anatomical and physiological barriers. These barriers can affect drug entry into the eye following multiple routes of administration (e.g.

Discovery of a Novel HDAC2 Inhibitor by a Scaffold-Merging Hybrid Query.

Histone deacetylases (HDACs) are part of a vast family of enzymes with crucial roles in numerous biological processes, largely through their repressive influence on transcription, with serious implications in a variety of human diseases. Among different isoforms, human HDAC2 in particular draws attention as a promising target for the treatment of cancer and memory deficits associated with neurodegenerative diseases. Now the challenge is to obtain a compound that is structurally novel and truly selective to HDAC2 because most current HDAC2 inhibitors do not show isoforms selectivity and suffer from metabolic instability.

Recent patents on ophthalmic nanoformulations and therapeutic implications.

Nanoformulations (NF) are widely explored as potential alternatives for traditional ophthalmic formulation approaches. The effective treatment of ocular diseases using conventional eye drops is often hampered by factors such as: physiological barriers, rapid elimination, protein binding, and enzymatic drug degradation. Combined, these factors are known to contribute to reduced ocular residence time and poor bioavailability.

Development of a sensitive HPLC method to measure in vitro permeability of E- and Z-isomeric forms of thiosemicarbazones in Caco-2 monolayers.

In the current study, we developed a HPLC method to quantitatively measure the permeability of the BpT-based chelators, 2-benzoylpyridine 4-ethyl-3-thiosemicarbazone (Bp4eT) and 2-benzoylpyridine 4-allyl-3-thiosemicarbazone (Bp4aT), across human colorectal adenocarcinoma (Caco-2) monolayers as a model of gut absorption. In aqueous solution, Bp4eT and Bp4aT formed inter-convertible Z and E isomers that were resolved by HPLC. Peak area was linear with respect to chelator concentration.

Novel nanoparticulate gel formulations of steroids for the treatment of macular edema.

Purpose: This article describes the development and characterization of PLGA nanoparticles of dexamethasone (DEX), hydrocortisone acetate (HA), and prednisolone acetate (PA) suspended in thermosensitive gels indicated for the treatment of macular edema (ME).

Methods: Nanoparticles were prepared by oil-in-water (O/W) emulsion and dialysis methods using PLGA 50:50 and PLGA 65:35. These particles were characterized for entrapment efficiency, size distribution, surface morphology, crystallinity, and in vitro release.

Expression of multidrug resistance associated protein 5 (MRP5) on cornea and its role in drug efflux.

Purpose: The purpose of this manuscript is to investigate the presence of nucleoside/nucleotide efflux transporter in cornea and to evaluate the role in ocular drug efflux.

Methods: RT-PCR, immunoprecipitation followed by Western blot analysis and immunostaining were employed to establish molecular presence of multidrug resistance associated protein 5 (MRP5) on cornea. Corneal efflux by MRP5 was studied with bis(POM)-PMEA and acyclovir using rabbit and human corneal epithelial cells along with MRP5 over expressing cells (MDCKII-MRP5).

Molecular expression and functional evidence of a drug efflux pump (BCRP) in human corneal epithelial cells.

Purpose: Breast Cancer Resistance Protein (BCRP) belongs to the family of efflux transporters involved in drug efflux leading to drug resistance. The objective of this study was to explore physical barriers for ocular drug absorption and to verify the presence and possible role of BCRP as a barrier for ocular drug resistance.

Methods: Transfected human corneal epithelial cells (SV40-HCEC) were selected as an in vitro model for corneal epithelium with MDCKII-BCRP as positive control.

Molecular evidence and functional expression of a novel drug efflux pump (ABCC2) in human corneal epithelium and rabbit cornea and its role in ocular drug efflux.

Cornea is considered as a major barrier for ocular drug delivery. Low ocular bioavailability of drugs has been attributed primarily to low permeability across corneal epithelium, thus leading to sub-therapeutic concentrations of drug in the eye and treatment failure. The role of drug efflux proteins, particularly the P-glycoprotein (P-gp) in ocular drug bioavailability has been reported.

Molecular evidence and functional expression of multidrug resistance associated protein (MRP) in rabbit corneal epithelial cells.

Multidrug resistance associated protein (MRP) is a major family of efflux transporters involved in drug efflux leading to drug resistance. The objective of this study was to explore physical barriers for ocular drug absorption and to verify if the role of efflux transporters. MRP-2 is a major homologue of MRP family and found to express on the apical side of cell membrane.

The functional role of C-reactive protein in aortic wall calcification.

As an ongoing effort to elucidate the mechanisms involved in bioprosthetic heart valve (BHV) calcification, the role of C-reactive protein (CRP) in the tissue calcification process was investigated. The profile of calcium-associated proteins (CAP) on glutaraldehyde-preserved (0.6%) porcine aortic wall, which were subcutaneously implanted in rats for up to 8 weeks, showed a temporal appearance pattern.