Poor drug encapsulation efficiency and rapid release of the encapsulated drug limit the use of nanoparticles in biomedical applications involving water-soluble drugs. We have developed a novel polymer-surfactant nanoparticle formulation, using the anionic surfactant Aerosol OT (AOT) and polysaccharide polymer alginate, for sustained release of water-soluble drugs. Particle size of nanoparticles...

Poly(ADP-ribose)polymerase-1 (PARP-1) is an important target for drug design for several therapeutic applications. 5-Aminoisoquinolin-1-one (5-AIQ) is a highly water-soluble lead compound; synthetic routes to 3-substituted analogues were explored. Tandem Hurtley coupling of β-diketones with 2-bromo-3-nitrobenzoic acid, retro-Claisen acyl cleavage and cyclisation gave the corresponding 3-substit...

A novel approach to hyperbranched polymers is presented in this work. Hyperbranched polyesters with a large amount of terminal hydroxyl groups are prepared by a one-pot synthesis from commercially available AB-type and CD(n)-type monomers (n >/= 2). In this paper, Michael addition of diethanolamine (CD(2)) or N-methyl-d-glucamine (CD(5)) to methyl acrylate (AB) generates dominantly AD(n)-type i...

Guaifenesin, a highly water-soluble active (50 mg/mL), classified as a BCS class I drug.Owing to its poor flowability and compressibility, formulating tablets especially high-dose one,may be a challenge. Direct compression may not be feasible. Bilayer tablet technology appliedto Mucinex®, endures challenges to deliver a robust formulation. To overcome challengesinvolved in bilayer-tablet manufa...

Cyclodextrins and liposomes have been used in recent years as drug delivery vehicles, improving the bioavailability and therapeutic efficacy of many poorly water-soluble drugs. In this study, we used two approaches to enhance the availability of the poorly water-soluble antibiotic, clarithromycin, by inclusion complex formation and by liposome-encapsulation. We examined the efficacies of these ...

Surface solid dispersion with insoluble carriers is considered a recently developed technique, widely applied for the enhancement of solubility and dissolution of poorly water soluble drugs. The objective of this research article is to study the effect of surface solid dispersion of ketoprofen with colloidal silicon dioxide (Aerosil 200) on the dissolution rate. Surface solid dispersion (Adsorb...

A dendrimer described as a macromolecule characterized by its highly branched 3D structure which provides a high degree of surface functionality and versatility. Dendrimers also referred to as the “Polymers of the 21 century.” Dendrimers components, namely (1) an initiator core (2) Interior layers (generations) composed of repeating units, radically attached to the interior core. (3) Exterior (...

Clarithromycin (CLA), a broad-spectrum macrolide, is a poorly soluble drug with dissolution rate limited absorption. The aim of this investigation was to prepare CLA nanoparticles from a ternary ground mixture in the presence of sodium lauryl sulfate (SLS) and polyvinyl pyrrolidone (PVP) as co-grinding water-soluble compounds, in order to improve the drug dissolution rate. Different weight rati...

Clarithromycin (CLA), a broad-spectrum macrolide, is a poorly soluble drug with dissolution rate limited absorption. The aim of this investigation was to prepare CLA nanoparticles from a ternary ground mixture in the presence of sodium lauryl sulfate (SLS) and polyvinyl pyrrolidone (PVP) as co-grinding water-soluble compounds, in order to improve the drug dissolution rate. Different weight rati...

The effect of ionic and non-ionic excipients and additives as modulators of swelling and erosion kinetics and verapamil HCl release from guar-based matrix tablets was investigated. Tablet dissolution, erosion and water uptake studies were carried out using a modified USP 23 Apparatus 2 method. The kinetics of gel strength and texture development were studied by textural analysis. Near linear dr...