Paracetamol is a sparingly soluble bitter tasting drug. It is widely used as an analgesic and antipyretic. Complexation of drug with different cyclodextrins (?, ? and HP-?-CD) was attempted to improve solubility of Paracetamol. During the drug excipient interaction studies, ?, ? cyclodextrins elicited analytical interference and showed considerable absorbance at ?max (243.5 nm) of Paracetamol w...

Paracetamol is a sparingly soluble bitter tasting drug. It is widely used as an analgesic and antipyretic. Complexation of drug with different cyclodextrins (?, ? and HP-?-CD) was attempted to improve solubility of Paracetamol. During the drug excipient interaction studies, ?, ? cyclodextrins elicited analytical interference and showed considerable absorbance at ?max (243.5 nm) of Paracetamol w...

The inclusion complexation behavior of azadirachtin with several cyclodextrins and their methylated derivatives has been investigated in both solution and the solid state by means of XRD, TG-DTA, DSC, NMR, and UV-vis spectroscopy. The results show that the water solubility of azadirachtin was obviously increased after resulting inclusion complex with cyclodextrins. Typically, beta-cyclodextrin ...

Water-cast films of two ethers of cellulose, hydroxypropylcellulose (HPC) and hydroxyethylcellulose (HEC), with dispersed silica particles, were deposited on flat substrates. X-ray specular reflectivity was used to characterize the structure of these solid ca. 1000 Å thick films as a function of the added colloidal fraction. It was shown that the structural changes resulting from increasing amo...

From a pharmacophore model of bicyclic heterocycles as aromatase inhibitors we have designed three series of imidazo[1,2-a]pyridine derivatives. The synthesis and the spectroscopy determination of various compounds are reported. The crystal data of one of these compounds (10b) was obtained. The aromatase inhibition potency was evaluated in vitro and no activity was found.

The complex nature of in vivo gene transfer establishes the need for multifunctional delivery vectors capable of meeting these challenges. An additional consideration for clinical translation of synthetic delivery formulations is reproducibility and scale-up of materials. In this review, we summarize our work over the last five years in developing a modular approach for synthesizing peptide-bas...

Employment or Leadership: D. Mant, Oxford University. Consultant or Advisory Role: None declared. Stock Ownership: None declared. Honoraria: None declared. Research Funding: Funding from the U.K. National Institute for Health Research Health Technology Assessment (NIHR HTA) program (project no. 99/10/99) to the Nuffield Department of Primary Care Health Sciences, University of Oxford. Expert Te...

Despite intensive study, the molecular mechanism for cell toxicity of N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-bound doxorubicin remains unclear. Moreover, the ability of the released drug to accumulate in the nucleus has also been questioned. We have hypothesized that the pattern of cell cycle progression is a useful indicator for the presence of free doxorubicin in the nucleus and i...

A poly(ethylene glycol) (PEG) macromolecular chain transfer agent (macro-CTA) is prepared in high yield (>95%) with 97% dithiobenzoate chain-end functionality in a three-step synthesis starting from a monohydroxy PEG113 precursor. This PEG113-dithiobenzoate is then used for the reversible addition-fragmentation chain transfer (RAFT) aqueous dispersion polymerization of 2-hydroxypropyl methacryl...

We describe design, synthesis, physico-chemical characterization and preliminary biological evaluation of micelle-forming polymer drug conjugates with controlled drug release intended for tumor treatment. The structure of the conjugates was designed to enable tumor tissueand cell-specific drug release and micelle disassembly to avoid side effects accompanying classic chemotherapy and guarantee ...