Spartium junceum aromatic water: chemical composition and antitumor activity.

The purpose of this study was to analyse the chemical composition of Spartium junceum L. (also known as Spanish Broom) aromatic water and to evaluate its cytotoxic activity against a series of human cancer cell lines (melanoma: RPMI 7932; leukemia: K562; breast cancer cell: MCF7-Bart and MCF7-ICLC, colon adenocarcinoma: SW480). The results show that the aromatic water was cytotoxic toward the tumor cell lines analyzed (RPMI 7932, K562, MCF7-Bart, MCF7-ICLC, SW480), while it did not appreciably alter the viability of normal keratinocytes (NCTC 2544) suggesting its potential use as an antitumor agent for cancer treatment and/or prevention.

Albumin nanoparticles carrying cyclodextrins for nasal delivery of the anti-Alzheimer drug tacrine.

Peroral administration of tacrine, the first acetylcholinestearse inhibitor licensed for the treatment of Alzheimer's disease, is associated with low bioavailability, due to an extended first-pass methabolism, short elimination half-life and hepatotoxicity. Nasal drug delivery may reduce the degree of these problems. Tacrine hydrochloride nasal delivery is here investigated by means of albumin nanoparticles carrying beta cyclodextrin and two different beta cyclodextrin derivatives (hydroxypropyl beta cyclodextrin and sulphobutylether beta cyclodextrin).

Chitosan-based hydrogels for nasal drug delivery: from inserts to nanoparticles.

Importance Of The Field: Chitosan represents a multifunctional polymer, featuring both mucoadhesive and permeation-enhancing properties and therefore is a widely studied excipient for mucosal drug delivery. As regards nasal administration, chitosans have been used for the preparation of gels, solid inserts, powders and nanoparticles in which a three-dimensional network can be recognized.

Areas Covered In This Review: This review provides a discussion of the different nasal dosage forms based on chitosan hydrogels.

Hydroxypropylmethylcellulose films for prolonged delivery of the antipsychotic drug chlorpromazine.

Objectives: The aim of this study was to develop transdermal films based on hydroxypropylmethylcellulose with the purpose of improving transdermal permeation of chlorpromazine hydrochloride, an antipsychotic drug used to alleviate the symptoms and signs of psychosis.

Methods: Hydroxypropylmethylcellulose films were prepared and evaluated for their drug content, film thickness, residual water content and bioadhesive properties. In-vitro permeation experiments were performed in the absence and in the presence of permeation enhancers (oleic acid, polysorbate 80, or both) with the purpose of improving drug availability.

Freeze-dried chitosan/pectin nasal inserts for antipsychotic drug delivery.

The objective of this investigation was the development of chitosan/pectin based nasal inserts to improve bioavailability of antipsychotic drugs in the treatment of psychotic symptoms. In fact, the nasal route of administration ensures systemic availability avoiding the first-pass metabolism and obtaining more efficacious treatments. Chitosan/pectin polyelectrolyte complexes were prepared at pH 5.

Gastroresistant microcapsules: new approaches for site-specific delivery of ketoprofen.

Ketoprofen is a potent non-steroidal anti-inflammatory drug (NSAID) that has been widely used in the treatment of rheumatoid arthritis and other related conditions. However, it carries the risk of undesirable systemic side effects and gastrointestinal irritation at the usual dose of oral administration. The aim of this study was to prepare and evaluate gastroresistant microcapsules containing ketoprofen.

Novel mucoadhesive nasal inserts based on chitosan/hyaluronate polyelectrolyte complexes for peptide and protein delivery.

Objectives: The purpose of this study was the preparation and characterisation of mucoadhesive nasal inserts based on chitosan/hyaluronate polyelectrolyte complexes prepared at various pHs and at different molar ratios.

Methods: A suspension of chitosan/hyaluronate complexes with or without the model drugs (vancomycin or insulin) was lyophilised into small inserts. Complexation yield, FT-IR spectra and thermogravimetric analysis were used to study the degree of interactive strength between polyions.

Pectin-based microspheres for colon-specific delivery of vancomycin.

Objectives: The aim of this study was to describe a colon-specific delivery system based on pectin hydrogels formed by complexation with chitosan.

Methods: Hydrogels were prepared at different weight ratios (4:1, 7:1, 10:1; pectin/chitosan), loaded with vancomycin hydrochloride (2:1, 4:1; polymer/drug weight ratio) and collected by spray-drying. The microspheres obtained were characterized in terms of morphology, swelling behaviour, mucoadhesive properties and drug loading efficiency.

Determination of insulin in innovative formulations by means of LC coupled to fluorescence detection.

A fast and simple method based on LC with fluorescence detection has been developed for the determination of insulin in innovative formulations consisting of microparticles and inserts for oral and nasal drug administration, respectively. A reverse-phase C8 column and a mobile phase composed of pH 3.7, 40 mM sodium sulphate solution and acetonitrile (24%, v/v) were employed.

Chitosan salts coated with stearic acid as colon-specific delivery systems for vancomycin.

Site-specific controlled release systems have been extensively investigated during the last decade. The aim of this study was to describe a pH-dependent drug release system based on chitosan salts for vancomycin hydrochloride delivery. Chitosan salts with succinic acid, adipic acid, and suberic acid were prepared by spray-drying and were coated with stearic acid by the same technique.

New environmental sensitive system for colon-specific delivery of peptidic drugs.

Nano and micro preparative technologies for the realization of pharmaceutical carriers represent an actual strategy for reaching the therapeutic success of drugs, particularly in the case of peptidic drugs. Vancomycin is here entrapped in carriers composed by a swellable, mucoadhesive and biodegradable albumin core, coated with fatty acids able to improve a colon-specific release. Bovine serum albumin nanospheres (core) were prepared from protein solutions using a coacervation method followed by thermal cross-linking at different temperature, or from protein solutions at different pHs using a coacervation method followed by thermal cross-linking at 75 degrees C.

Substituted polyvinylalcohol as a drug carrier for beta-carotene.

The objective of this study was to evaluate the in vitro characteristics of polyvinylalcohol 10,000 (PVA10,000) and polyvinylalcohol 15,000 (PVA15,000) substituted with different alkyl chains (Iodododecane, Bromotetradecane) and crosslinked with Bis-chloro-ethoxy-ethane as an injectable drug carrier. beta-carotene was used as a lipophilic model drug. Physical mixtures of the drug and the spray-dried polymers were prepared and the release of the drug from the mixtures was evaluated in vitro at pH 7.

pH-sensitive polymeric physical-mixture for possible site-specific delivery of ibuprofen.

Delivery of drugs to the large bowel has been extensively investigated during the last decade. The aim of this work was to study polymethacrylic acid-co-methylmethacrylate substituted with fatty acids (lauric, myristic, palmitic and stearic) at 20% substitution degree (PMA-LAUR20, PMA-MIR20, PMA-PALM20 and PMA-STEA20) or 40% substitution degree (PMA-LAUR40, PMA-MIR40, PMA-PALM40 and PMA-STEA40) for preparing a pH-sensitive physical mixture for site-specific delivery of ibuprofen chosen as a model drug. The preparation and characterization of the substituted polymers were described.

Polyvinylalcohol substituted with triethyleneglycolmonoethylether as a new material for preparation of solid dispersions of hydrophobic drugs.

Among the different methods used to increase the aqueous drug solubility, the preparation of a solid dispersion with a soluble carrier represents an interesting formulative approach. We substituted polyvinylalcohol with triethyleneglycolmonoethylether and obtained a suitable material for the formulation of a solid dispersion of progesterone, by spray-drying. In particular, we evaluated the influence of the polyvinylalcohol substitution degree and the polymer-drug weight ratios in the preparative mixture on the progesterone dissolution rate in the aqueous environment.