AC Biosusceptometry as a Tool for Monitoring the Gastrointestinal Transit of Multiparticulate Drug Delivery System

Drug delivery systems based on natural polysaccharides, such as chitosan (CS) and pectin (PC), rather than on synthetic polymers, have been widely studied. Some reasons for that are low toxicity and costs and high biodegradability of the formers. A multiparticulate system based on CS and PC was developed in our laboratories, including the addition of an enteric polymer, cellulose acetate phtalate (CAP). Such improvement promoted stronger gastric and enteric resistances, as assessed in vitro, making the systems more selective to enzymatic degradation in the colon. Although in vitro dissolution tests can simulate some properties concerning the gastrointestinal transit (GT), collaborating to characterize the systems behavior in the biological fluids, frequently they do not result in satisfactory in vitro/in vivo correlations. The objective of this work was to follow in vivo the GT of the particles developed by means of AC biosusceptometry (ACB), a non-invasive and of low cost methodology. The particles containing ferrite in powder form were prepared by complex coacervation using an ideal 3:1:1 mass ratio for PC:CS:CAP. The magnetic particles were administered to healthy volunteers by oral route. The GT was monitored by using multi-sensor ACB system and the signal acquisition was performed every IS min until the colonic region was reached. By means of ACB technique, it was possible to acquiring images generated by the magnetic particles within the whole gastrointestinal tract including the colonic region. Variable particles transit times were observed among the volunteers, but without interference on the mapping of the particles until the colonic region. The particles were able to produce magnetic field strong enough to generate signals adequate for mapping the particles. The results suggest that integral particles reached the colon, after they resisted against gastric and enteric media. Studies associating transit time and in vivo drug release are in development in order to confirm the efficiency of the systems.

Natural rubber latex used as drug delivery system in guided bone regeneration (GBR)

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

In vitro characterization of coevaporates containing chitosan for colonic drug delivery

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Biocompatibility of a chlorhexidine local delivery system in a subcutaneous mouse model

Objective: This study aimed evaluating histologically and histomorphometrically the response of the conjunctive tissue face to the implant of chlorhexidine chips in the subcutaneous tissues of rats. Study Design: In this research 35 male rats Wistar were used to analyze the biocompatibility and the degradation process of chlorhexidine chip. In each animal, it was made 2 incisions for subcutaneous implantation of chlorhexidine chip (test group) and a polytetrafluorethylene membrane (control group). The morphological changes in subcutaneous implantations were assessed after 1, 3, 5, 7, 10, 14, 21 days. The data were submitted to Friedman nonparametric test to analyze the comparisons among observation periods and to allow the comparison among groups. Results: Differences were found in the analysis of the inflammatory response when comparing the tested materials (p values <= 0.05). In test group was observed hemorrhage, edema and intense inflammatory infiltrate predominantly neutrophilic around material. From 3-day and subsequent periods was verified granulation tissue externally at this infiltrate. From 10-day on was observed crescent area of degradation of chlorhexidine chip, associated with neutrophilic and macrophagic infiltrate, that maintained until 21-day. In the control group, moderate inflammatory infiltrate was observed initially, predominantly polymorphonuclear, edema and granulation tissue 3-day period. The inflammatory infiltrate was gradually replaced for granulation tissue, culminating in a fibrous capsule. Giant multinucleate cells situated at contact interface with the coating was examined since 3-day and persisted until 21-day. Conclusion: The chlorhexidine chip induces an intense acute inflammatory response at subcutaneous tissue of rats. Therefore, at conditions of this study was not biocompatible.

Liposomes and micro/nanoparticles as colloidal carriers for nasal drug delivery

The use of the nasal route for drug delivery has attracted much interest in recent years in the pharmaceutical field. Local and principally systemic drug delivery can be achieved by this route of administration. But the nasal route of delivery is not applicable to all drugs. Polar drugs and some macromolecules are not absorbed in sufficient concentration due to poor membrane permeability, rapid clearance and enzymatic degradation into the nasal cavity. Thus, alternative means that help overcome these nasal barriers are currently in development. Absorption enhancers such as phospholipids and surfactants are constantly used, but care must be taken in relation to their concentration. Drug delivery systems including liposomes, cyclodextrins, micro- and nanoparticles are being investigated to increase the bioavailability of drugs delivered intranasally. This review article discusses recent progress and specific development issues relating to colloidal drug delivery systems in nasal drug delivery. © 2006 Bentham Science Publishers Ltd.

Nanotechnology-based drug delivery systems for treatment of hyperproliferative skin diseases - a review

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Preparation, characterization and evaluation of drug-delivery systems: Pectin and mefenamic acid films

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Nanotechnology-based drug delivery systems for melanoma antitumoral therapy: a review

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Polyacrylic acid polymers hydrogels intended to topical drug delivery: preparation and characterization

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Modeling a system of phosphated cross-linked high amylose for controlled drug release. Part 2: Physical parameters, cross-linking degrees and drug delivery relationships

High amylose cross-linked to different degrees with sodium trimetaphosphate by varying base strength (2% or 4%) and contact time (0.5-4 h) was evaluated as non-compacted systems for sodium diclophenac controlled release. The physical properties and the performance of these products for sodium diclophenac controlled release from non-compacted systems were related to the structures generated at each cross-linking degree. For samples at 2% until 2 h the swelling ability, G' and eta* values increased with the cross-linking degree, because the longer polymer chains became progressively more entangled and linked. This increases water uptake and holding, favoring the swelling and resulting in systems with higher viscosities. Additionally, the increase of cross-linking degree should contribute for a more elastic structure. The shorter chains with more inter-linkages formed at higher cross-linking degrees (2%4h and 4%) make water caption and holding difficult, decreasing the swelling, viscosity and elasticity. For 2% samples, the longer drug release time exhibited for 2%4h sample indicates that the increase of swelling and viscosity contribute for a more sustained drug release, but the mesh size of the polymeric network seems to be determinant for the attachment of drug molecules. For the 4% samples, smaller meshes size should determine less sustained release of drug. (C) 2008 Elsevier B.V. All rights reserved.

Development and characterization of biocompatible isotropic and anisotropic oil-in-water colloidal dispersions as a new delivery system for methyl dihydrojasmonate antitumor drug

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Mucoadhesive drug delivery systems

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Chitosan-pectin multiparticulate systems associated with enteric polymers for colonic drug delivery

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Oil-in-water lecithin-based microemulsions as a potential delivery system for amphotericin B

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Development and in vitro evaluation of coated pellets containing chitosan to potential colonic drug delivery

In this work pellets containing chitosan for colonic drug delivery were developed. The influence of the polysaccharide in the pellets was evaluated by swelling, drug dissolution and intestinal permeation studies. Drug-loaded pellets containing chitosan as swellable polymer were coated with an inner layer of Kollicoat® SR 30 D and an outer layer of the enteric polymer Kollicoat® MAE 30 DP in a fluidized-bed apparatus. Metronidazole released from pellets was assessed using Bio-Dis dissolution method. Swelling, drug release and intestinal permeation were dependent on the chitosan and the coating composition. The drug release data fitted well with the Weibull equation, indicating that the drug release was controlled by diffusion, polymer relaxation and erosion occurring simultaneously. The film coating was found to be the main factor controlling the drug release and the chitosan controlling the drug intestinal permeation. Coated pellets containing chitosan show great potential as a system for drug delivery to the colon. © 2012 Elsevier Ltd.