Biomedical subjects

P Giunchedi

Publications and source records attributed to P Giunchedi.

28 records · Page 2Linked to original sources

PubMedDate not supplied

Preparation and analgesic activity of Eudragit RS100 microparticles containing diflunisal.

Two different techniques, the quasi-emulsion solvent diffusion method and spray drying that provide polar and nonpolar preparation environments, were used to prepare microspheres from Eudragit RS100 (RS) (acrylic/methacrylic copolymer) incorporating the nonsteroidal anti-inflammatory drug diflunisal. The effects of pH on the preparation medium and drug/polymer ratio on production yield and drug incorporation, as well as on the in vitro drug release at pH 1.2 and 6.8 from tabletted microparticles, were evaluated. The drug-polymer interactions and the effect of diflunisal incorporation in the polymer matrix on drug crystallinity have been evaluated by using differential scanning calorimetry, IR and ultraviolet spectroscopy, x-ray diffraction, and microscopy analysis. A preliminary biological assay confirmed that diflunisal maintains its analgesic activity after intraperitoneal administration to rats.

Acrylic Resins↗

PubMedDate not supplied

Evaluation of spray drying as a method for polylactide and polylactide-co-glycolide microsphere preparation.

Polylactide and polylactide-co-glycolide microspheres containing a lipophilic model drug (vitamin D3) were prepared by spray drying. The purpose of this work is to evaluate the efficacy of spray drying as a method for microsphere preparation. The study was carried out on five different polymers of lactide class: poly-L-lactide 57000 MW, poly-D,L-lactide 209,000 MW, 109,000 MW, 16,000 MW, and polylactide-co-glycolide 22,000 MW. The process conditions were experimentally assessed for each polymer used. The microspheres obtained were characterized for their shape, size and drug content, and the influence of the polymer on microsphere characteristics was evaluated. Results show that polymer type, polymer molecular weight and its concentration in the spraying solution greatly affect microsphere characteristics. In vitro dissolution tests performed with the rotating bottle method resulted in different release profiles depending on type of polymer and on microsphere morphology.

Biocompatible Materials↗

PubMedDate not supplied

Cellulose acetate butyrate and polycaprolactone for ketoprofen spray-dried microsphere preparation.

Ketoprofen-loaded microspheres made with a polymeric blend were prepared by a spray-drying technique. Organic solutions of two polymers, cellulose acetate butyrate (CAB) and poly(epsilon-caprolactone) (PCL), in different weight ratios, and of ketoprofen (Ket) were prepared and sprayed, in different experimental conditions, achieving drug-loaded microspheres. The obtained spray-dried microspheres were characterized in terms of yield of production, shape, size, surface properties and drug content, and their in vitro drug release behaviours were determined at different pH values.

Cellulose↗

PubMedDate not supplied

Spray-dried albumin microspheres for the intra-articular delivery of dexamethasone.

This work deals with the preparation of corticosteroid-loaded albumin microspheres designed for intra-articular administration. Dexamethasone was chosen as the model drug and bovine serum albumin was used as the biodegradable, natural polymer. Albumin microspheres were produced by spray drying, a 'one-step' technique seldom used in the preparation of microparticulate drug delivery systems with particle sizes < 10 microns. The effects of both polymer/drug ratio used in the formulations and the different heat-stabilization conditions were evaluated on morphology, size, solubility characteristics, drug loading and 'in vitro' drug release of the microparticles.

Dexamethasone↗

PubMedDate not supplied

Cellulose acetate trimellitate ethylcellulose blends for non-steroidal anti-inflammatory drug (NSAID) microspheres.

Ketoprofen (Ket), a non-steroidal anti-inflammatory drug, has been incorporated into polymeric micromatrices (microspheres) prepared by a spray drying process and made of cellulose acetate trimellitate (CAT)/ethylcellulose (EC) blends. Drug loaded microspheres were obtained by spray-drying organic solutions of the two polymers and the drug. Characterization of the microparticles (morphology, particle size distribution, drug content, yield of production, surface properties, solvent residues) was carried out and in-vitro release behaviour measured. The release rate of the drug diminished as the proportion of EC was raised.

Anti-Inflammatory Agents, Non-Steroidal↗

PubMedDate not supplied

Thymopentin loaded microsphere preparation by w/o/w emulsion technique: in vitro/ex vivo evaluation.

Poly-D,L-lactide (PDLLA) and polylactide-co-glycolide (PLGA) microspheres containing thymopentin have been prepared by a water-in-oil-in-water-emulsion/solvent evaporation technique. The goal is to stabilize the active compound thymopentin, and to prolong its therapeutic activity, by embedding the drug in a polymeric matrix. The microspheres obtained have been characterized for their morphology and drug content. In-vitro dissolution tests have been performed on the microspheres. Results show that the type of polymer employed (PDLLA or PLGA) does not seem to affect microsphere morphology, while in-vitro dissolution profiles are greatly influenced by the composition of polymer matrix. Ex-vivo evaluation of PLGA microspheres performed on mouse thymocites shows that biological activity of Thymopentin is maintained after loading into PLGA microspheres.

Adjuvants, Immunologic↗

PubMedDate not supplied

PDLLA microspheres containing steroids: spray-drying, o/w and w/o/w emulsifications as preparation methods.

Hydrocortisone and its more soluble ester, hydrocortisone 21-acetate, have been incorporated into poly(D,L-lactic) acid (PDLLA) microspheres using single, double emulsion/solvent evaporation and by spray-drying techniques. This paper describes the characterization of the microparticles obtained (morphology, particle size distribution, drug content, yield of production, in vitro drug release behaviour) and a comparison of the results (drug loading, drug release, size of the microspheres) obtained from the different techniques used. These results demonstrate that by using a relatively more soluble ester of an insoluble steroid, hydrocortisone, the drug content within the microspheres can be increased, together with a high efficiency of loading, irrespective of the technique employed. In the case of hydrocortisone, spray-drying produces the highest loading and encapsulation efficiency compared to both single and double emulsion methods for microspheres of similar size (about 2-4 microns) and suitable for lung delivery, but with lower yields (about 55% versus about 33%).

Calorimetry, Differential Scanning↗

PubMedDate not supplied

Polylactide microspheres for the modified release of corticosteroids.

A steroidal drug, prednisolone 21-acetate, has been incorporated into polylactide (PDLLA) microspheres using a single emulsion/evaporation technique. This paper describes the method used and the characterization of the microspheres obtained: morphology, particle size distribution, drug content, yield of production and in vitro drug release behaviour.

Adrenal Cortex Hormones↗

PubMedDate not supplied

Compressed biodegradable matrices of spray-dried PLGA microspheres for the modified release of ketoprofen.

A spray-drying technique was used to prepare poly(lactide-co-glycolide) (PLGA) drug loaded microspheres. Ketoprofen was chosen as a model NSAID drug. The microspheres were characterized in terms of morphology, drug content and release behaviour. The spray-dried particles were subject to a direct compression process for the preparation of biodegradable matrix tablets. The spray-dried powders were found to have good compaction properties. Tablets were also prepared from a mixture of microspheres and microcrystalline cellulose, mannitol and hydroxypropylmethylcellulose or sodium alginate. The release of ketoprofen in phosphate buffer (pH 7.4) was significantly sustained, indicating the suitability of using tabletted spray-dried PLGA microspheres for controlled drug delivery. The results show that spray-dried PLGA particles have promising properties as direct compression and release controlling excipients in matrix tablets for oral administration.

Administration, Oral↗

PubMedDate not supplied

Cross-linked sodium carboxymethylcellulose as a carrier for dissolution rate improvement of drugs.

The dissolution rate is often the limiting step in gastrointestinal absorption of water insoluble drugs from solid oral dosage forms. The aim of this work was to use a swellable polymer chosen among superdisintegrants, for improving the dissolution rate of a sparingly soluble drug, loaded on its surface. Nifedipine, which has a very low water solubility, was chosen as a model drug, while cross-linked sodium carboxymethylcellulose (Ac-Di-Sol) was chosen as the swellable polymer. The Nifedipine/Ac-Di-Sol systems were prepared using two different techniques: evaporation and spraying; in some preparations polyethylene glycol (PEG 1500), or sucrose palmitate (Sucrodet), or dioctyl sodium sulfosuccinate (Aerosol OT) were added. The results of the dissolution tests showed that the dissolution rate of Nifedipine from the systems prepared increases, particularly in the case of the preparation composed of Ac-Di-Sol plus surfactant agents.

Carboxymethylcellulose Sodium↗