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1.
Int J Pharm ; 514(1): 229-237, 2016 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-27863666

RESUMO

In this work nasal powder formulations of thalidomide were designed and studied to be used by persons affected by hereditary hemorrhagic telangiectasia as a complementary anti-epistaxis therapy, with the goal of sustaining the effect obtained with thalidomide oral treatment after its discontinuation for adverse effects. Three nasal powders were prepared using as carriers ß-CD or its more hydrophilic derivatives such as hydropropyl-ß-CD and sulphobutylether-ß-CD and tested with respect to technological and biopharmaceutical features after emission with active and passive nasal powder devices. For all formulated powders, improved dissolution rate was found compared to that of the raw material, making thalidomide promptly available in the nasal environment at a concentration favouring an accumulation in the mucosa. The very limited transmucosal transport measured in vitro suggests a low likelihood of significant systemic absorption. The topical action on bleeding could benefit from the poor absorption and from the fact that about 2-3% of the thalidomide applied on the nasal mucosa was accumulated within the tissue, particularly with the ß-CD nasal powder.


Assuntos
Epistaxe/tratamento farmacológico , Pós/administração & dosagem , Telangiectasia Hemorrágica Hereditária/tratamento farmacológico , Talidomida/administração & dosagem , Administração Intranasal , Animais , Química Farmacêutica/métodos , Portadores de Fármacos/química , Humanos , Mucosa Nasal/efeitos dos fármacos , Coelhos , Solubilidade , beta-Ciclodextrinas/administração & dosagem
2.
Eur J Pharm Sci ; 66: 20-8, 2015 Jan 23.
Artigo em Inglês | MEDLINE | ID: mdl-25277680

RESUMO

In this paper we propose an in situ forming ionically cross-linked alginate (Alg) hydrogel delivering a Tea Tree Oil microemulsion (MeTTO) and potentially useful as an advanced dressing for infected wounds. Alg hydrogels were prepared by a spray-by-spray deposition method with the aim to minimize the discomforts during application. From pseudoternary phase diagrams, it was found that proper combination of TTO, water, polysorbate 80 and ethanol gave stable spherical MeTTO with good antimicrobial activity. On this basis, MeTTO at 20% TTO was selected for further inclusion in an Alg hydrogel prepared by alternating sprays of Alg/MeTTO and calcium chloride solutions. Homogeneous dispersion of MeTTO inside cross-linked Alg was assessed by different macroscopic and microscopic methods demonstrating the superior propensity of MeTTO to be integrated in the water-based hydrogel as compared to TTO. Antimicrobial effect of Alg/MeTTO hydrogels on Escherichia Coli strains was remarkable, highlighting the potential of the system as bioactive wound dressing.


Assuntos
Alginatos/química , Emulsões/química , Hidrogéis/química , Óleo de Melaleuca/química , Aerossóis , Antibacterianos/química , Antibacterianos/farmacologia , Escherichia coli/efeitos dos fármacos , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Testes de Sensibilidade Microbiana , Microscopia Eletrônica de Varredura/métodos , Polissorbatos
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