RESUMO
The aim of this study was to prepare a new microsphere (fucosphere) system based on polyion complexation of fucoidan with chitosan, and to evaluate its treatment efficiency on dermal burns. The physicochemical properties such as mean particle size and distribution, zeta potential and bioadhesive properties of the microspheres were investigated. The formulation which had the high surface charge, narrow size distribution and the highest bioadhesive property was selected and applied on seven male New Zealand white rabbits with dermal burns. Biopsy samples were taken on day 7, 14 and 21. Each burn site was evaluated macroscopically and histopathologically and the findings were compared with controls of fucoidan solution and chitosan microspheres. The microspheres between the size ranges of 367 and 1017 nm were obtained. The work of bioadhesion of microspheres, with the surface charges +6.1 to +26.3 mV, changed between 0.081 and 0.191 mJ cm(-2). Macroscopically and histopathological observations indicated that the fastest healing of the burns was obtained in group treated with fucosphere after 21 days of treatment (P<0.05). Rete peg formation values and nuclear organize regions (NORs) were higher with treated fucospheres than the other groups on day 14. In conclusion, in vitro and in vivo evaluation of fucospheres indicated that the new microsphere system shortened the treatment period of burns and provided fast and effective healing by improving regeneration and re-epithelization. Hence fucosphere may find application in the treatment of dermal burns.
Assuntos
Queimaduras/terapia , Quitosana/química , Microesferas , Polissacarídeos/química , Cicatrização , Animais , Química Farmacêutica/métodos , Epitélio/efeitos dos fármacos , Masculino , Microscopia Eletrônica de Varredura , Região Organizadora do Nucléolo/metabolismo , Tamanho da Partícula , Coelhos , Regeneração , Tecnologia Farmacêutica/métodosRESUMO
Ciprofloxacin hydrochloride-loaded microspheres were prepared by a spray-drying method using pectin and chitosan. The effects of different polymers and drug ratios were investigated. The most appropriate carriers were selected by in vitro testing. A rat methicillin-resistant Staphylococcus aureus osteomyelitis model was used to evaluate the effects of the loaded microspheres. The drug was released rapidly from the pectin carrier but this was more sustained in the chitosan formulation.Chitosan microspheres loaded with ciprofloxacin hydrochloride were more effective for the treatment of osteomyelitis than equivalent intramuscular antibiotics.
Assuntos
Anti-Infecciosos/uso terapêutico , Materiais Biocompatíveis/uso terapêutico , Quitosana/uso terapêutico , Ciprofloxacina/uso terapêutico , Microesferas , Osteomielite/tratamento farmacológico , Pectinas/uso terapêutico , Infecções Estafilocócicas/tratamento farmacológico , Animais , Varredura Diferencial de Calorimetria/métodos , Preparações de Ação Retardada/uso terapêutico , Modelos Animais de Doenças , Composição de Medicamentos/métodos , Avaliação Pré-Clínica de Medicamentos , Masculino , Microscopia Eletrônica de Varredura/métodos , Ratos , Ratos Wistar , Resultado do TratamentoRESUMO
The aim of the present study was to investigate the in vitro release properties of tiaprofenic acid (TA) from different topical vehicles. Carbopol 940 gel, chitosan gel, two types of emulsion-based ointment formulations (o/w and w/o) and hydrophilic petrolatum USP were prepared with 2% drug content. Drug release from all vehicles through a standard cellophane membrane was evaluated by using Franz-type diffusion cells. In vitro release study results showed that the diffusion coefficients of the drug from vehicles rank according to the following order: Carbopol 940 gel (D = 3.11 x 10(-7) +/- 0.54 cm(2)/s) > chitosan gel (D = 0.27 x 10(-7) +/- 0.08 cm(2)/s) > emulsion-based ointment (o/w) (D = 0.18 x 10(-7) +/- 0.05 cm(2)/s) > emulsion-based ointment (w/o) (D = 0.13 x 10(-7) +/- 0.02 cm(2)/s) > hydrophilic petrolatum USP (D = 0.02 x 10(-7) +/- 0.01 cm(2)/s). Carbopol 940 gel base showed significantly higher drug release than other vehicles (P < 0.001). These results indicated that Carbopol 940 gel base is a good candidate for the topical delivery of TA, giving significantly higher drug release than the other vehicles.
Assuntos
Propionatos/química , Resinas Acrílicas/química , Administração Tópica , Materiais Biocompatíveis/química , Química Farmacêutica , Quitosana/química , Emulsões , Géis , Bases para Pomadas , Propionatos/administração & dosagem , Absorção Cutânea , ViscosidadeRESUMO
Mefenamic acid (MA) has analgesic, anti-inflammatory and antipyretic properties. Available conventional dosage forms are capsules and film-coated tablets. No commercial sustained release preparation of MA exists in the market. The usual oral dose is 250 or 500 mg and reported half-life is 2 h. Sodium alginate (NaAL) is the sodium salt of alginic acid, a natural polysaccharide extracted from marine brown algae. It has the ability to form a water-insoluble gel with a bivalent metal ions as calcium. Therefore, NaAL has been studied for preparing sustained release formulations in pharmaceutical technology. In this study, tablet formulations containing different ratios of NaAL and calcium gluconate (CaGL) were prepared by direct compression method. In vitro release studies were carried out using USP 23 basket method and release data were kinetically evaluated. According to release studies, it can be emphasized that NaAL and CaGL can be used for design of sustained release preparation of MA.