Interaction of sodium diclofenac with freeze-dried soya phosphatidylcholine and unilamellar liposomes

Fosfolipídios são freqüentemente usados como compostos anfifílicos estruturais em formulações de lipossomas. Neste estudo foi analisada a interação do diclofenaco sódico (SD) com a fosfatidilcolina de soja liofilizada e a fosfatidilcolina de soja (PC) obtida de lipossomas unilamelares pequenos liofilizados (SUV). As modificações nas propriedades da mistura fármaco/PC co-liofilizados a partir de SUV pré-formados, lipossomas de PC vazios e PC liofilizada foram estudadas por Calorimetria Diferencial de Varredura (DSC). Os resultados de DSC mostraram que a organização prévia das moléculas PC para formar lipossomas interfere significativamente no perfil de DSC da PC, quando comparada ao perfil de DSC da PC não-lipossômica. Verificou-se que o SD afeta intensamente o grupo de picos situados nas regiões de 120-140ºC e na região de mais alta temperatura (240-260ºC). Os resultados deste trabalho demonstraram que em todos os casos a presença do fármaco modificou o perfil de DSC da PC e que essas modificações podem ser facilmanete monitoradas através da análise de DSC.Phospholipids are widely used as structural amphiphilic compounds in liposome formulations. In this study, we have analyzed the interaction the sodium diclofenac (SD) with soya phosphaditylcholine (PC) and soya phosphatidylcholine from lyophilized small unilamellar liposomes (SUV). The changes in the properties of the co-lyophilized drug/PC from SUV liposomes, lyophilized PC from SUV liposomes, and lyophilized soya phosphatidylcholine, were studied by Differential Scanning Calorimetry (DSC). The DSC data showed that the previous organization of phospholipids molecules to form liposome affects intensely the thermal behavior of PC when compared to non-lipossomal PC. SD modified the thermal properties of PC from liposomes. It was verified that SD affects intensely the located group peaks in the regions of 120-140 ºC and in the higher temperature region of 240-260 ºC. The results of this work demonstrated that the presence of the drug modified the DSC behavior for both liposomal and non-liposomal PC and that these modifications can be easily monitored by DSC analysis

New Approaches for Cryptococcosis Treatment

Cryptococcosis is an important opportunistic infection and a leading cause of meningitis in patients with HIV infection. The antifungal pharmacological treatment is limited to amphotericin B, fluconazole and 5- flucytosine. In addition to the limited pharmacological options, the high toxicity, increased resistance rate and difficulty of the currently available antifungal molecules to cross the blood–brain barrier hamper the treatment. Thus, the search for new alternatives for the treatment of cryptococcal meningitis is extremely necessary. In this review, we describe the therapeutic strategies currently available, discuss new molecules with antifungal potential in different phases of clinical trials and in advanced pre-clinical phase, and examine drug nanocarriers to improve delivery to the central nervous system