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1.
J Drug Target ; 22(6): 469-77, 2014 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-24830300

RESUMO

Glioma is one of the most commonly occurring malignant brain tumours which need proper treatment strategy. The current therapies for treating glioma like surgical resection, radiotherapy, and chemotherapy have failed in achieving satisfactory results and this forms a rationale for the development of novel drug delivery systems. Among them, polymersomes are superior novel carriers with diverse functions like enhanced stability, low permeability, tunable membrane properties, surface functionality, and long blood circulation time which make them suitable for cancer therapy. These are bilayered vesicles capable of encapsulating both hydrophilic and hydrophobic drugs used to target glioma effectively. In this review, we have discussed on general preparation, characterization, and targeting aspects of surface modified polymersomes for effective delivery of therapeutic agents to glioma.


Assuntos
Antineoplásicos/administração & dosagem , Neoplasias Encefálicas/tratamento farmacológico , Portadores de Fármacos , Glioma/tratamento farmacológico , Polímeros , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Barreira Hematoencefálica , Emulsões , Receptores de Superfície Celular/efeitos dos fármacos , Solventes
2.
Expert Opin Drug Deliv ; 11(9): 1351-65, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24847779

RESUMO

OBJECTIVES: The major objective is to target diethylcarbamazine citrate (DEC) to the lymphatics and to increase its retention time. The effect of various excipients on the physicochemical characteristics of the nanoparticles was also studied. MATERIALS AND METHODS: Solid lipid nanoparticles (SLNs) of DEC were prepared by ultrasonication by varying the concentrations of compritol 888 ATO, poloxamer 188 and soya lecithin. The SLNs were evaluated for size, shape, texture, surface charge, physical nature of the entrapped drug, entrapment efficiency and in vitro drug release. In vivo animal studies were carried out to estimate the pharmacokinetic parameters in blood and drug concentration in lymph after oral administration. RESULTS: The size of the spherical particles was in the range of 27.25 ± 3.43 nm to 179 ± 3.08 nm and a maximum entrapment efficiency of 68.63 ± 1.53% was observed. In vitro release studies in pH 7.4 PBS displayed a rapid release and the maximum time taken for the complete drug to release was 150 min. In vivo studies indicated an enhancement in the amount of drug that reached lymphatics when administered via SLNs. CONCLUSION: Targeting of DEC to the lymphatics is possible through SLNs and the retention time in the lymphatics can also be enhanced.


Assuntos
Dietilcarbamazina/administração & dosagem , Sistemas de Liberação de Medicamentos , Excipientes/química , Nanopartículas , Administração Oral , Animais , Dietilcarbamazina/farmacocinética , Portadores de Fármacos/química , Ácidos Graxos/química , Lecitinas/química , Lipídeos/química , Sistema Linfático/metabolismo , Masculino , Tamanho da Partícula , Poloxâmero/química , Ratos , Ratos Sprague-Dawley , Glycine max/química , Fatores de Tempo
3.
Chem Pharm Bull (Tokyo) ; 56(4): 575-7, 2008 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-18379110

RESUMO

Telmisartan (anti-hypertensive) is insoluble in water; hence the drug may be slowly or incompletely dissolved in the gastro intestinal tract. So the rate of dissolution and therefore its bioavailability is less (bioavailability 42%). In the present study an attempt has been made to prepare immediate release tablets of telmisartan by using Polyplasdone XL-10 (Crosspovidone) at intragranular, extragranular and partly intra and extragranular level of addition to increase the rate of drug release from dosage form to increase the dissolution rate and hence its bioavailability. The prepared granules and tablets were evaluated for their physiochemical properties and in-vitro dissolution study was conducted for the prepared tablets. It was concluded that the immediate release tablets with proper hardness, disintegration time and with increase rate of dissolution can be made using Polyplasdone XL-10. Formuation-10 (F10) was selected for stability study and the in-vitro dissolution study showed that was no difference in percent of drug released between initial and sixth month sample.


Assuntos
Bloqueadores do Receptor Tipo 1 de Angiotensina II/administração & dosagem , Benzimidazóis/administração & dosagem , Benzoatos/administração & dosagem , Bloqueadores do Receptor Tipo 1 de Angiotensina II/química , Benzimidazóis/química , Benzoatos/química , Fenômenos Químicos , Química Farmacêutica , Físico-Química , Estabilidade de Medicamentos , Armazenamento de Medicamentos , Excipientes , Povidona , Pós , Comprimidos , Telmisartan , Temperatura
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