The site of action of griseofulvin, a drug which is reported to be fungistatic in nature, has been under study for some time. As yet though, there is still a great deal of uncertainty as to which observed effects are primary and which are secondary. In the study reported here, initial experiments were involved with effects of griseofulvin on oxygen uptake, in correlation with cell starvation. The effects of the drug on glucose oxidation also were studied. Definite alterations were noted in both of these areas. Further investigations were carried out, utilizing cell-free extracts and techniques for measurement of dehydrogenases, but these proved unsuccessful. Amino acid metabolism also was surveyed but no evidence of any alteration was observed. Attempts to produce protoplasts from dermatophytes were successful, and utilizing these structures, investigations into the effects of griseofulvin on cytoplasmic membrane permeability and on cell wall resynthesis, were carried out. In both cases the alterations were small and appeared to be secondary in nature. In the final study, purified cell walls of organisms grown in the presence and absence of griseofulvin, were compared on the basis of amino acid, amino sugar, and sugar content. No differences were observed in these preparations. In addition, no evidence was found to show that griseofulvin wlis incorporated into cell walls. It was concluded that griseofulvin may possibly affect the enzymes involved in the synthesis of the substrates of endogenous respiration, or the mechanisms controlling these enzymes. It was also concluded that the drug's site of action is probably on or near the cytoplasmic membrane, and by inference that the biochemical site may be in the area of purine and pyrimidine metabolism. / Science, Faculty of / Microbiology and Immunology, Department of / Graduate

Universiẗat, Diss.--Düsseldorf, 1984.

Thesis (Ph. D.)--University of Wisconsin--Madison, 1967. / Typescript. Vita. eContent provider-neutral record in process. Description based on print version record. Includes bibliographical references.

Phenobarbital pretreatment, in man and rat, has been observed to decrease the plasma levels attained after administration of solid dosage forms of griseofulvin. Various mechanisms including induced metabolism, increased gastrointestinal motility, diminished dissolution rate or a complex mechanism involving enzyme induction, first-pass metabolism and distribution rate-limited elimination of griseofulvin have been suggested. This present investigation was initiated in an attempt to clarify the mechanism of this interaction. Intravenous administration of griseofulvin in control and phenobarbital dosed rats confirmed that no obvious differences existed in griseofulvin metabolism under the experimental conditions. The influence of gut motility on the absorption of griseofulvin administered as single oral doses of either 100 mg/kg in 0.5% Tween 80 (suspension) or 50 mg/kg in 100% polyethylene glycol (PEG) 600 (solution) was evaluated by pretreating rats with single intraperitoneal doses of either 10 mg/kg metoclopramide hydrochloride or 5 mg/kg propantheline bromide two hours prior to griseofulvin administration. Metoclopramide pretreatment accelerated the absorption rate of griseofulvin suspension (the time of peak-plasma level, Tmax was shortened from 6 to 3 hours) but reduced its total absorption by 50%. Conversely, this treatment regimen increased the total absorption of griseofulvin by 230% when administered in solution form. Propantheline preadministration, however, retarded the absorption rate (Tmax prolonged from 6 to 19 hours) but increased the total absorption of a suspension of griseofulvin by 50% The propantheline treatment regimen elicited a sharply contrasting effect by decreasing the total absorption (23%) of griseofulvin when given in solution form. It was therefore, concluded that a) the interaction of griseofulvin with metoclopramide and propantheline is formulation-dependent and b) the gut motility has a significant influence on the absorption of griseofulvin. The interaction between griseofulvin and phenobarbital was evaluated by administering single oral doses of a) suspension of 100 mg/kg griseofulvin in either 0.5% or 2% Tween 80, b) suspensions of 20 or 100 mg/kg griseofulvin in 70% PEG 300, or c) solutions of 50 mg/kg griseofulvin in 100% PEG 600. Test rats received single oral doses of 15 mg/kg sodium phenobarbital 24 hours prior to griseofulvin administration. The treatment reduced the total absorption of griseofulvin administered in 0.5% Tween 80 by 50%. The extent of the interaction was reduced to an insignificant level on increasing the concentration of Tween 80 from 0.5% to 2%. Phenobarbital did not alter the apparent rate of griseofulvin absorption since the peak plasma concentrations were coincident between control and test animals. Phenobarbital treatment did not affect the availability of griseofulvin when administered as suspensions or solutions in PEG as reflected by equivalent areas under the plasma curves at the same dose level in test and control animals. It can therefore be concluded that the interaction between griseofulvin and phenobarbital in the rat is a) a formulation-dependent phenomenon and b) not caused by either enzyme induction or an increased gut motility. It is concluded that when griseofulvin is administered as a suspension in 0.5% Tween 80 the phenobarbital-griseofulvin interaction in the rat is caused by a complex mechanism resulting in a diminished dissolution rate and subsequent decreased absorption. / Pharmaceutical Sciences, Faculty of / Graduate

Universiẗat Diss., 2003--Tübingen.

Οι μικροσωληνίσκοι της μιτωτικής ατράκτου είναι υπεύθυνοι για τον αποχωρισμό των αδελφών χρωματιδίων κατά την Ανάφαση. Τροποποίηση ή καταστολή της δυναμικής του δικτύου των μικροσωληνίσκων συνεπάγεται αναστολή της κυτταρικής διαίρεσης μέσω ενεργοποίησης του σημείου ελέγχου της Μίτωσης. Έτσι, ενώσεις που προσδένονται στο μόριο της β-τουμπουλίνης και σταθεροποιούν τους μικροσωληνίσκους, όπως το paclitaxel και η griseofulvin, ή τους αποσταθεροποιούν, όπως η nocodazole, αποτελούν αποτελεσματικά φάρμακα έναντι του καρκίνου, αλλά και άλλων ασθενειών. Η πρόσδεση των φαρμάκων στους μικροσωληνίσκους έχει ως αποτέλεσμα, την αναστολή της αλληλεπίδρασης μικροσωληνίσκων-κινητοχώρου, βλάβες στη λειτουργία της μιτωτικής ατράκτου και ανώμαλο χρωμοσωματικό αποχωρισμό, με συνέπεια την εμφάνιση ανευπλοειδικών κυττάρων. Στόχος της παρούσας εργασίας είναι η συγκριτική διερεύνηση της ανευπλοειδογόνου δράσης των φαρμακευτικών ενώσεων nocodazole, paclitaxel και griseofulvin σε τρία κυτταρικά συστήματα in vitro: στους μυοβλάστες ποντικού C2C12, στους ινοβλάστες ανθρώπου HFFF2 και στα καρκινικά επιθηλιακά κύτταρα ανθρώπου MCF-7. Η συγκριτική ανάλυση πραγματοποιήθηκε με τη μελέτη επαγωγής μικροπυρήνων και του μηχανισμού προέλευσης τους, μέσω της διπλής ανοσοσήμανσης πρωτεϊνών του κινητοχώρου (CREST) και του δικτύου του κυτταροσκελετού (α- τουμπουλίνη). Ακολούθησε μελέτη της ακεραιότητας της μιτωτικής συσκευής, μέσω συνδυασμένης ανοσοσήμανσης πρωτεϊνών του κεντροσώματος (γ- τουμπουλίνη & Aurora A) και του δικτύου των μικροσωληνίσκων (β- τουμπουλίνη). Τέλος, πραγματοποιήθηκε μελέτη της έκφρασης πρωτεϊνών που συμμετέχουν στο χρωμοσωματικό αποχωρισμό, όπως οι Aurora A, β- και γ-τουμπουλίνη, μέσω της μεθόδου της ανοσοαποτύπωσης (Western Blot Analysis). Με την ολοκλήρωση της μελέτης παρατηρείται ότι και οι τρεις χημικές ενώσεις: επάγουν το φαινόμενο της χρωμοσωματικής καθυστέρησης, κατάσταση που υποδηλώνει την ύπαρξη ολόκληρου χρωμοσώματος, με αύξηση της συχνότητας των μικροπυρήνων με κινητοχώρο στο εσωτερικό τους και στις τρεις κυτταρικές σειρές. Επίσης, προκαλούν αύξηση του ποσοστού πολυπύρηνων μεσοφασικών κυττάρων και στα τρία κυτταρικά συστήματα. Προκαλούν αύξηση του μιτωτικού δείκτη και συσσώρευση των κυττάρων στο στάδιο της Μετάφασης στα κύτταρα C2C12, HFFF2 και MCF-7. Η συσσώρευση αυτή συνοδεύεται με ταυτόχρονη μείωση των Ανατελοφάσεων. Αποδιοργανώνουν, ακόμα, το δίκτυο των μικροσωληνίσκων, τόσο στα μεσοφασικά όσο και στα μιτωτικά κύτταρα. Ειδικότερα, η nocodazole επάγει την αύξηση του ποσοστού μεσοφασικών κυττάρων με πολύ συμπυκνωμένο δίκτυο και κατεστραμμένο (στικτό) γενετικό υλικό στα κύτταρα ποντικού C2C12. Επίσης, και οι τρεις ενώσεις επηρεάζουν τον κεντροσωματικό πολλαπλασιασμό, με την εμφάνιση ανώμαλων Μεταφάσεων και στις τρεις κυτταρικές σειρές. Η nocodazole επάγει το σχηματισμό μονοπολικών Μεταφάσεων, αντίθετα το paclitaxel σχηματίζει πολυπολικές Μεταφάσεις. Η griseofulvin παρουσιάζει κυτταρική εξειδίκευση με την πρόκληση μονοπολικών Μεταφάσεων στα κύτταρα C2C12, πολυπολικών Μεταφάσεων στα καρκινικά κύτταρα MCF-7 και κατά πλειονότητα μη-ομαδοποιημένων Μεταφάσεων στα κύτταρα HFFF2. Οι εν λόγω μελετηθείσες χημικές ενώσεις τροποποιούν επίσης την έκφραση των πρωτεϊνών Aurora A, β- & γ-τουμπουλίνης και στα τρία κυτταρικά συστήματα. Κύριο χαρακτηριστικό της δράσης της nocodazole είναι η μείωση της έκφρασης των πρωτεϊνών Aurora A και β-τουμπουλίνης. Αντίθετα το paclitaxel και η griseofulvin οδηγούν σε υπερέκφραση των Aurora A, β- και γ-τουμπουλίνη. Και οι τρεις φαρμακευτικές ενώσεις παρουσιάζουν κυτταρική εξειδίκευση ως προς τον επηρεασμό της έκφρασης των πρωτεϊνών που μελετήθηκαν. Τα ευρήματα αυτά υποδηλώνουν τη συμμετοχή των τριών πρωτεϊνών στην εκδήλωση της ανευπλοειδογόνου δράσης των τριών χημικών ενώσεων. Τα παραπάνω συμπεράσματα επιβεβαιώνουν και ερμηνεύουν την ανευπλοειδογόνο δράση των φαρμακευτικών ενώσεων, nocodazole, paclitaxel και griseofulvin. / The microtubules of the mitotic apparatus are responsible for the chromosome segregation during Anaphase. Modification or inhibition of the dynamics of the microtubules results to the activation of the mitotic checkpoint. Chemicals that bind at the molecule of β-tubulin and stabilize microtubules, like paclitaxel and griseofulvin or destabilize them, like nocodazole, act as drugs against cancer or other diseases. This binding results to the inhibition of microtubule-kinetochore interactions, damage of the organization of the mitotic spindle, abnormal chromosome segregation and thus the generation of aneuploid cells. In the present study we comparatively investigated the aneugenic potential of three chemical compounds, nocodazole, paclitaxel and griseofulvin in three cell lines in vitro: C2C12 mouse fibroblasts, HFFF2 human myoblasts and MCF-7 human epithelial cancer cells. The comparative analysis was established by three different experimental procedures. The study of micronucleus induction and their generation mechanism was accomplished by CREST analysis in combination with immunostaining of α- tubulin. The ability of the chemicals to affect the organization of mitotic apparatus was investigated by double immunofluorescence of microtubule network (β-tubulin) and centrosomes (γ-tubulin & Aurora A) in all cell lines. Finally, to understand further the mechanisms by which nocodazole, paclitaxel and griseofulvin exert their aneugenic potential, we examined the ability of these compounds to modulate the expression of proteins that participate in chromosome segregation, such as Aurora A, β- and γ-tubulin, by Western blot analysis in C2C12, HFFF2 and MCF-7 cells. Our results revealed that the three chemical compounds:  Induce chromosome delay, showing a high frequency of micronuclei with kinetochore, indicating the presence of intact chromosome in every studied cell line. In addition, all the drugs evoke induction of multinucleated cells in all cell lines.  Increase the mitotic index with simultaneous Metaphase arrest. The cell accumulation at the Metaphase is accompanied with reduction of Anatelophases in all cell lines.  Promote disorganization of the microtubule network. Especially, nocodazole causes induction of abnormal interphase cells with very condensed network (bundled cells) and punctuated genetic material in C2C12 mouse cell line.  Affect the centrosome proliferation, increasing the frequency of abnormal Metaphases in the three cell lines. Nocodazole induces high frequency of monopolar Metaphases, whereas paclitaxel generates polypolar Metaphases. Griseofulvin produces monopolar Metaphases in C2C12 cells, polypolar Metaphases in cancer MCF-7 cells and mainly non-congressed Metaphases in HFFF2 cells, exhibiting cell specificity.  Modify the expression of the proteins Aurora A, β- and γ-tubulin in all cell lines. Nocodazole reduces Aurora’s A expression in C2C12, HFFF2 and MCF-7 cell lines. The same is observed for β- tubulin’s expression, as for C2C12 and MCF-7 cells. Paclitaxel exerts its aneugenic potential by enhancing the expression of Aurora A and γ-tubulin in all cell lines, whereas enhancing β- tubulin’s expression is only noticed in C2C12 and MCF-7 cells. Griseofulvin increases the expression of Aurora A and β-tubulin in human cancer cells MCF-7. As for γ-tubulin’s expression, is elevated only in the human cell lines HFFF2 and MCF-7. Thus, we suggest that the activity of the pharmaceutical compounds on the expression of the above proteins, exhibit cell specificity. These findings implicate that the aneugenic potential of the studied drugs is mediated through changes in the expression of these proteins. The conclusions above confirm and explain the aneugenic potential of the pharmaceutical compounds, nocodazole, paclitaxel and griseofulvin.

O estudo sobre a utilizaÃÃo de copolÃmeros na dissoluÃÃo de fÃrmacos pouco solÃveis em Ãgua vem sendo cada vez mais praticado, devido, principalmente, à baixa toxicidade desses carreadores e da sua alta eficiÃncia no processo de dissoluÃÃo. Com o uso de copolÃmeros surfactantes, que formam micelas em soluÃÃo, à possÃvel aumentar a solubilidade e controlar o tempo e/ou atuar na liberaÃÃo de fÃrmacos hidrofÃbicos no organismo. Os copolÃmeros triblocos anfifÃlicos denominados EmPnEm (PluronicÂ), P123 (E21P69E21) e F127 (E98P69E98), onde E representa o monÃmero Ãxido de etileno [â(OCH2CH2) â], P, o monÃmero Ãxido de propileno [âOCH2CH(CH3)â], e os subscritos m e n denotam o comprimento do bloco, estÃo sendo alvos desta pesquisa devido as suas propriedades de formaÃÃo de gel a temperatura ambiente (termorresponsidade), possibilitando a aplicaÃÃo subcutÃnea, e sua capacidade de solubilizaÃÃo de ativos lipofÃlicos no nÃcleo micelar de polioxipropileno (Pn). Misturas binÃrias de Pluronics de hidrofobicidades semelhantes, em sua grande maioria, apresentam capacidade de solubilizaÃÃo maior que para os Pluronics sozinhos. Assim, visando potencializar a solubilizaÃÃo dos fÃrmacos griseofulvina, fÃrmaco modelo utilizado em vÃrios trabalhos, e mangiferina, ativo antioxidante, e promover a maior biodisponibilidade desses fÃrmacos no organismo, sistemas de micelas mistas compostas por F127 e P123 serà o foco dessa pesquisa, com finalidade de unir suas propriedades geleificantes e de biocompatibilidade para aplicaÃÃo subcutÃnea / T he use of copolymers in the dissolution of poorly soluble drugs in water is being increasingly practiced, principally, due to the low toxicity of these carriers and their high ef ficiency in the dissolution process. Using copolymer surfactants, which form micelles in solution, can enhance the solubility and control the time and act in the release of hydrophobic drugs in the body. The amphiphilic triblock copolymers known E m P n E m (Pl uronicÂ), P123 (E 21 P 67 E 21 ) and F127 (E 98 P 67 E 98 ), where E is the ethylene oxide monomer [ - (OCH 2 CH 2 ) - ] and P, propylene oxide monomer [ - OCH 2 CH(CH 3 ) - ], and the subscripts, n and m , denote the block length, being targets of this research due to their gelling p roperties at room temperature, enabling the application subcutaneo us, and its ability to solubilis e the active lipophilic in the micellar core. Binary mixtures of Pluronics of similar hydrophobicities, mos tly, show greater solubilis ation capacity for Plur onics alone. Thus, i n order to enhance the solubilis ation of griseofulvin drugs, drug model used in several works, and mangiferin, active antioxidant, and promote greater bioavailability of these drugs in the body systems of mixed micelles composed of F12 7 and P123 will be the focus of this research, in order to unite their gelling properties and biocompatibility for subcutaneous administration

Thesis (M.Pharm. (Pharmaceutics) -- University of Limpopo, 2018 / Griseofulvin is an antibiotic fungistatic drug used in the treatment of dermatophyte and ringworm infections. About 50% of a dose of griseofulvin passes the gastro- intestinal tract unabsorbed and is excreted in faeces. Since griseofulvin is highly soluble in acidic pH, a gastro-retentive floating matrix system was developed to control dissolution rate and thereby enhance solubility in an effort to develop an improved and convenient dosage form. Preformulation studies included selection of excipients and evaluation of their compatibility with griseofulvin. Using the chosen excipients, floating tablets of griseofulvin were formulated. Floating tablets containing 100 mg of griseofulvin were prepared by wet granulation technique with varying ratios of Methocel™, Accurel MP and Polyvinylpyrrolidone as determined by Design Expert software. Pre and post-compression studies, buoyancy capability and dissolution studies were carried out to assess the influence of the tablet components. Results obtained revealed that a density of less than 0.00091 g/cm3 was necessary for tablet floatation. Tablets that float immediately upon contact with dissolution medium and continue floating for over 12 hours were achieved with at least 28% Accurel MP by mass of the tablet. Dissolution studies revealed that an increase in tablet hardness reduced the rate of griseofulvin release only up to 120 minutes. From 120 minutes onwards, tablet hardness had no significant influence on griseofulvin release from tablets. Methocel™ had the most significant influence on griseofulvin release. The amount of Methocel™ included in the formulation was indirectly proportional to the rate of griseofulvin release. Using Design Expert software, optimized formulation was achieved with 1% Polyvinylpyrrolidone, 30% Methocel™, 60% Accurel MP and hardness ranging between 8 – 9 N. Pre and post-compression parameters of the optimized tablets were found to be within pharmacopoeial limits and thus compressed tablets were of acceptable quality. Tablets produced floated immediately upon contact with the medium and remained floating for at least 12 hours. Griseofulvin was released from the optimized tablets in a near zero order fashion, with a total of 80.8% griseofulvin released at the end of the 12 hour dissolution test period. Results of accelerated stability studies indicated potential stability of the manufactured tablets months.

As dermatofitoses dos carnívoros domésticos são infecções fúngicas superficiais, causadas habitualmente por dois gêneros fúngicos: Microsporum sp e Trichophyton sp. Trata-se de uma antropozoonose, com importância na saúde pública Objetivou-se: caracterizar a população de cães e gatos acometidos por dermatofitose atendidos no Serviço de Dermatologia do HOVET /USP num período de 27 meses; determinar a valia do exame histopatológico como metodologia diagnóstica; e comparar a eficácia da griseofulvina e da terbinafina na terapia das dermatofitoses. Foram atendidos 76 animais com diagnóstico de dermatofitose, 47,3% pertenciam à espécie fetina e 52,7% à canina O agente etiológico isolado com maior freqüência em caninos e felinos foi Microsporum canis. Não se observou distribuição sazonal. Os cães de raça definida foram os mais acometidos (75,0%), dentre estes, aqueles da raça Yorkshire Temer (23,3%). Os felinos com e sem definição racial igualmente acometidos, porém os Persas (93,7%) foram os mais acometidos dentre aqueles com plena definição. Observou-se que a maioria dos animais infectados apresentava menos de um ano de idade (65,8%). As lesões mais observadas foram: alopecia, eritema, escamas e crostas. A maioria das lesões apresentava configuração circular e estavam localizadas nas regiões cefálicas, de tronco e de membros. O prurido esteve ausente em 50,0% dos caninos e em 88,8% dos felinos. As lesões dos cães tinham caráter mais inflamatório. O exame histopatológico mostrou-se pouco sensível (28,6%) e com alto número de falsos negativos (71,4%). A griseofulvina (5Omg/kg/dia) foi eficaz em l00,0% dos casos, sem acarretar efeitos colaterais, com média de tempo para cura de 41 dias. Já a terbinafina na dose de cinco mg/kg/dia, apresentou eficácia de 81,8%, sem induzir efeitos colaterais e com êxito terapêutico em 21 dias. Demonstrou-se assim, que a dose de 20 mg/kg/dia demonstrou a mesma eficácia que a dose de cinco, porém, com efeitos colaterais em 16,6% dos animais tratados, com tempo médio para cura de 33 dias. Demonstrou-se que a terbinafina é uma boa alternativa terapêutica, porém, a griseofulvina ainda se constitui na droga de eleição para o tratamento das dermatofitoses de caninos e felinos. / Dermatophytosis in domestic carnivorous are superficial infections caused mainly by two genus of fungus: Microsporum sp and Trichophyton sp. This disease is an anthropozoonosis important for public health. The goals of this study were: characterize the population of cats and dogs with dermatophytosis treated in the Dermatology Service of HOVET FMVZ/USP in a period of 27 months; evaluate the validity of the histopathological exam as a methodology of diagnosis; and compare the efficacy of griseofulvin and terbinafine in the therapy of the dermatophytosis. Seventy six animals (47,3% were felines and 52,7% were canines) were evaluated in this study. The more frequent isolated etiological agent in canines and felines was Microsporum canis. Seasonality was not observed. The dogs with a defined breed were more predisposed (75,0%) and the Yorkshire Terrier dogs had a higher proportion of positive cultures (23,3%). The felines with or without breed definition got the same frequency, however, the Persians (93,7%) were more predisposed among those of pure breed. It was noticed that the majority of infected animals were under one year of age (65,8%). The most observed lesions were: alopecia, crusts, erythema and scales. The majority of the lesions had a circular form and were found in the cephalic, trunk and limb regions. There was no pruritus in 50,0% of the canines and 88,8% of the felines. The lesions were more inflammatory in dogs. The histopathological exam had a low sensitivity (28,6%) and a high number of false negatives (71,4%).Griseofulvin (50 mg/kg/day) was effective in 100,0% of the cases, with no side effects, the average time for cure was 41 days. The terbinafine used at the dosage of 5 mg/kg/day showed an efficacy of 81,3%, no side effects were observed as well and average time for cure was 21 days. The same efficacy using the dosage of 20 mg/kg/day of terbinafine was observed, although side effects were observed in 16,6% of the animals treated with an average time for cure of 33 days. The present study demonstrated that terbinafine is a good therapeutical alternative, although griseofulvin is still the first choice drug for the treatment of dermatophytosis in dogs and cats.

Conselho Nacional de Desenvolvimento CientÃfico e TecnolÃgico / CoordenaÃÃo de AperfeiÃoamento de Pessoal de NÃvel Superior / A solubilidade do fÃrmaco em Ãgua à um fator importante para sua eficÃcia. Entretanto, a maioria dos fÃrmacos apresenta baixa solubilidade em Ãgua. Para resolver este problema, copolÃmeros em bloco com propriedades surfactantes tÃm sido bastante investigados. O objetivo deste trabalho à investigar os copolÃmeros F87 (E62P39E62), E43B14E43 e suas misturas 50/50 a 90/10, com proporÃÃo crescente do copolÃmero mais hidrofÃbico (E43B14E43), a sÃrie de diblocos EmBn para carrear o fÃrmaco modelo griseofulvina atravÃs de diferentes mÃtodos de solubilizaÃÃo e estudar a sua liberaÃÃo, bem como o estudo da solubilizaÃÃo dos fÃrmacos quercetina e mangiferina nos copolÃmeros E65G5 e E65G7E65 visando suas aplicaÃÃes no carreamento e liberaÃÃo controlada de fÃrmacos. Utilizou-se a tÃcnica de inversÃo de tubo para o estudo das propriedades geleificantes dos copolÃmeros F87, E43B14E43 e suas misturas 50/50 a 90/10. Para a determinaÃÃo da concentraÃÃo micelar crÃtica (CMC) utilizou-se o mÃtodo de solubilizaÃÃo de corante medida por fluorescÃncia. A solubilidade dos fÃrmacos griseofulvina, quercetina e mangiferina nos sistemas micelares foi medida por espectrofotometria UV-Vis e para os sistemas dos copolÃmeros E65G5 e E65G7E65 utilizou-se a cromatografia lÃquida de alta eficiÃncia (HPLC). Os copolÃmeros puros e os sistemas contendo os fÃrmacos foram caracterizados por tÃcnicas de espectroscopia de absorÃÃo na regiÃo do infravermelho (FT-IR), espectroscopia RAMAN (FT-RAMAN), raios-X, tamanho de partÃcula por espalhamento de luz dinÃmico (Zetasizer), e experimentos de liberaÃÃo in vitro foram realizados para alguns dos sistemas. Os copolÃmeros F87, E43B14E43, suas misturas, os diblocos da sÃrie EmBn e os copolÃmeros E65G5 e E65G7E65 sÃo promissores para administraÃÃo de fÃrmacos hidrofÃbicos, pois apresentaram bons valores de capacidade de solubilizaÃÃo (Scp). Os copolÃmeros E65G5 e E65G7E65 foram os que mais se destacaram na solubilizaÃÃo da quercetina (HPLC): seu sistema micelar aumentou a solubilidade aquosa da quercetina em 264 vezes a 25 ÂC em ambos os copolÃmeros e 118 e 135 vezes a 37ÂC, no dibloco e tribloco, respectivamente, e suas partÃculas apresentaram total eficiÃncia de encapsulaÃÃo da quercetina. Portanto, o dibloco de glicidil (E65G5) à o melhor copolÃmero para encapsulamento de fÃrmaco. / Most drug candidates fail to progress in their formulations due to its low solubility in water. To resolve this issue, block copolymers with surfactant properties have been well investigated. The objective of this study was to investigate the copolymers F87 (E62P39E62), and mixtures thereof E43B14E43 50/50 to 90/10, with increasing proportion of the more hydrophobic copolymer (E43B14E43), the series of diblock EmBn to carry the model drug through different griseofulvin solubilization methods and study their release, and the study of drug solubilization of quercetin and mangiferin E65G5 the copolymers and their applications in order E65G7E65 Entrainment and controlled release of drugs. We used the technique of inversion of the tube for the study of gelling properties of copolymers F87, and mixtures thereof E43B14E43 50/50 to 90/10. To determine the critical micelle concentration (CMC) used the dye solubilization method measured by fluorescence. The solubility of drugs griseofulvin, quercetin and mangiferin in micellar systems was measured by UV-Vis spectrophotometry and systems of copolymers E65G5 E65G7E65 and used the high performance liquid chromatography (HPLC). The pure copolymers and the systems containing the drugs were characterized by infrared spectroscopy (FT-IR), Raman spectroscopy (FT-Raman), X-rays, particle size by dynamic light scattering (Zetasizer), and experiments in vitro release were carried out for some systems. The copolymers F87, E43B14E43, their mixtures, the number of diblock copolymers and EmBn E65G5 E65G7E65 and are promising for administration of hydrophobic drugs, because they showed good solubilising capacity values ​​(Scp). The copolymers were E65G7E65 E65G5 and those who stood out in solubilization of quercetin (HPLC): its micellar system increased the aqueous solubility of quercetin in 253 times at 25  C for both copolymers and 124 and 142 times at 37  C for the diblock and triblock, respectively, and its particles showed complete encapsulation efficiency of quercetin