Biodegradable polyesters for controlled release of trypanocidal drugs: In vitro and in vivo studies

Lemmouchi, Yahia; Schacht, Etienne; Kageruka, P; Deken, R. De; Diarra, B.; Diall, O.; Geerts, S.

doi:10.1016/s0142-9612(98)00074-x

Cited by 77 publications

(67 citation statements)

References 26 publications

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“…These thermal properties were capitalized to fabricate drug delivery systems by means of processes such as melt molding (Ayres et al, 2007), extrusion (Bourges et al, 2006) without risking neither the polymer nor the drug molecular integrity due to an aggressive heating treatment (Sprockel et al, 1997;Lemmouchi et al, 1998;Carcaboso et al, 2010). Recently, the pharmaceutical companies have adopted the injection molding as a technique for designing polymeric drug delivery systems, due to the possibility to manufacture in large scale (Altpeter et al, 2004).…”

Section: Introductionmentioning

confidence: 99%

Efficacy of methotrexate-loaded poly(ε-caprolactone) implants in Ehrlich solid tumor-bearing mice

Pereira

Barbosa

et al. 2013

Drug Delivery

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Context: Methotrexate (MTX) is used in the treatment of malignancies; however, its clinical application is limited by its toxic dose-related side effects. An alternative to overcome the toxicity of the MTX in healthy tissues is the design of an implantable device capable of controlling the delivery of this drug for an extended period within the tumor site. Objective: To develop methotrexate-loaded poly("-caprolactone) implants (MTX PCL implants) and to demonstrate their efficacy as local drug delivery systems capable of inhibiting Ehrlich solid tumor bearing mice. Materials and methods: MTX PCL implants were produced by the melt-molding technique and were characterized by FTIR, WAXS, DSC and SEM. The in vitro and in vivo release of MTX from the PCL implants was also evaluated. The efficacy of implants in inhibiting tumor cells in culture and the solid tumor in a murine model was revealed. Results and discussion: The chemical and morphological integrity of the drug was preserved into the polymeric matrix. The in vitro and in vivo release processes of the MTX from the PCL implants were modulated by diffusion. MTX diffused from the implants revealed an antiproliferative effect on tumor cells. Finally, MTX controlled and sustained released from the polymeric implants efficiently reduced 42.7% of the solid tumor in mice paw. Conclusion: These implantable devices represented a contribution to improve the efficacy and safety of chemotherapy treatments, promoting long-term local drug accumulation in the targeted site.

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Section: Introductionmentioning

confidence: 99%

Efficacy of methotrexate-loaded poly(ε-caprolactone) implants in Ehrlich solid tumor-bearing mice

Pereira

Barbosa

et al. 2013

Drug Delivery

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“…Analisando os resultados da Tabela 1, pode-se afirmar que o processo de degradação "in vitro" influencia a perda de massa molar do dispositivo da seguinte forma: nas 2 primeiras semanas de estudo já é possível notar uma discreta diminuição no valor da massa molar; transcorridas 8 De maneira geral, tanto a massa molar ponderal média (Mw) como a massa molar numérica (Mn) são os parâmetros mais sensíveis para o estudo da degradação "in vitro" dessa classe de polímeros bioreabsorviveis [9]. A queda do tamanho das cadeias (M w ) é acompanhada pela queda no número de cadeias (M n ) ao longo do processo de degradação.…”

Section: Resultsunclassified

“…A queda do tamanho das cadeias (M w ) é acompanhada pela queda no número de cadeias (M n ) ao longo do processo de degradação. O perfil de queda de massa molar apresentado pelo copolímero PLDLA foi compatível com um estudo realizado por Lemmouchi et al [9], em que foi verificado o comportamento de queda de massa molar em função do tempo de degradação para vários materiais poliméricos. Leenslag et al [10] relacionam a queda inicial da massa molar, no processo de hidrólise dos poliésteres alifáticos, à degradação preferencial que as regiões amorfas apresentam durante a entrada das moléculas de água nas cadeias do polímero, sendo verificado ainda por Lemmouchi et al [9] que a queda da massa molar de um copolímero da família dos poliésteres alifáticos se mostra mais intensa quanto maior for a concentração de partes amorfas DL-lactide em sua seqüência.…”

Section: Resultsunclassified

Estudo inicial da degradação "in vitro" de poli (L-co-DL ácido lático) sintetizado em laboratório

Duek

2008

Matéria (Rio J.)

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RESUMOO copolímero poli (L-co-DL ácido lático), PLDLA, tem se destacado no campo das próteses temporárias, porque o seu tempo de degradação é bastante compatível com aquele requerido no caso de fraturas ósseas. Neste trabalho, estudou-se a degradação "in vitro" de dispositivos processados na forma de placas do copolímero PLDLA sintetizado em laboratório. As placas do PLDLA foram imersas numa solução tampão fosfato (pH = 7,4) em um banho termostatizado a 37 o C ± 1 o C, durante especificados períodos (0, 2, 4, 8, 16, e 30 semanas), e avaliadas pelas seguintes técnicas: cromatografia de permeação em gel (GPC), calorimetria diferencial de varredura (DSC), microscopia eletrônica de varredura (MEV) e ensaios de flexão por três pontos. Foi observado, através do estudo "in vitro", que o processo de degradação afeta a massa molecular desde a segunda semana de estudo. As análises das curvas de DSC demonstram que o material, inicialmente amorfo, apresenta vestígios de cristalinidade durante o processo de degradação, enquanto que as análises de TGA demonstram que a estabilidade térmica do copolímero só é afetada após 16 semanas de estudo. A análise por meio de MEV mostrou que o dispositivo passa de denso para poroso após 18 semanas de estudo "in vitro". O ensaio de resistência à flexão mostrou que o copolímero consegue reter mais de 80 % de sua resistência após período de 4 meses de imersão, um resultado bastante compatível com aquele requerido para consolidação óssea. Palavras-chaves: Síntese, PLDLA, degradação in vitro. In vitro initial study degradation of poly (L-co-DL lactide acid) synthesized in laboratory ABSTRACTThe poly (L-co-DL lactic acid) copolymer, PLDLA, has achieved outstanding position in the temporary prostheses because its degradation life is up to goog extent compatible with the requirement for the bone fracture repair. In vitro degradation of the in-Lab synthesized PLDLA was studied. The PLDLA plates were immersed in a phosphate buffer solution with pH = 7,4 at 37 o C +-1 o C provided by a thermostat controlled bath for specified test times (2, 4, 8, 16 and 30 weeks) and evaluated by using the following techniques: gel permeation chromatography (GPC), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and three point flexural strength test. From in vitro test, it was found that change in the PLDLA molecular weight due to its degradation is already noticeable since the second test-week. The initially amorphous PLDLA presented traces of cristalline signs according to DSC curves, while the thermal stability of the copolymer is affected only after 16 test-weeks as shown by TGA results. The change of PLDLA pieces from dense to porous took 18 in-vitro test-weeks as revealed by SEM. After four test months, PLDLA was capable of retaining more than 80% of its original three-point flexural strengh, which is up to good extent compatible with the requirements for bone consolidation.

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“…In last few years, PCL have become a major area of research in order to develop controlled drug delivery systems mainly used for proteins and peptides 102 . Lemmouchi and his co-workers have studied the in-vivo and in-vitro release of the drugs that have selected such as isometamidium chloride and ethidium bromide from the rods made up of poly caprolactone-poly L-lactic acid (PCL-PLLA), poly caprolactone-poly D-lactic acid (PCL-DLLA) and PCL-TMC 103 .…”

Section: Synthesis Of Pclmentioning

confidence: 99%

Untitled

2018

IJPSR

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Biodegradable polyesters for controlled release of trypanocidal drugs: In vitro and in vivo studies

Cited by 77 publications

References 26 publications

Efficacy of methotrexate-loaded poly(ε-caprolactone) implants in Ehrlich solid tumor-bearing mice

Efficacy of methotrexate-loaded poly(ε-caprolactone) implants in Ehrlich solid tumor-bearing mice

Estudo inicial da degradação "in vitro" de poli (L-co-DL ácido lático) sintetizado em laboratório

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